PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 17953471-3 2007 Repaglinide is an insulin secretagogue that lowers blood glucose levels in patients with T2DM. repaglinide 0-11 insulin Homo sapiens 18-25 16513447-0 2006 Telithromycin, but not montelukast, increases the plasma concentrations and effects of the cytochrome P450 3A4 and 2C8 substrate repaglinide. repaglinide 129-140 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-118 17253883-8 2007 In addition to CYP3A4, repaglinide is metabolised via CYP2C8, while nateglinide metabolism also involves CYP2C9. repaglinide 23-34 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 54-60 17253883-15 2007 The most impressive pharmacokinetic interaction was reported with combined administration of gemfibrozil (a strong CYP2C8 inhibitor) and repaglinide (8-fold increase in repaglinide AUC). repaglinide 137-148 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 115-121 16796707-2 2006 A recent study showed that SLCO1B1 (which codes the OATP1B1 gene, also known as OATP-C, OATP2) is a major determinant which markedly affects the pharmacokinetics of repaglinide. repaglinide 165-176 solute carrier organic anion transporter family member 1B1 Homo sapiens 27-34 16796707-2 2006 A recent study showed that SLCO1B1 (which codes the OATP1B1 gene, also known as OATP-C, OATP2) is a major determinant which markedly affects the pharmacokinetics of repaglinide. repaglinide 165-176 solute carrier organic anion transporter family member 1B1 Homo sapiens 52-59 16796707-2 2006 A recent study showed that SLCO1B1 (which codes the OATP1B1 gene, also known as OATP-C, OATP2) is a major determinant which markedly affects the pharmacokinetics of repaglinide. repaglinide 165-176 solute carrier organic anion transporter family member 1B1 Homo sapiens 80-86 16796707-2 2006 A recent study showed that SLCO1B1 (which codes the OATP1B1 gene, also known as OATP-C, OATP2) is a major determinant which markedly affects the pharmacokinetics of repaglinide. repaglinide 165-176 solute carrier organic anion transporter family member 1B1 Homo sapiens 88-93 16865362-0 2006 Selectivity of repaglinide and glibenclamide for the pancreatic over the cardiovascular K(ATP) channels. repaglinide 15-26 ATPase phospholipid transporting 8A2 Homo sapiens 90-93 16865362-2 2006 The insulinotrope repaglinide is successful in therapy, but has been reported to inhibit the recombinant K(ATP) channels of beta cells, cardiocytes and non-vascular smooth muscle cells with similar potencies, suggesting that the (patho-)physiological role of the cardiovascular K(ATP) channels may be overstated. repaglinide 18-29 ATPase phospholipid transporting 8A2 Homo sapiens 107-110 16865362-2 2006 The insulinotrope repaglinide is successful in therapy, but has been reported to inhibit the recombinant K(ATP) channels of beta cells, cardiocytes and non-vascular smooth muscle cells with similar potencies, suggesting that the (patho-)physiological role of the cardiovascular K(ATP) channels may be overstated. repaglinide 18-29 ATPase phospholipid transporting 8A2 Homo sapiens 280-283 16865362-3 2006 We therefore re-examined repaglinide"s potency at and affinity for the recombinant pancreatic, myocardial and vascular K(ATP) channels in comparison with glibenclamide. repaglinide 25-36 ATPase phospholipid transporting 8A2 Homo sapiens 110-125 16865362-8 2006 CONCLUSIONS/INTERPRETATION: Repaglinide and glibenclamide show higher potency and efficacy in inhibiting the pancreatic than the cardiovascular K(ATP) channels, thus supporting their clinical use. repaglinide 28-39 ATPase phospholipid transporting 8A2 Homo sapiens 146-149 17211567-0 2006 Preprandial repaglinide decreases exogenous insulin requirements and HbA1c levels in type 2 diabetic patients taking intensive insulin treatment. repaglinide 12-23 insulin Homo sapiens 44-51 17211567-0 2006 Preprandial repaglinide decreases exogenous insulin requirements and HbA1c levels in type 2 diabetic patients taking intensive insulin treatment. repaglinide 12-23 insulin Homo sapiens 127-134 17211567-1 2006 In this study, we investigated the effects of combining preprandial repaglinide to the insulin therapy for reducing the exogenous insulin requirements and serum HbA(1c) levels in type 2 diabetic patients whose blood glucose levels were previously regulated by multiple dose intensive insulin therapy. repaglinide 68-79 insulin Homo sapiens 130-137 17211567-1 2006 In this study, we investigated the effects of combining preprandial repaglinide to the insulin therapy for reducing the exogenous insulin requirements and serum HbA(1c) levels in type 2 diabetic patients whose blood glucose levels were previously regulated by multiple dose intensive insulin therapy. repaglinide 68-79 insulin Homo sapiens 130-137 17211567-9 2006 A significant reduction regarding exogenous insulin requirements and serum HbA(1c) levels were demonstrated in patients taking preprandial repaglinide (p<0.01). repaglinide 139-150 insulin Homo sapiens 44-51 16539642-1 2006 The purpose of this study was to investigate the use of the short-acting insulin secretion drug repaglinide in new-onset diabetes mellitus (NODM) after renal transplantation. repaglinide 96-107 insulin Homo sapiens 73-80 16513447-1 2006 BACKGROUND AND OBJECTIVE: The antidiabetic repaglinide is metabolized by cytochrome P450 (CYP) 2C8 and CYP3A4. repaglinide 43-54 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 73-98 16513447-1 2006 BACKGROUND AND OBJECTIVE: The antidiabetic repaglinide is metabolized by cytochrome P450 (CYP) 2C8 and CYP3A4. repaglinide 43-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-109 16513447-12 2006 CONCLUSIONS: Telithromycin increases the plasma concentrations and blood glucose-lowering effect of repaglinide by inhibiting its CYP3A4-catalyzed biotransformation and may increase the risk of hypoglycemia. repaglinide 100-111 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 130-136 16176562-0 2005 Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: effect of fibrates and rifampicin. repaglinide 14-25 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 29-35 16447051-2 2006 Repaglinide, a meglitinide analogue antidiabetic, is metabolised by CYP2C8 and CYP3A4. repaglinide 0-11 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 68-74 16447051-2 2006 Repaglinide, a meglitinide analogue antidiabetic, is metabolised by CYP2C8 and CYP3A4. repaglinide 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 79-85 16299161-9 2006 The results described have important implications for the mechanism of the clinical interaction reported between gemfibrozil and CYP2C8 substrates such as cerivastatin, repaglinide, rosiglitazone, and pioglitazone. repaglinide 169-180 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 129-135 16176562-5 2005 At therapeutic repaglinide concentrations (<0.4 microM), CYP2C8 and CYP3A4 metabolised repaglinide at similar rates. repaglinide 15-26 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 60-66 16433710-5 2006 RESULTS: Adenosine diphosphate (ADP)-induced platelet P-selectin expression increased post-meal in Type 2 diabetic patients both at baseline and after treatment with repaglinide and glibenclamide (P < 0.01 for all; repeated measures anova). repaglinide 166-177 selectin P Homo sapiens 54-64 16433710-6 2006 Repaglinide treatment reduced fasting ADP-induced P-selectin expression compared with baseline (P = 0.01), but did not influence meal-induced platelet hyper-reactivity (P = 0.32). repaglinide 0-11 selectin P Homo sapiens 50-60 16433710-8 2006 Plasma concentrations of VWF and ICAM-1 were elevated in patients with Type 2 diabetes compared with control subjects (P < 0.05 for both) and were reduced during treatment with repaglinide (P < 0.01 for both) but did not change during glibenclamide treatment. repaglinide 180-191 von Willebrand factor Homo sapiens 25-28 16433710-8 2006 Plasma concentrations of VWF and ICAM-1 were elevated in patients with Type 2 diabetes compared with control subjects (P < 0.05 for both) and were reduced during treatment with repaglinide (P < 0.01 for both) but did not change during glibenclamide treatment. repaglinide 180-191 intercellular adhesion molecule 1 Homo sapiens 33-39 16475928-4 2006 Blockers of Kir6.2/SUR1 channels, e.g. glibenclamide and repaglinide stimulate release of insulin and are used for treatment of type 2 diabetes. repaglinide 57-68 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 12-18 16475928-4 2006 Blockers of Kir6.2/SUR1 channels, e.g. glibenclamide and repaglinide stimulate release of insulin and are used for treatment of type 2 diabetes. repaglinide 57-68 ATP binding cassette subfamily C member 8 Homo sapiens 19-23 16475928-4 2006 Blockers of Kir6.2/SUR1 channels, e.g. glibenclamide and repaglinide stimulate release of insulin and are used for treatment of type 2 diabetes. repaglinide 57-68 insulin Homo sapiens 90-97 16176562-5 2005 At therapeutic repaglinide concentrations (<0.4 microM), CYP2C8 and CYP3A4 metabolised repaglinide at similar rates. repaglinide 90-101 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 60-66 16176562-5 2005 At therapeutic repaglinide concentrations (<0.4 microM), CYP2C8 and CYP3A4 metabolised repaglinide at similar rates. repaglinide 90-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 16176562-9 2005 In conclusion, both CYP2C8 and CYP3A4 are important in the metabolism of therapeutic concentrations of repaglinide in vitro, but their predicted contributions in vivo are highly dependent on the scaling factor used. repaglinide 103-114 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 20-26 16176562-9 2005 In conclusion, both CYP2C8 and CYP3A4 are important in the metabolism of therapeutic concentrations of repaglinide in vitro, but their predicted contributions in vivo are highly dependent on the scaling factor used. repaglinide 103-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 16176562-0 2005 Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: effect of fibrates and rifampicin. repaglinide 14-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-46 16176562-1 2005 Repaglinide is an antidiabetic drug metabolised by cytochrome P450 (CYP) 2C8 and CYP3A4 enzymes. repaglinide 0-11 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 51-76 16176562-1 2005 Repaglinide is an antidiabetic drug metabolised by cytochrome P450 (CYP) 2C8 and CYP3A4 enzymes. repaglinide 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 16176562-3 2005 We studied repaglinide metabolism using pooled human liver microsomes, recombinant CYP2C8 and recombinant CYP3A4 enzymes. repaglinide 11-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-112 16142016-7 2005 Analysis of the insulin and glucose concentrations throughout the meal test revealed that AUC for glucose (758 +/- 19 vs 780 +/- 28 mg/Lxmin; P = 0.02) was significantly lower after repaglinide than glimepiride administration despite similar AUC for insulin (2327 +/- 269 vs 2148 +/- 292 mU/Lxmin; P = 0.105). repaglinide 182-193 insulin Homo sapiens 16-23 16198658-1 2005 BACKGROUND AND OBJECTIVE: Repaglinide is an antidiabetic drug metabolized by cytochrome P450 (CYP) 2 C 8 and 3A4, and it appears to be a substrate of the hepatic uptake transporter organic anion transporting polypeptide 1B1 (OATP1B1). repaglinide 26-37 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 77-104 16198658-1 2005 BACKGROUND AND OBJECTIVE: Repaglinide is an antidiabetic drug metabolized by cytochrome P450 (CYP) 2 C 8 and 3A4, and it appears to be a substrate of the hepatic uptake transporter organic anion transporting polypeptide 1B1 (OATP1B1). repaglinide 26-37 solute carrier organic anion transporter family member 1B1 Homo sapiens 225-232 16198658-13 2005 The effect of cyclosporine on repaglinide AUC0-infinity was 42% lower in subjects with the SLCO1B1 521TC genotype than in subjects with the 521TT (reference) genotype (P=.047). repaglinide 30-41 solute carrier organic anion transporter family member 1B1 Homo sapiens 91-98 16198658-15 2005 CONCLUSIONS: Cyclosporine raised the plasma concentrations of repaglinide, probably by inhibiting its CYP3A4-catalyzed biotransformation and OATP1B1-mediated hepatic uptake. repaglinide 62-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 16198658-15 2005 CONCLUSIONS: Cyclosporine raised the plasma concentrations of repaglinide, probably by inhibiting its CYP3A4-catalyzed biotransformation and OATP1B1-mediated hepatic uptake. repaglinide 62-73 solute carrier organic anion transporter family member 1B1 Homo sapiens 141-148 16176204-0 2005 Repaglinide treatment amplifies first-phase insulin secretion and high-frequency pulsatile insulin release in Type 2 diabetes. repaglinide 0-11 insulin Homo sapiens 44-51 16176204-2 2005 The present study was undertaken to explore a possible influence of the oral prandial glucose regulator, repaglinide, on first-phase insulin secretion and high-frequency insulin pulsatility in Type 2 diabetes. repaglinide 105-116 insulin Homo sapiens 133-140 16176204-10 2005 In addition, glucose entrained insulin secretory burst mass and amplitude increased markedly (burst mass: repaglinide, 44.4 +/- 6.0 pmol/l/pulse vs. placebo, 31.4 +/- 3.3 pmol/l/pulse, P < 0.05; burst amplitude: repaglinide, 17.7 +/- 2.4 pmol/l/min vs. placebo, 12.6 +/- 1.3 pmol/l/min, P < 0.05) while basal insulin (non-pulsatile) secretion was unaltered. repaglinide 106-117 insulin Homo sapiens 31-38 16176204-10 2005 In addition, glucose entrained insulin secretory burst mass and amplitude increased markedly (burst mass: repaglinide, 44.4 +/- 6.0 pmol/l/pulse vs. placebo, 31.4 +/- 3.3 pmol/l/pulse, P < 0.05; burst amplitude: repaglinide, 17.7 +/- 2.4 pmol/l/min vs. placebo, 12.6 +/- 1.3 pmol/l/min, P < 0.05) while basal insulin (non-pulsatile) secretion was unaltered. repaglinide 215-226 insulin Homo sapiens 31-38 16176204-11 2005 After acute repaglinide exposure (0.5 mg) basal insulin secretion increased significantly (P < 0.05). repaglinide 12-23 insulin Homo sapiens 48-55 16176204-13 2005 CONCLUSION/INTERPRETATION: Repaglinide augments first-phase insulin secretion as well as high-frequency insulin secretory burst mass and amplitude during glucose entrainment in patients with Type 2 diabetes, while regularity of the insulin release process was unaltered. repaglinide 27-38 insulin Homo sapiens 60-67 15944840-3 2005 Catalase activity was significantly increased in diabetic liver (67.5+/-3.6 vs. 39.7+/-5.6 and 62.3+/-2.7 vs. 52.6+/-5.3 micromol H(2)O(2)/min/mg protein) and normalised by repaglinide (49.2+/-4.0 and 41.2+/-3.8 micromol H(2)O(2)/min/mg protein). repaglinide 173-184 catalase Oryctolagus cuniculus 0-8 16142016-4 2005 Lowering in plasma PAI-1 and PAP levels was significantly greater in repaglinide group. repaglinide 69-80 serpin family E member 1 Homo sapiens 19-24 16142016-5 2005 Furthermore, repaglinide administration resulted in a significant decrease in fasting plasma free fatty acids, fibrinogen, thrombin-antithrombin complex and reaction product of malondialdehyde with thiobarbituric acid (TBARS) levels, in absence of significant difference in fasting plasma insulin levels. repaglinide 13-24 fibrinogen beta chain Homo sapiens 111-121 16142016-5 2005 Furthermore, repaglinide administration resulted in a significant decrease in fasting plasma free fatty acids, fibrinogen, thrombin-antithrombin complex and reaction product of malondialdehyde with thiobarbituric acid (TBARS) levels, in absence of significant difference in fasting plasma insulin levels. repaglinide 13-24 coagulation factor II, thrombin Homo sapiens 123-131 16142016-7 2005 Analysis of the insulin and glucose concentrations throughout the meal test revealed that AUC for glucose (758 +/- 19 vs 780 +/- 28 mg/Lxmin; P = 0.02) was significantly lower after repaglinide than glimepiride administration despite similar AUC for insulin (2327 +/- 269 vs 2148 +/- 292 mU/Lxmin; P = 0.105). repaglinide 182-193 insulin Homo sapiens 250-257 16142016-5 2005 Furthermore, repaglinide administration resulted in a significant decrease in fasting plasma free fatty acids, fibrinogen, thrombin-antithrombin complex and reaction product of malondialdehyde with thiobarbituric acid (TBARS) levels, in absence of significant difference in fasting plasma insulin levels. repaglinide 13-24 serpin family C member 1 Homo sapiens 132-144 16142016-5 2005 Furthermore, repaglinide administration resulted in a significant decrease in fasting plasma free fatty acids, fibrinogen, thrombin-antithrombin complex and reaction product of malondialdehyde with thiobarbituric acid (TBARS) levels, in absence of significant difference in fasting plasma insulin levels. repaglinide 13-24 insulin Homo sapiens 289-296 16142016-8 2005 At time 120" of meal test, repaglinide vs glimepiride administration was associated with a significant decline in plasma triglycerides, free fatty acids, fibrinogen, Plasminogen Activator Inhibitor-1, plasmin-alpha(2)-antiplasmin complex, thrombin-antithrombin complex, TBARS levels and increase in plasma HDL-cholesterol levels. repaglinide 27-38 fibrinogen beta chain Homo sapiens 154-164 16142016-8 2005 At time 120" of meal test, repaglinide vs glimepiride administration was associated with a significant decline in plasma triglycerides, free fatty acids, fibrinogen, Plasminogen Activator Inhibitor-1, plasmin-alpha(2)-antiplasmin complex, thrombin-antithrombin complex, TBARS levels and increase in plasma HDL-cholesterol levels. repaglinide 27-38 serpin family E member 1 Homo sapiens 166-199 16142016-8 2005 At time 120" of meal test, repaglinide vs glimepiride administration was associated with a significant decline in plasma triglycerides, free fatty acids, fibrinogen, Plasminogen Activator Inhibitor-1, plasmin-alpha(2)-antiplasmin complex, thrombin-antithrombin complex, TBARS levels and increase in plasma HDL-cholesterol levels. repaglinide 27-38 coagulation factor II, thrombin Homo sapiens 239-247 16142016-8 2005 At time 120" of meal test, repaglinide vs glimepiride administration was associated with a significant decline in plasma triglycerides, free fatty acids, fibrinogen, Plasminogen Activator Inhibitor-1, plasmin-alpha(2)-antiplasmin complex, thrombin-antithrombin complex, TBARS levels and increase in plasma HDL-cholesterol levels. repaglinide 27-38 serpin family C member 1 Homo sapiens 248-260 16142016-9 2005 In repaglinide group a negative correlation between insulin secretion during 1st phase of meal-test and plasma TBARS levels (r = -0.55; P < 0.03) at time 120" was found. repaglinide 3-14 insulin Homo sapiens 52-59 15938025-9 2005 In chronic renal failure, the oral agents that can be used therefore include the insulin secretagogues repaglinide and nateglinide and the thiazolidinediones (rosiglitazone and pioglitazone) with caution. repaglinide 103-114 insulin Homo sapiens 81-88 20496449-4 2005 Two other oral antidiabetic drugs that work by stimulating insulin secretion, repaglinide and nateglinide, are available in the U.S. repaglinide 78-89 insulin Homo sapiens 59-66 15855557-1 2005 OBJECTIVE: To assess the effects of incremental doses of repaglinide on postprandial insulin and glucose profiles after a standard 500-kcal test meal. repaglinide 57-68 insulin Homo sapiens 85-92 15855557-6 2005 Proinsulin-to-insulin ratios at 30 and 60 min improved with increasing doses of repaglinide; higher drug doses (2 and 4 mg) were more effective than the 0.5- and 1-mg doses. repaglinide 80-91 insulin Homo sapiens 0-10 15855557-6 2005 Proinsulin-to-insulin ratios at 30 and 60 min improved with increasing doses of repaglinide; higher drug doses (2 and 4 mg) were more effective than the 0.5- and 1-mg doses. repaglinide 80-91 insulin Homo sapiens 3-10 15846457-8 2005 The antidiabetic repaglinide and HMG CoA reductase inhibitor fluvastatin were found to inhibit hPEPT1 with sub-millimolar potency (IC(50) 178 +/- 1.0 and 337 +/- 4 microM, respectively). repaglinide 17-28 solute carrier family 15 member 1 Homo sapiens 95-101 15678092-0 2005 Kir6.2-dependent high-affinity repaglinide binding to beta-cell K(ATP) channels. repaglinide 31-42 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 0-6 15678092-15 2005 The results suggest that Kir6.2 causes a conformational change in SUR1 required for high-affinity repaglinide binding, or that the high-affinity repaglinide-binding site includes contributions from both SUR1 and Kir6.2. repaglinide 98-109 ATP binding cassette subfamily C member 8 Homo sapiens 66-70 15678092-15 2005 The results suggest that Kir6.2 causes a conformational change in SUR1 required for high-affinity repaglinide binding, or that the high-affinity repaglinide-binding site includes contributions from both SUR1 and Kir6.2. repaglinide 145-156 ATP binding cassette subfamily C member 8 Homo sapiens 203-207 15678092-4 2005 In this study, we investigate the interaction of the hypoglycaemic agents repaglinide and glibenclamide with SUR1 and the effect of Kir6.2 on this interaction. repaglinide 74-85 ATP binding cassette subfamily C member 8 Homo sapiens 109-113 15678092-5 2005 We further explore how the binding properties of repaglinide and glibenclamide are affected by functional uncoupling of SUR1 and Kir6.2 in Kir6.2DeltaN14/SUR1 channels. repaglinide 49-60 ATP binding cassette subfamily C member 8 Homo sapiens 120-124 15678092-5 2005 We further explore how the binding properties of repaglinide and glibenclamide are affected by functional uncoupling of SUR1 and Kir6.2 in Kir6.2DeltaN14/SUR1 channels. repaglinide 49-60 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 129-135 15678092-5 2005 We further explore how the binding properties of repaglinide and glibenclamide are affected by functional uncoupling of SUR1 and Kir6.2 in Kir6.2DeltaN14/SUR1 channels. repaglinide 49-60 ATP binding cassette subfamily C member 8 Homo sapiens 154-158 15678092-7 2005 Repaglinide was found to bind with low affinity (K(D)=59+/-16 nM) to SUR1 alone, but with high affinity (increased approximately 150-fold) when SUR1 was co-expressed with Kir6.2 (K(D)=0.42+/-0.03 nM). repaglinide 0-11 ATP binding cassette subfamily C member 8 Homo sapiens 69-73 15678092-7 2005 Repaglinide was found to bind with low affinity (K(D)=59+/-16 nM) to SUR1 alone, but with high affinity (increased approximately 150-fold) when SUR1 was co-expressed with Kir6.2 (K(D)=0.42+/-0.03 nM). repaglinide 0-11 ATP binding cassette subfamily C member 8 Homo sapiens 144-148 15678092-7 2005 Repaglinide was found to bind with low affinity (K(D)=59+/-16 nM) to SUR1 alone, but with high affinity (increased approximately 150-fold) when SUR1 was co-expressed with Kir6.2 (K(D)=0.42+/-0.03 nM). repaglinide 0-11 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 171-177 15678092-10 2005 Repaglinide bound with low affinity (K(D)=51+/-23 nM) to SUR1 co-expressed with Kir6.2DeltaN14. repaglinide 0-11 ATP binding cassette subfamily C member 8 Homo sapiens 57-61 15678092-13 2005 In whole-cell patch-clamp experiments inhibition of Kir6.2DeltaN14/SUR1 currents by both repaglinide and nateglinde is abolished. repaglinide 89-100 ATP binding cassette subfamily C member 8 Homo sapiens 67-71 16372821-12 2005 Repaglinide is metabolised by CYP2C8 and, according to clinical studies, CYP2C8*3 carriers had higher clearance than carriers of the wild-type genotypes; however, this was not consistent with in vitro data and therefore further studies are needed. repaglinide 0-11 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 30-36 15729954-1 2005 BACKGROUND: Repaglinide, a new insulin secretagogue, is purported to be as effective as sulphonylurea but is less hypoglycemic-prone. repaglinide 12-23 insulin Homo sapiens 31-38 16372821-12 2005 Repaglinide is metabolised by CYP2C8 and, according to clinical studies, CYP2C8*3 carriers had higher clearance than carriers of the wild-type genotypes; however, this was not consistent with in vitro data and therefore further studies are needed. repaglinide 0-11 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 73-79 15294453-8 2004 Taurine at the concentration of 10 mM enhanced the high-affinity bindings of glibenclamide and repaglinide on all types of SUR, whereas the low-affinity binding on Kir6.2 was not affected. repaglinide 95-106 ATP binding cassette subfamily C member 8 Rattus norvegicus 123-126 15601807-1 2005 Cytochrome P450 2C8 is involved in the metabolism of drugs such as paclitaxel, repaglinide, rosiglitazone, and cerivastatin, among others. repaglinide 79-90 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 0-19 15386823-7 2004 While initially quite similar, in the period from 240 to 300 min, insulin, proinsulin and C-peptide levels were lower during repaglinide treatment (insulin 133 +/- 20 vs 153 +/- 25 pmol L(-1) (P < 0.05), proinsulin 14 +/- 3 vs 19 +/- 4 pmol L(-1) (P = 0.06) and C-peptide 0.81 +/- 0.19 vs 1.14 +/- 0.18 nmol L(-1) (P = 0.05) for repaglinide vs glibenclamide, respectively). repaglinide 125-136 insulin Homo sapiens 66-73 15386823-7 2004 While initially quite similar, in the period from 240 to 300 min, insulin, proinsulin and C-peptide levels were lower during repaglinide treatment (insulin 133 +/- 20 vs 153 +/- 25 pmol L(-1) (P < 0.05), proinsulin 14 +/- 3 vs 19 +/- 4 pmol L(-1) (P = 0.06) and C-peptide 0.81 +/- 0.19 vs 1.14 +/- 0.18 nmol L(-1) (P = 0.05) for repaglinide vs glibenclamide, respectively). repaglinide 125-136 insulin Homo sapiens 75-85 15386823-7 2004 While initially quite similar, in the period from 240 to 300 min, insulin, proinsulin and C-peptide levels were lower during repaglinide treatment (insulin 133 +/- 20 vs 153 +/- 25 pmol L(-1) (P < 0.05), proinsulin 14 +/- 3 vs 19 +/- 4 pmol L(-1) (P = 0.06) and C-peptide 0.81 +/- 0.19 vs 1.14 +/- 0.18 nmol L(-1) (P = 0.05) for repaglinide vs glibenclamide, respectively). repaglinide 125-136 insulin Homo sapiens 90-99 15386823-7 2004 While initially quite similar, in the period from 240 to 300 min, insulin, proinsulin and C-peptide levels were lower during repaglinide treatment (insulin 133 +/- 20 vs 153 +/- 25 pmol L(-1) (P < 0.05), proinsulin 14 +/- 3 vs 19 +/- 4 pmol L(-1) (P = 0.06) and C-peptide 0.81 +/- 0.19 vs 1.14 +/- 0.18 nmol L(-1) (P = 0.05) for repaglinide vs glibenclamide, respectively). repaglinide 125-136 insulin Homo sapiens 78-85 15386823-7 2004 While initially quite similar, in the period from 240 to 300 min, insulin, proinsulin and C-peptide levels were lower during repaglinide treatment (insulin 133 +/- 20 vs 153 +/- 25 pmol L(-1) (P < 0.05), proinsulin 14 +/- 3 vs 19 +/- 4 pmol L(-1) (P = 0.06) and C-peptide 0.81 +/- 0.19 vs 1.14 +/- 0.18 nmol L(-1) (P = 0.05) for repaglinide vs glibenclamide, respectively). repaglinide 125-136 insulin Homo sapiens 207-217 15386823-7 2004 While initially quite similar, in the period from 240 to 300 min, insulin, proinsulin and C-peptide levels were lower during repaglinide treatment (insulin 133 +/- 20 vs 153 +/- 25 pmol L(-1) (P < 0.05), proinsulin 14 +/- 3 vs 19 +/- 4 pmol L(-1) (P = 0.06) and C-peptide 0.81 +/- 0.19 vs 1.14 +/- 0.18 nmol L(-1) (P = 0.05) for repaglinide vs glibenclamide, respectively). repaglinide 125-136 insulin Homo sapiens 265-274 15386823-8 2004 CONCLUSIONS: Following glucose stimulation, plasma glucose levels, and insulin concentration decrease more rapidly after repaglinide treatment than after glibenclamide. repaglinide 121-132 insulin Homo sapiens 71-78 15197140-8 2004 CIMT regression, defined as a decrease of >0.020 mm, was observed in 52% of diabetics receiving repaglinide and in 18% of those receiving glyburide (P<0.01). repaglinide 99-110 CIMT Homo sapiens 0-4 15324515-4 2004 At the end of the study, changes in HbA1c from baseline were -1.28% points and -0.67% points for repaglinide/metformin and nateglinide/metformin, respectively. repaglinide 97-108 hemoglobin subunit alpha 1 Homo sapiens 36-40 15197140-9 2004 Interleukin-6 (P=0.04) and C-reactive protein (P=0.02) decreased more in the repaglinide group than in the glyburide group. repaglinide 77-88 interleukin 6 Homo sapiens 0-13 15197140-9 2004 Interleukin-6 (P=0.04) and C-reactive protein (P=0.02) decreased more in the repaglinide group than in the glyburide group. repaglinide 77-88 C-reactive protein Homo sapiens 27-45 12817528-6 2003 Concomitant treatment with CYP3A4 substrates altered mean AUC0-5 h and mean Cmax for repaglinide by 1% and 17% (ethinyloestradiol/levonorgestrel), 2% and 27% (simvastatin), or 11% and 3% (nifedipine). repaglinide 85-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 15334790-1 2004 This study was designed to compare the effects of repaglinide plus acarbose combination treatment to repaglinide alone on postprandial glucose, serum insulin, C-peptide and proinsulin concentrations. repaglinide 50-61 insulin Homo sapiens 173-183 15099124-26 2004 Repaglinide, a meglitinide analogue, is an oral insulin secretagogue that reduces postprandial glucose excursions by targeting postprandial insulin release. repaglinide 0-11 insulin Homo sapiens 48-55 15099124-31 2004 In general, results showed statistically significant improvements in glycaemic control when repaglinide was used in combination with metformin, various thiazolidinediones, or metformin plus bedtime insulin compared with monotherapy with either comparator drug in each study (or metformin plus bedtime insulin in one trial). repaglinide 92-103 insulin Homo sapiens 301-308 15099124-40 2004 Repaglinide is metabolised by the cytochrome P450 (CYP) 3A4 enzyme system and therefore has the potential to interact with other CYP3A4 substrates when administered concurrently. repaglinide 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 14632720-10 2003 Both treatments were associated with significant improvements in Diabetes Treatment Satisfaction [Diabetes Treatment Satisfaction Questionnaire-potential range 0 (min) to 36 (max)]; in the insulin/gliclazide group, by 4.9 +/- 1.1 points to 33.3 +/- 0.6 (P<0.0001) and by 3.0 +/- 0.9 points to 34.6 +/- 0.4 (P=0.0006) in the insulin/repaglinide group (P=0.29 between groups). repaglinide 335-346 insulin Homo sapiens 189-196 14614647-9 2003 Nateglinide and repaglinide as short-acting insulin secretagogues may be associated with a reduced risk of hypoglycaemia compared with glibenclamide, in particular when dosed flexibly. repaglinide 16-27 insulin Homo sapiens 44-51 12919179-0 2003 CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. repaglinide 121-132 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 0-6 12919179-0 2003 CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. repaglinide 121-132 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 11-17 12919179-0 2003 CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. repaglinide 121-132 insulin Homo sapiens 100-107 12919179-1 2003 AIMS: To identify the principal human cytochrome P450 (CYP) enzyme(s) responsible for the human in vitro biotransformation of repaglinide. repaglinide 126-137 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 38-53 12919179-1 2003 AIMS: To identify the principal human cytochrome P450 (CYP) enzyme(s) responsible for the human in vitro biotransformation of repaglinide. repaglinide 126-137 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 55-58 12919179-2 2003 Previous experiments have identified CYP3A4 as being mainly responsible for the in vitro metabolism of repaglinide, but the results of clinical investigations have suggested that more than one enzyme may be involved in repaglinide biotransformation. repaglinide 103-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 12919179-3 2003 METHODS: [14C]-Repaglinide was incubated with recombinant CYP and with human liver microsomes (HLM) from individual donors in the presence of inhibitory antibodies specific for individual CYP enzymes. repaglinide 15-26 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 58-61 12919179-3 2003 METHODS: [14C]-Repaglinide was incubated with recombinant CYP and with human liver microsomes (HLM) from individual donors in the presence of inhibitory antibodies specific for individual CYP enzymes. repaglinide 15-26 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 188-191 12919179-5 2003 RESULTS: CYP3A4 and CYP2C8 were found to be responsible for the conversion of repaglinide into its two primary metabolites, M4 (resulting from hydroxylation on the piperidine ring system) and M1 (an aromatic amine). repaglinide 78-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 9-15 12919179-5 2003 RESULTS: CYP3A4 and CYP2C8 were found to be responsible for the conversion of repaglinide into its two primary metabolites, M4 (resulting from hydroxylation on the piperidine ring system) and M1 (an aromatic amine). repaglinide 78-89 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 20-26 12919179-17 2003 CONCLUSIONS: The results confirm an important role for both CYP3A4 and CYP2C8 in the human in vitro biotransformation of repaglinide. repaglinide 121-132 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 12919179-17 2003 CONCLUSIONS: The results confirm an important role for both CYP3A4 and CYP2C8 in the human in vitro biotransformation of repaglinide. repaglinide 121-132 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 71-77 12919179-18 2003 This dual CYP biotransformation may have consequences for the clinical pharmacokinetics and drug-drug interactions involving repaglinide if one CYP pathway has sufficient capacity to compensate if the other is inhibited. repaglinide 125-136 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 10-13 12919179-18 2003 This dual CYP biotransformation may have consequences for the clinical pharmacokinetics and drug-drug interactions involving repaglinide if one CYP pathway has sufficient capacity to compensate if the other is inhibited. repaglinide 125-136 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 144-147 12817528-0 2003 Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide. repaglinide 131-142 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-42 12817528-1 2003 The object of this study was to analyze drug interactions between repaglinide, a short-acting insulin secretagogue, and five other drugs interacting with CYP3A4: ketoconazole, rifampicin, ethinyloestradiol/levonorgestrel (in an oral contraceptive), simvastatin, and nifedipine. repaglinide 66-77 insulin Homo sapiens 94-101 12817528-1 2003 The object of this study was to analyze drug interactions between repaglinide, a short-acting insulin secretagogue, and five other drugs interacting with CYP3A4: ketoconazole, rifampicin, ethinyloestradiol/levonorgestrel (in an oral contraceptive), simvastatin, and nifedipine. repaglinide 66-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 154-160 15239026-7 2004 The insulin sensitivity index (ISI) was increased by 35 % after 1 week of combination therapy with repaglinide plus metformin (1.11 +/- 0.03 x 10 (2) vs. 0.83 +/- 0.21 x 10 (2) mg x kg (-1) body weight x min (-1) x pmol (-1) x l, respectively; p = 0.033). repaglinide 99-110 insulin Homo sapiens 4-11 15239026-8 2004 Repaglinide increased early and late phases of insulin responses in HC, without markedly enhancing insulin secretion in euglycaemia. repaglinide 0-11 insulin Homo sapiens 47-54 15239026-9 2004 Repaglinide in combination with metformin produced a significant enhancement of ISI, suggesting a synergistic effect on insulin sensitivity. repaglinide 0-11 insulin Homo sapiens 120-127 15025742-0 2004 The CYP2C8 inhibitor trimethoprim increases the plasma concentrations of repaglinide in healthy subjects. repaglinide 73-84 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 4-10 15025742-1 2004 AIMS: Our aim was to investigate the effect of the CYP2C8 inhibitor trimethoprim on the pharmacokinetics and pharmacodynamics of the antidiabetic drug repaglinide, and to examine the influence of the former on the metabolism of the latter in vitro. repaglinide 151-162 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 51-57 15025742-10 2004 CONCLUSIONS: Trimethoprim raised the plasma concentrations of repaglinide probably by inhibiting its CYP2C8-mediated biotransformation. repaglinide 62-73 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 101-107 14715864-0 2004 The insulin secretagogues glibenclamide and repaglinide do not influence growth hormone secretion in humans but stimulate glucagon secretion during profound insulin deficiency. repaglinide 44-55 insulin Homo sapiens 4-11 14715864-2 2004 The present study was undertaken to explore in more detail a possible influence of a single dose of SU (glibenclamide) and a non-SU (repaglinide) insulin secretagogue on circulating GH dynamics. repaglinide 133-144 insulin Homo sapiens 146-153 14534525-0 2003 Polymorphism in CYP2C8 is associated with reduced plasma concentrations of repaglinide. repaglinide 75-86 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 16-22 14534525-1 2003 OBJECTIVE: Our objective was to investigate the effects of genetic polymorphisms of cytochrome P450 (CYP) 2C8 on the pharmacokinetics and pharmacodynamics of the meglitinide analog antidiabetic drug repaglinide. repaglinide 199-210 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 84-109 14534525-2 2003 METHODS: We genotyped 28 healthy volunteers who had participated in our pharmacokinetic studies on repaglinide for variant alleles of the CYP2C8 gene. repaglinide 99-110 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 138-144 14534525-9 2003 The mean AUC(0- infinity ) of repaglinide was 45% (P <.005) lower and the peak concentration in plasma was 39% lower (P <.05) in subjects with the CYP2C8*1/*3 genotype compared with those with the CYP2C8*1/*1 genotype. repaglinide 30-41 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 153-159 14534525-11 2003 CONCLUSIONS: Unexpectedly, the CYP2C8*3 variant allele was associated with reduced plasma concentrations of repaglinide. repaglinide 108-119 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 31-37 12817528-13 2003 These results are probably explained by the metabolic pathway of repaglinide that involves other enzymes than CYP3A4, reflected to some extent by a small change in repaglinide pharmacodynamics. repaglinide 65-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 12817528-14 2003 Thus, careful monitoring of blood glucose in repaglinide-treated patients receiving strong inhibitors or inducers of CYP3A4 is recommended, and an increase in repaglinide dose may be necessary. repaglinide 45-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-123 12702002-9 2002 Repaglinide, a novel prandial glucose regulator, improves the insulin secretory burst mass in healthy people. repaglinide 0-11 insulin Homo sapiens 62-69 12749508-14 2003 Repaglinide significantly lowered levels of Lp(a), PAI-1, and Hcy after 12 months (all, P < 0.05 vs baseline). repaglinide 0-11 lipoprotein(a) Homo sapiens 44-49 12749508-14 2003 Repaglinide significantly lowered levels of Lp(a), PAI-1, and Hcy after 12 months (all, P < 0.05 vs baseline). repaglinide 0-11 serpin family E member 1 Homo sapiens 51-56 12482641-10 2003 There was a significant increase after repaglinide in total serum antioxidant capacity (P<0.05) and serum SOD activity (P<0.0004); the difference compared to the control group being significant (P<0.002). repaglinide 39-50 superoxide dismutase 1 Homo sapiens 109-112 12652355-4 2003 RESULTS: Although oral administration of nateglinide and repaglinide elicited similar maximum increments of plasma insulin (+403 and +448 pmol/l, respectively), the effects of nateglinide were more rapidly manifest and less prolonged. repaglinide 57-68 insulin Macaca fascicularis 115-122 12652355-8 2003 Repaglinide increased total insulin release (AUC(0-210)=298 nmol/l min) and reduced glucose excursions by 53%. repaglinide 0-11 insulin Macaca fascicularis 28-35 12702004-7 2002 The novel insulin secretagogue repaglinide, by contrast, augments early-phase prandial insulin secretion when taken before meals, as shown by studies in non-diabetic people and patients with newly diagnosed, previously untreated T2DM. repaglinide 31-42 insulin Homo sapiens 10-17 12702004-7 2002 The novel insulin secretagogue repaglinide, by contrast, augments early-phase prandial insulin secretion when taken before meals, as shown by studies in non-diabetic people and patients with newly diagnosed, previously untreated T2DM. repaglinide 31-42 insulin Homo sapiens 87-94 12702004-0 2002 Early-phase prandial insulin secretion: its role in the pathogenesis of type 2 diabetes mellitus and its modulation by repaglinide. repaglinide 119-130 insulin Homo sapiens 21-28 12196472-1 2002 Repaglinide and nateglinide represent a new class of insulin secretagogues, structurally unrelated to sulphonylureas, that were developed for the treatment of type 2 diabetes. repaglinide 0-11 insulin Homo sapiens 53-60 12702004-8 2002 Repaglinide exerts its greatest effect on the insulin secretion rate during the first 30 min after a meal is started, thereby going some way to restoring the early insulin secretion curve seen after a meal in non-diabetic people. repaglinide 0-11 insulin Homo sapiens 46-53 12702004-8 2002 Repaglinide exerts its greatest effect on the insulin secretion rate during the first 30 min after a meal is started, thereby going some way to restoring the early insulin secretion curve seen after a meal in non-diabetic people. repaglinide 0-11 insulin Homo sapiens 164-171 12351462-9 2002 The Diabetes Treatment Satisfaction Questionnaire score (potential range 0 [minimum] to 36 [maximum]) increased from 32.4 +/- 0.8 to 34.1 +/- 0.5 (P = 0.01) with insulin/metformin but decreased from 32.5 +/- 0.9 to 29.1 +/- 1.3 (P < 0.002) with insulin/repaglinide. repaglinide 256-267 insulin Homo sapiens 162-169 12196472-3 2002 Nateglinide and repaglinide dose-dependently inhibited whole-cell Kir6.2/SUR1 currents with half-maximal inhibitory concentration (IC(50)) values of 800 and 21 nmol/l, respectively. repaglinide 16-27 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 66-72 12196472-3 2002 Nateglinide and repaglinide dose-dependently inhibited whole-cell Kir6.2/SUR1 currents with half-maximal inhibitory concentration (IC(50)) values of 800 and 21 nmol/l, respectively. repaglinide 16-27 ATP binding cassette subfamily C member 8 Homo sapiens 73-77 11194214-5 2001 RESULTS: Treatment with repaglinide significantly improved glycemic control with respect to baseline and placebo, reducing HbA1c by 1.14% from baseline and fasting plasma glucose by 1.8 mmol/l. repaglinide 24-35 hemoglobin subunit alpha 1 Homo sapiens 123-127 12073790-6 2002 A more physiological post-meal profile of insulin may be obtained in type 2 diabetes by using new insulin secretagogues of the glinide family (repaglinide, nateglinide) with an earlier and shorter insulinotropic action or, mainly in type 1 diabetes but also in type 2 diabetes, by using short-acting insulin analogues (lispro. repaglinide 143-154 insulin Homo sapiens 42-49 12073790-6 2002 A more physiological post-meal profile of insulin may be obtained in type 2 diabetes by using new insulin secretagogues of the glinide family (repaglinide, nateglinide) with an earlier and shorter insulinotropic action or, mainly in type 1 diabetes but also in type 2 diabetes, by using short-acting insulin analogues (lispro. repaglinide 143-154 insulin Homo sapiens 98-105 12073790-6 2002 A more physiological post-meal profile of insulin may be obtained in type 2 diabetes by using new insulin secretagogues of the glinide family (repaglinide, nateglinide) with an earlier and shorter insulinotropic action or, mainly in type 1 diabetes but also in type 2 diabetes, by using short-acting insulin analogues (lispro. repaglinide 143-154 insulin Homo sapiens 98-105 11815507-7 2002 RESULTS: Repaglinide increased postprandial insulin levels and markedly reduced postprandial glucose levels relative to baseline in both groups. repaglinide 9-20 insulin Homo sapiens 44-51 11574430-0 2001 Insulin and glucose excursion following premeal insulin lispro or repaglinide in cystic fibrosis-related diabetes. repaglinide 66-77 insulin Homo sapiens 0-7 11574430-1 2001 OBJECTIVE: Insulin and glucose levels in response to premeal insulin lispro or repaglinide were evaluated in adult patients with cystic fibrosis-related diabetes (CFRD) without fasting hyperglycemia. repaglinide 79-90 insulin Homo sapiens 11-18 11483229-10 2001 Test meal assessments confirmed that repaglinide effectively controls glucose levels by stimulating mealtime insulin secretion. repaglinide 37-48 insulin Homo sapiens 109-116 11483229-12 2001 Twice-daily meal-related insulin secretagogue therapy with repaglinide, a new short and rapid-acting prandial glucose regulator, is capable of improving all measures of glycaemic control without increased hypoglycaemia or fasting hyperinsulinaemia. repaglinide 59-70 insulin Homo sapiens 25-32 11440368-1 2001 AIMS/HYPOTHESIS: The carbamoylbenzoic acid derivative repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. repaglinide 54-65 insulin S homeolog Xenopus laevis 91-98 12432213-0 2002 Repaglinide: a short acting insulin secretagogue for postprandial hyperglycaemia. repaglinide 0-11 insulin Homo sapiens 28-35 12189909-9 2002 Prandial oral antidiabetic agents such as alpha-glucosidase inhibitors (acarbose, miglitol) and rapidly acting insulin secretagogues (nateglinide, repaglinide) have recently been introduced to improve the control of post-prandial hyperglycemia. repaglinide 147-158 insulin Homo sapiens 111-118 12405866-16 2002 Although there are no formal studies available, calcium channel antagonists and repaglinide may have significant interactions and toxicity when used with HIV protease inhibitors because of their metabolism by CYP3A4. repaglinide 80-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 209-215 11525087-4 2001 Repaglinide is an insulin secretion enhancer with a different mechanism of action to the sulphonylureas, which means it does not continuously stimulate insulin secretion. repaglinide 0-11 insulin Homo sapiens 18-25 11440368-8 2001 MgADP potentiated the inhibitory effect of repaglinide on Kir6.2/SUR1 and (to a lesser extent) Kir6.2/SUR2B, but not on Kir6.2/SUR2A. repaglinide 43-54 ATP-binding cassette sub-family C member 8 Xenopus laevis 65-69 11472451-8 2001 Change in HbA1c from baseline was significantly better with repaglinide than with glipizide after 12 months (P < 0.05). repaglinide 60-71 hemoglobin subunit alpha 1 Homo sapiens 10-14 11194245-8 2001 After 2 mg repaglinide, peak insulin concentrations were delayed and returned to baseline more slowly than with nateglinide treatment. repaglinide 11-22 insulin Homo sapiens 29-36 11577798-2 2001 Like the sulphonylureas, repaglinide reduces blood glucose by stimulating insulin release from pancreatic beta-cells, but differs from these and other antidiabetic agents in its structure, binding profile, duration of action and mode of excretion. repaglinide 25-36 insulin Homo sapiens 74-81 11577798-7 2001 Repaglinide showed additive effects when used in combination with other oral antidiabetic agents including metformin, troglitazone, rosiglitazone and pioglitazone, and intermediate-acting insulin (NPH) given at bedtime. repaglinide 0-11 insulin Homo sapiens 188-195 10929931-7 2000 The second modality involves increasing insulin availability by the administration of exogenous insulin, insulin analogues, sulphonylureas and the new insulin secretagogue, repaglinide. repaglinide 173-184 insulin Homo sapiens 40-47 11460577-4 2001 There are also newer insulin secretagogues (such as neteglinide and repaglinide) with a rapid onset of action on the beta-cell, therefore inducing a more physiological profile of insulin secretion during meals. repaglinide 68-79 insulin Homo sapiens 21-28 11190420-7 2000 Repaglinide and nateglinide are absorbed rapidly, stimulate insulin release within a few minutes, are rapidly metabolised in the liver and are mainly excreted in the bile. repaglinide 0-11 insulin Homo sapiens 60-67 11063282-7 2000 More recently, the availability of the rapid or early augmentor of insulin secretion--repaglinide--provides a means for restoring prandial glucose regulation with oral therapy. repaglinide 86-97 insulin Homo sapiens 67-74 11063282-9 2000 Prandial glucose regulation with repaglinide has also been demonstrated to provide synergies when used as combination therapy with insulin sensitising agents. repaglinide 33-44 insulin Homo sapiens 131-138 10959157-2 2000 Repaglinide is the first stimulator of insulin secretion from the new meglitinide family. repaglinide 0-11 insulin Homo sapiens 39-46 10959157-4 2000 In preclinical studies, the insulin-stimulating effect of repaglinide has been found to be 10 to 20 times more potent than that of glibenclamide. repaglinide 58-69 insulin Homo sapiens 28-35 11249478-1 2000 Repaglinide is a novel insulin secretagogue that was developed as a prandial glucose regulator for the treatment of people with Type 2 diabetes mellitus. repaglinide 0-11 insulin Homo sapiens 23-30 11249478-6 2000 Importantly, the pharmacokinetic properties of repaglinide, are expected to reduce the risk of hypoglycaemia in comparison to the conventional insulin secretagogues (sulphonylureas). repaglinide 47-58 insulin Homo sapiens 143-150 10857945-10 2000 CONCLUSIONS: A single dose of repaglinide (0.5-4.0 mg) before breakfast improves insulin secretion and reduces prandial hyperglycemia dose-dependently Administration of repaglinide had no effect on insulin secretion with the second meal, which was consumed 4 h after breakfast. repaglinide 30-41 insulin Homo sapiens 81-88 10857945-0 2000 Increased prandial insulin secretion after administration of a single preprandial oral dose of repaglinide in patients with type 2 diabetes. repaglinide 95-106 insulin Homo sapiens 19-26 10872292-6 2000 Among the stimulators of insulin secretion are the sulfonylureas (e.g. glibenclamide, glibonuride, glisoxepid, glimepiride), and the so-called prandial glucose regulators, such as repaglinide, which differ from the sulfonylureas both chemically and in their pharmacodynamic properties. repaglinide 180-191 insulin Homo sapiens 25-32 10834429-2 2000 The aim of this study was to explore actions of repaglinide on the rapid pulsatile insulin release by high-frequency insulin sampling and analysis of insulin-concentration time series. repaglinide 48-59 insulin Homo sapiens 83-90 10834429-2 2000 The aim of this study was to explore actions of repaglinide on the rapid pulsatile insulin release by high-frequency insulin sampling and analysis of insulin-concentration time series. repaglinide 48-59 insulin Homo sapiens 117-124 10834429-2 2000 The aim of this study was to explore actions of repaglinide on the rapid pulsatile insulin release by high-frequency insulin sampling and analysis of insulin-concentration time series. repaglinide 48-59 insulin Homo sapiens 117-124 10834429-7 2000 RESULTS: Average insulin concentration was increased after repaglinide administration (basal vs. stimulated period, P values are placebo vs. repaglinide) (25.1 +/- 3.6 vs. 33.5 +/- 4.1 pmol/l, P < 0.001). repaglinide 59-70 insulin Homo sapiens 17-24 10834429-7 2000 RESULTS: Average insulin concentration was increased after repaglinide administration (basal vs. stimulated period, P values are placebo vs. repaglinide) (25.1 +/- 3.6 vs. 33.5 +/- 4.1 pmol/l, P < 0.001). repaglinide 141-152 insulin Homo sapiens 17-24 10834429-8 2000 Insulin secretory burst mass (15.8 +/- 2.2 vs. 19.6 +/- 2.8 pmol x l(-1) x pulse(-1), P = 0.02) and amplitude (6.1 +/- 0.9 vs. 7.7 +/- 1.2 pmol x l(-1) x min(-1), P = 0.008) were augmented after repaglinide administration. repaglinide 195-206 insulin Homo sapiens 0-7 10834429-10 2000 ApEn increased significantly after repaglinide administration (0.623 +/- 0.045 vs. 0.670 +/- 0.034, P = 0.04), suggesting less orderly oscillatory patterns of insulin release. repaglinide 35-46 insulin Homo sapiens 159-166 10834429-11 2000 CONCLUSIONS: In conclusion, a single dose of repaglinide amplifies insulin secretory burst mass (and basal secretion) with no change in burst frequency. repaglinide 45-56 insulin Homo sapiens 67-74 10857945-5 2000 RESULTS: During the first meal period (0-240 min), administration of repaglinide reduced significantly the area under the curve (AUC) for glucose concentration and significantly increased the AUC for insulin levels, C-peptide levels, and the insulin secretion rate. repaglinide 69-80 insulin Homo sapiens 200-207 10857945-5 2000 RESULTS: During the first meal period (0-240 min), administration of repaglinide reduced significantly the area under the curve (AUC) for glucose concentration and significantly increased the AUC for insulin levels, C-peptide levels, and the insulin secretion rate. repaglinide 69-80 insulin Homo sapiens 242-249 10857945-7 2000 The effect of repaglinide administration on insulin secretion was most pronounced in the early prandial period. repaglinide 14-25 insulin Homo sapiens 44-51 10664920-1 2000 Repaglinide is a novel insulin secretagogue developed in response to the need for a fast-acting, oral prandial glucose regulator for the treatment of type 2 (non-insulin-dependent) diabetes mellitus. repaglinide 0-11 insulin Homo sapiens 23-30 11060717-1 2000 Repaglinide (NovoNorm((R))) is a novel oral antidiabetic agent, the first of a new class of insulin secretagogues known as the prandial glucose regulators to be approved for use in patients with Type 2 diabetes. repaglinide 0-11 insulin Homo sapiens 92-99 11060717-3 2000 After repaglinide administration, the resulting insulin profile reflects that of healthy individuals more closely, providing tighter glycaemic control and reducing the risk of hypoglycaemic events. repaglinide 6-17 insulin Homo sapiens 48-55 11225759-11 2000 When glucose targets are not met using repaglinide monotherapy, the combination of repaglinide with metformin can further improve glycaemic control by enhancing insulin secretion and improving insulin sensitivity. repaglinide 83-94 insulin Homo sapiens 161-168 10664920-1 2000 Repaglinide is a novel insulin secretagogue developed in response to the need for a fast-acting, oral prandial glucose regulator for the treatment of type 2 (non-insulin-dependent) diabetes mellitus. repaglinide 0-11 insulin Homo sapiens 162-169 10631622-3 2000 For the repaglinide treatment groups at the end of the study, changes in HbA1c from baseline values ranged from 1.8 to 1.9 percentage points lower than the placebo group. repaglinide 8-19 hemoglobin subunit alpha 1 Homo sapiens 73-77 11475269-4 1999 Efficacy of repaglinide therapy was assessed by measuring changes from baseline in mean levels of blood glucose (BGmean), fasting serum glucose (FSG), and mean levels of serum insulin (INSmean). repaglinide 12-23 insulin Homo sapiens 176-183 10605995-4 1999 Two new long-acting sulfonylureas (glimepiride and extended-release glipizide) and a short-acting sulfonylurea-like agent (repaglinide) simply and reliably augment the patient"s insulin supply. repaglinide 123-134 insulin Homo sapiens 178-185 10746004-3 1999 During type 2 diabetes mellitus, repaglinide is the first fast-acting oral antidiabetic drug able to stimulate endogenous insulin secretion during meal by mimicking physiological insulin secretion pattern. repaglinide 33-44 insulin Homo sapiens 122-129 10746004-3 1999 During type 2 diabetes mellitus, repaglinide is the first fast-acting oral antidiabetic drug able to stimulate endogenous insulin secretion during meal by mimicking physiological insulin secretion pattern. repaglinide 33-44 insulin Homo sapiens 179-186 10498841-6 1999 However, repaglinide only weakly inhibited CFTR Cl- currents. repaglinide 9-20 CF transmembrane conductance regulator Homo sapiens 43-47 10522838-1 1999 The action of repaglinide, a carbamoylmethyl benzoic acid derivative, mimics the physiological insulin secretion that is deficient in Type 2 diabetes mellitus. repaglinide 14-25 insulin Homo sapiens 95-102 10820647-7 1999 Other recently introduced drugs include glimepiride and the meglitinide insulin secretagogue, repaglinide. repaglinide 94-105 insulin Homo sapiens 72-79 11220287-8 1999 Repaglinide, a new, fast-acting insulin secretagogue with a short duration of action, reduces postprandial hyperglycaemia when taken shortly before meals. repaglinide 0-11 insulin Homo sapiens 32-39 10501822-17 1999 These properties make repaglinide a suitable insulin secretagogue for all patients with type-2 diabetes who retain sufficient beta-cell function. repaglinide 22-33 insulin Homo sapiens 45-52 10333912-7 1999 Subjects receiving repaglinide either alone or in combination with metformin, had an increase in fasting levels of insulin between baseline and the end of the trial of 4.04 +/- 1.56 and 4.23 +/- 1.50 mU/l, respectively (P < 0.02). repaglinide 19-30 insulin Homo sapiens 115-122 10522838-2 1999 Repaglinide stimulates insulin release from beta-cells only in the presence of glucose. repaglinide 0-11 insulin Homo sapiens 23-30 10522838-4 1999 In one study, repaglinide (0.25-4.0 mg preprandially) caused a dose-dependent decrease in blood glucose and a non-dose-dependent increase in insulin over 4 weeks (all doses p < 0.001 vs. placebo). repaglinide 14-25 insulin Homo sapiens 141-148 9855316-1 1998 Repaglinide is a new, short-acting, insulin-releasing agent recently approved for the monotherapy of type 2 diabetes mellitus, and in combination with metformin in patients failing repaglinide or metformin monotherapy. repaglinide 0-11 insulin Homo sapiens 36-43 9802740-9 1998 Concentrations of fasting and postprandial insulin and C-peptide were lower at the last visit compared with baseline for patients treated with placebo and higher for patients treated with repaglinide, and the differences between groups were statistically significant (P < 0.05). repaglinide 188-199 insulin Homo sapiens 43-50 9855316-2 1998 Repaglinide appears to trigger insulin release by regulating adenosine triphosphate-sensitive potassium channels on the surface of pancreatic beta cells, which in turn affect calcium influx, the principal mediator of insulin release. repaglinide 0-11 insulin Homo sapiens 31-38 9855316-2 1998 Repaglinide appears to trigger insulin release by regulating adenosine triphosphate-sensitive potassium channels on the surface of pancreatic beta cells, which in turn affect calcium influx, the principal mediator of insulin release. repaglinide 0-11 insulin Homo sapiens 217-224 15989662-4 1997 Four novel non-sulfonylurea insulin secretagogues are in advanced clinical development: A-4166, KAD-1229, BTS 67 582 and repaglinide. repaglinide 121-132 insulin Homo sapiens 28-35 9657067-3 1997 Both repaglinide (0.01 microM) and A-4166 (1.0 microM) stimulated insulin and somatostatin release, but failed to affect glucagon output, from pancreases exposed to 5.6 mM D-glucose. repaglinide 5-16 insulin Homo sapiens 66-73 9657067-5 1997 Although repaglinide was tested at a concentration a hundred times lower than that of A-4166, the drug-induced increase in both insulin and somatostatin secretion persisted for a longer time after exposure to repaglinide, than to A-4166. repaglinide 209-220 insulin Homo sapiens 128-135 9739505-1 1998 Repaglinide is a novel insulin secretagogue being developed for the management of type 2 (non-insulin-dependent) diabetes mellitus. repaglinide 0-11 insulin Homo sapiens 23-30 9868989-10 1998 In other studies, repaglinide caused a decrease of 5.8 mmol x l(-1) in peak postprandial glucose levels, and a decrease of 3.1 mmol x l(-1) in fasting levels with a reduction in HbA1c of 1.8% compared with placebo. repaglinide 18-29 hemoglobin subunit alpha 1 Homo sapiens 178-182 8223830-6 1993 Fasting plasma insulin in the repaglinide group decreased from 80 (median value) to 67 pmol.l-1; it did not change in the glibenclamide group. repaglinide 30-41 insulin Homo sapiens 15-22 8944206-6 1996 A new class of drugs with insulin secretory capacity, of which repaglinide (NovoNorm) is the leading compound, is now in phase III clinical trials. repaglinide 63-74 insulin Homo sapiens 26-33 32475902-7 2021 At the end of monotherapy, insulin secretion relative to glucose elevation (ISG0-30: area under the curve of insulin from 0 to 30 min during MTT [AUC0-30 of IRI]/AUC0-30 of plasma glucose) was significantly increased only in the repaglinide group; ISG0-30 did not significantly increase in either group after the addition of alogliptin.ConclusionsThe addition of alogliptin to repaglinide monotherapy did not cause glucose-independent inappropriate insulin secretion and did not appear to increase the incidence of hypoglycemia. repaglinide 229-240 insulin Homo sapiens 27-34 34939558-1 2021 Repaglinide is an antidiabetic drug that works by stimulating insulin secretion from pancreatic beta cells. repaglinide 0-11 insulin Homo sapiens 62-69 33933705-0 2021 High-Performance affinity chromatographic studies of repaglinide and nateglinide interactions with normal and glyoxal- or methylglyoxal-modified human albumin serum. repaglinide 53-64 albumin Homo sapiens 151-158 34157903-7 2022 Remarkably, inhibiting FOXO3 with repaglinide delayed OTM by severely impairing mechanical force-induced bone formation in vivo. repaglinide 34-45 forkhead box O3 Homo sapiens 23-28 32970826-8 2021 Recent studies have shown clinically significant increases in exposure to CYP2C8 substrates (repaglinide, dasabuvir, desloratidine) and a CYP2B6 substrate (s-sibutramine) following co-administration with clopidogrel, indicating that therapeutic strategies with clopidogrel should avoid these drugs. repaglinide 93-104 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 74-80 33455494-4 2021 Eliminations from plasma of cilomilast, phenytoin, repaglinide, tolbutamide, and S-warfarin in the CYP2C19 PM group were significantly slow; these drugs are known substrates of human CYP2C8/9/19. repaglinide 51-62 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 99-106 32475902-7 2021 At the end of monotherapy, insulin secretion relative to glucose elevation (ISG0-30: area under the curve of insulin from 0 to 30 min during MTT [AUC0-30 of IRI]/AUC0-30 of plasma glucose) was significantly increased only in the repaglinide group; ISG0-30 did not significantly increase in either group after the addition of alogliptin.ConclusionsThe addition of alogliptin to repaglinide monotherapy did not cause glucose-independent inappropriate insulin secretion and did not appear to increase the incidence of hypoglycemia. repaglinide 229-240 insulin Homo sapiens 109-116 32475902-7 2021 At the end of monotherapy, insulin secretion relative to glucose elevation (ISG0-30: area under the curve of insulin from 0 to 30 min during MTT [AUC0-30 of IRI]/AUC0-30 of plasma glucose) was significantly increased only in the repaglinide group; ISG0-30 did not significantly increase in either group after the addition of alogliptin.ConclusionsThe addition of alogliptin to repaglinide monotherapy did not cause glucose-independent inappropriate insulin secretion and did not appear to increase the incidence of hypoglycemia. repaglinide 377-388 insulin Homo sapiens 27-34 32475902-7 2021 At the end of monotherapy, insulin secretion relative to glucose elevation (ISG0-30: area under the curve of insulin from 0 to 30 min during MTT [AUC0-30 of IRI]/AUC0-30 of plasma glucose) was significantly increased only in the repaglinide group; ISG0-30 did not significantly increase in either group after the addition of alogliptin.ConclusionsThe addition of alogliptin to repaglinide monotherapy did not cause glucose-independent inappropriate insulin secretion and did not appear to increase the incidence of hypoglycemia. repaglinide 377-388 insulin Homo sapiens 109-116 33191904-5 2021 MATERIALS AND METHODS: An in silico DDI study was conducted using a population-based physiological pharmacokinetic simulator to estimate the CR of cytochrome P450 (CYP)3A4 for zolpidem, sildenafil, omeprazole, triazolam, and repaglinide. repaglinide 225-236 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 147-171 33088647-1 2020 Repaglinide, an oral hypoglycemic agent, is a short-acting insulin secretagogue. repaglinide 0-11 insulin Homo sapiens 59-66 32401667-2 2020 In the present study, we examined eight compounds (bosentan, cerivastatin, fluvastatin, pitavastatin, pravastatin, repaglinide, rosuvastatin, valsartan) as typical organic anion transporting polypeptide (OATP) substrates and six compounds metabolized by P450 and non-P450 enzymes to evaluate the predictability of CLt, Vdss and plasma concentration-time profiles after intravenous administration to chimeric mice.The predicted CLt and Vdss of drugs that undergo OATP-mediated uptake and P450/non-P450-mediated metabolism reflected the observed data from humans within a three-fold error range.We also examined the possibility of predicting plasma concentration-time profiles of drugs that undergo OATP-mediated uptake using the complex Dedrick plot in chimeric mice. repaglinide 115-126 solute carrier organic anion transporter family, member 1a6 Mus musculus 164-202 33210826-6 2021 Interestingly, repaglinide, one of the six antidiabetic drugs employed the highest docking score for Mpro , was similar to a previously predicted active molecule-nelfinavir, which is a potential anti-HIV and anti-COVID-19 drug. repaglinide 15-26 NEWENTRY Severe acute respiratory syndrome-related coronavirus 101-105 33210826-7 2021 Moreover, we found repaglinide shared similar docking pose and pharmacophores with reported ligand (N3 inhibitor) and nelfinavir, demonstrating that repaglinide would interact with Mpro in a similar way. repaglinide 19-30 n3 None 100-102 33210826-7 2021 Moreover, we found repaglinide shared similar docking pose and pharmacophores with reported ligand (N3 inhibitor) and nelfinavir, demonstrating that repaglinide would interact with Mpro in a similar way. repaglinide 19-30 NEWENTRY Severe acute respiratory syndrome-related coronavirus 181-185 33210826-7 2021 Moreover, we found repaglinide shared similar docking pose and pharmacophores with reported ligand (N3 inhibitor) and nelfinavir, demonstrating that repaglinide would interact with Mpro in a similar way. repaglinide 149-160 n3 None 100-102 33210826-7 2021 Moreover, we found repaglinide shared similar docking pose and pharmacophores with reported ligand (N3 inhibitor) and nelfinavir, demonstrating that repaglinide would interact with Mpro in a similar way. repaglinide 149-160 NEWENTRY Severe acute respiratory syndrome-related coronavirus 181-185 33716254-2 2021 Repaglinide is an insulin secretagogue with a low hypoglycemic risk because of its rapid- and short-acting effects. repaglinide 0-11 insulin Homo sapiens 18-25 32621047-8 2020 HbA1C and basal insulin requirement were significantly lower in repaglinide group (p = 0.004, p = 0.0002). repaglinide 64-75 insulin Homo sapiens 16-23 32187961-0 2020 Molecular pharmacokinetic mechanism of the drug-drug interaction between genistein and repaglinide mediated by P-gp. repaglinide 87-98 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 111-115 32187961-1 2020 This study was devised to investigate if P-glycoprotein (P-gp) mediated the drug-drug interaction (DDI) between genistein and repaglinide. repaglinide 126-137 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 41-55 32187961-1 2020 This study was devised to investigate if P-glycoprotein (P-gp) mediated the drug-drug interaction (DDI) between genistein and repaglinide. repaglinide 126-137 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 57-61 32187961-10 2020 In conclusion, genistein inhibited the efflux of repaglinide mediated by P-gp in rats and in vitro. repaglinide 49-60 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 73-77 32187961-11 2020 The findings suggested that the DDI between genistein and repaglinide is mediated by P-gp, and a dosage adjustment may be needed when they are co-administered in a clinical setting. repaglinide 58-69 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 85-89 33088647-6 2020 Detection of plasma repaglinide 10 h after administration in this case indicates delayed elimination of the agent, which might be derived from reduced hepatocyte uptake due to inhibitory effects of nilotinib on OATP1B1 and reduced oxidation of the agents by inhibitory effects of nilotinib, mainly on CYP3A4 activities, and of febuxostat on CYP2C8 activities. repaglinide 20-31 solute carrier organic anion transporter family member 1B1 Homo sapiens 211-218 33088647-6 2020 Detection of plasma repaglinide 10 h after administration in this case indicates delayed elimination of the agent, which might be derived from reduced hepatocyte uptake due to inhibitory effects of nilotinib on OATP1B1 and reduced oxidation of the agents by inhibitory effects of nilotinib, mainly on CYP3A4 activities, and of febuxostat on CYP2C8 activities. repaglinide 20-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 301-307 33088647-6 2020 Detection of plasma repaglinide 10 h after administration in this case indicates delayed elimination of the agent, which might be derived from reduced hepatocyte uptake due to inhibitory effects of nilotinib on OATP1B1 and reduced oxidation of the agents by inhibitory effects of nilotinib, mainly on CYP3A4 activities, and of febuxostat on CYP2C8 activities. repaglinide 20-31 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 341-347 33088647-7 2020 Repaglinide is eliminated by the liver, and is a short-acting insulin secretagogue with a good safety profile in patients with type 2 diabetes complicated by renal impairment, including elderly patients; however, its delayed elimination due to drug-drug interactions should be noted. repaglinide 0-11 insulin Homo sapiens 62-69 31129789-0 2019 Physiologically Based Pharmacokinetic Models for Prediction of Complex CYP2C8 and OATP1B1 (SLCO1B1) Drug-Drug-Gene Interactions: A Modeling Network of Gemfibrozil, Repaglinide, Pioglitazone, Rifampicin, Clarithromycin and Itraconazole. repaglinide 164-175 solute carrier organic anion transporter family member 1B1 Homo sapiens 82-89 32206324-2 2020 It has been suggested that the concomitant use of repaglinide with clopidogrel may inhibit repaglinide metabolism, because repaglinide is a substrate of cytochrome P450 2C8 (CYP2C8) and the main metabolite of clopidogrel acyl-beta-D-glucuronide inhibits CYP2C8 activity. repaglinide 50-61 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 153-172 32206324-2 2020 It has been suggested that the concomitant use of repaglinide with clopidogrel may inhibit repaglinide metabolism, because repaglinide is a substrate of cytochrome P450 2C8 (CYP2C8) and the main metabolite of clopidogrel acyl-beta-D-glucuronide inhibits CYP2C8 activity. repaglinide 50-61 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 174-180 32206324-2 2020 It has been suggested that the concomitant use of repaglinide with clopidogrel may inhibit repaglinide metabolism, because repaglinide is a substrate of cytochrome P450 2C8 (CYP2C8) and the main metabolite of clopidogrel acyl-beta-D-glucuronide inhibits CYP2C8 activity. repaglinide 50-61 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 254-260 32206324-2 2020 It has been suggested that the concomitant use of repaglinide with clopidogrel may inhibit repaglinide metabolism, because repaglinide is a substrate of cytochrome P450 2C8 (CYP2C8) and the main metabolite of clopidogrel acyl-beta-D-glucuronide inhibits CYP2C8 activity. repaglinide 91-102 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 174-180 32206324-2 2020 It has been suggested that the concomitant use of repaglinide with clopidogrel may inhibit repaglinide metabolism, because repaglinide is a substrate of cytochrome P450 2C8 (CYP2C8) and the main metabolite of clopidogrel acyl-beta-D-glucuronide inhibits CYP2C8 activity. repaglinide 91-102 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 174-180 31861249-0 2019 Repaglinide Silences the FOXO3/Lumican Axis and Represses the Associated Metastatic Potential of Neuronal Cancer Cells. repaglinide 0-11 forkhead box O3 Homo sapiens 25-30 31861249-5 2019 By a drug-library screen we identified the small molecular weight compound repaglinide (RPG) as a putative FOXO3 inhibitor. repaglinide 75-86 forkhead box O3 Homo sapiens 107-112 31129789-0 2019 Physiologically Based Pharmacokinetic Models for Prediction of Complex CYP2C8 and OATP1B1 (SLCO1B1) Drug-Drug-Gene Interactions: A Modeling Network of Gemfibrozil, Repaglinide, Pioglitazone, Rifampicin, Clarithromycin and Itraconazole. repaglinide 164-175 solute carrier organic anion transporter family member 1B1 Homo sapiens 91-98 31129789-5 2019 METHODS: PBPK models of the CYP2C8 and organic-anion-transporting polypeptide (OATP) 1B1 perpetrator drug gemfibrozil (parent-metabolite model) and the CYP2C8 victim drugs repaglinide (also an OATP1B1 substrate) and pioglitazone were developed using a total of 103 clinical studies. repaglinide 172-183 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 28-34 31452966-0 2019 Interaction of repaglinide with bovine serum albumin: Spectroscopic and molecular docking approaches. repaglinide 15-26 albumin Homo sapiens 39-52 31787898-0 2019 MTNR1B Gene Polymorphisms Are Associated With the Therapeutic Responses to Repaglinide in Chinese Patients With Type 2 Diabetes Mellitus. repaglinide 75-86 melatonin receptor 1B Homo sapiens 0-6 31787898-1 2019 The objective of this study was to investigate whether MTNR1B gene variants influence repaglinide response in Chinese patients with newly diagnosed type 2 diabetes mellitus (T2DM). repaglinide 86-97 melatonin receptor 1B Homo sapiens 55-61 31787898-4 2019 After 8-week repaglinide monotherapy, patients with at least one G allele of MTNR1B rs10830963 showed a smaller decrease in fasting plasma glucose (FPG) (P = 0.031) and a smaller increase in homeostasis model assessment for beta cell function (HOMA-B) (P = 0.002) levels than those with the CC genotype did. repaglinide 13-24 melatonin receptor 1B Homo sapiens 77-83 31787898-6 2019 These data suggest that the MTNR1B rs10830963 and rs1387153 polymorphisms are associated with repaglinide monotherapy efficacy in Chinese patients with T2DM. repaglinide 94-105 melatonin receptor 1B Homo sapiens 28-34 31118371-0 2019 A Variation in the ABCC8 Gene Is Associated with Type 2 Diabetes Mellitus and Repaglinide Efficacy in Chinese Type 2 Diabetes Mellitus Patients. repaglinide 78-89 ATP binding cassette subfamily C member 8 Homo sapiens 19-24 31118371-1 2019 Objective Previous studies have suggested that variations in the ABCC8 gene may be closely associated with T2DM susceptibility and repaglinide response. repaglinide 131-142 ATP binding cassette subfamily C member 8 Homo sapiens 65-70 31118371-9 2019 Conclusion These results suggested that the ABCC8 rs1801261 polymorphism might influence T2DM susceptibility and the therapeutic effect of repaglinide in Chinese Han T2DM patients. repaglinide 139-150 ATP binding cassette subfamily C member 8 Homo sapiens 44-49 31452966-1 2019 Repaglinide (RPG) regulates the amount of glucose by stimulating the pancreas to release insulin in the blood. repaglinide 0-11 insulin Homo sapiens 89-96 31452966-1 2019 Repaglinide (RPG) regulates the amount of glucose by stimulating the pancreas to release insulin in the blood. repaglinide 13-16 insulin Homo sapiens 89-96 31067468-1 2019 Repaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. repaglinide 0-11 insulin Homo sapiens 36-43 31026357-6 2019 Attenuation of IL-1beta secretion by Nateglinide/Repaglinide further suggests involvement of Kir6 channels. repaglinide 49-60 interleukin 1 beta Homo sapiens 15-23 31086218-2 2019 We recently showed that reduced DREAM expression or blockade of DREAM activity by repaglinide is neuroprotective in Huntington"s disease (HD). repaglinide 82-93 potassium voltage-gated channel interacting protein 3 Homo sapiens 32-37 31086218-2 2019 We recently showed that reduced DREAM expression or blockade of DREAM activity by repaglinide is neuroprotective in Huntington"s disease (HD). repaglinide 82-93 potassium voltage-gated channel interacting protein 3 Homo sapiens 64-69 31086218-3 2019 Here we used structure-based drug design to guide the identification of IQM-PC330, which was more potent and had longer lasting effects than repaglinide to inhibit DREAM in cellular and in vivo HD models. repaglinide 141-152 potassium voltage-gated channel interacting protein 3 Homo sapiens 164-169 31067468-1 2019 Repaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. repaglinide 13-16 insulin Homo sapiens 36-43 30636597-0 2019 Effects of CYP2C8 and SLCO1B1 Genetic Polymorphisms on Repaglinide Pharmacokinetics: A Systematic Review and Meta-Analysis. repaglinide 55-66 solute carrier organic anion transporter family member 1B1 Homo sapiens 22-29 30833929-10 2019 Insulin secretagogue agents have to be used with caution because of their significant hypoglycemic risk; if used, short-acting sulfonylureas, as gliclazide, or glinides as repaglinide, should be preferred. repaglinide 172-183 insulin Homo sapiens 0-7 29901213-4 2019 The model was then used to prospectively predict the interaction between letermovir and CYP2C8 substrates such as repaglinide, a substrate of CYP2C8, CYP3A, and OATP1B. repaglinide 114-125 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 88-94 29901213-4 2019 The model was then used to prospectively predict the interaction between letermovir and CYP2C8 substrates such as repaglinide, a substrate of CYP2C8, CYP3A, and OATP1B. repaglinide 114-125 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 142-148 29901213-4 2019 The model was then used to prospectively predict the interaction between letermovir and CYP2C8 substrates such as repaglinide, a substrate of CYP2C8, CYP3A, and OATP1B. repaglinide 114-125 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-155 30636597-1 2019 OBJECTIVE: The purpose of this systematic review and meta-analysis was to summarize the potential impact of CYP2C8 and SLCO1B1 genetic polymorphisms on repaglinide pharmacokinetics. repaglinide 152-163 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 108-114 30636597-1 2019 OBJECTIVE: The purpose of this systematic review and meta-analysis was to summarize the potential impact of CYP2C8 and SLCO1B1 genetic polymorphisms on repaglinide pharmacokinetics. repaglinide 152-163 solute carrier organic anion transporter family member 1B1 Homo sapiens 119-126 30636597-10 2019 CONCLUSION: The current systematic review and meta-analysis indicated that the genotype of CYP2C8, but not SLCO1B1, may affect repaglinide pharmacokinetics. repaglinide 127-138 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 91-97 31089348-0 2019 An Investigation into the Role of P-Glycoprotein in the Intestinal Absorption of Repaglinide: Assessed by Everted Gut Sac and Caco-2 Cell Line. repaglinide 81-92 ATP binding cassette subfamily B member 1 Homo sapiens 34-48 31122183-7 2019 RESULTS: SLCs and AMPK variations are considered for metformin, CYP2C9, KATP channel, CDKAL1, CDKN2A/2B and KCNQ1 for sulphonylureas, OATP1B, and KCNQ1 for repaglinide and the last but not the least ADIPOQ, PPAR-gamma, SLC, CYP2C8, and SLCO1B1 for thiazolidinediones response prediction. repaglinide 156-167 C-C motif chemokine ligand 21 Homo sapiens 9-12 31089348-1 2019 The present study aimed at exploring the potential of the P-glycoprotein (P-gp) transporters as a barrier to the repaglinide (REG) epithelial permeability. repaglinide 113-124 ATP binding cassette subfamily B member 1 Homo sapiens 58-72 31089348-1 2019 The present study aimed at exploring the potential of the P-glycoprotein (P-gp) transporters as a barrier to the repaglinide (REG) epithelial permeability. repaglinide 113-124 ATP binding cassette subfamily B member 1 Homo sapiens 74-78 30559648-3 2018 Small-molecules able to bind DREAM, like the anti-diabetic drug repaglinide, disrupt some of the interactions with other proteins and modulate DREAM activity on Kv4 channels or on the processing of activating transcription factor 6 (ATF6). repaglinide 64-75 Kv channel interacting protein 3, calsenilin Mus musculus 29-34 30559648-3 2018 Small-molecules able to bind DREAM, like the anti-diabetic drug repaglinide, disrupt some of the interactions with other proteins and modulate DREAM activity on Kv4 channels or on the processing of activating transcription factor 6 (ATF6). repaglinide 64-75 Kv channel interacting protein 3, calsenilin Mus musculus 143-148 30559648-3 2018 Small-molecules able to bind DREAM, like the anti-diabetic drug repaglinide, disrupt some of the interactions with other proteins and modulate DREAM activity on Kv4 channels or on the processing of activating transcription factor 6 (ATF6). repaglinide 64-75 activating transcription factor 6 Mus musculus 198-231 30559648-3 2018 Small-molecules able to bind DREAM, like the anti-diabetic drug repaglinide, disrupt some of the interactions with other proteins and modulate DREAM activity on Kv4 channels or on the processing of activating transcription factor 6 (ATF6). repaglinide 64-75 activating transcription factor 6 Mus musculus 233-237 30559648-5 2018 We show that repaglinide disrupts the interaction between DREAM and the C-terminal PS2 fragment (Ct-PS2) by coimmunoprecipitation assays. repaglinide 13-24 Kv channel interacting protein 3, calsenilin Mus musculus 58-63 30559648-5 2018 We show that repaglinide disrupts the interaction between DREAM and the C-terminal PS2 fragment (Ct-PS2) by coimmunoprecipitation assays. repaglinide 13-24 presenilin 2 Mus musculus 83-86 30559648-5 2018 We show that repaglinide disrupts the interaction between DREAM and the C-terminal PS2 fragment (Ct-PS2) by coimmunoprecipitation assays. repaglinide 13-24 cytidine 5'-triphosphate synthase 2 Mus musculus 97-103 30559648-6 2018 Exposure to sub-micromolar concentrations of repaglinide reduces the levels of Ct-PS2 fragment in N2a neuroblastoma cells. repaglinide 45-56 cytidine 5'-triphosphate synthase 2 Mus musculus 79-85 30260092-5 2018 The clearance of atorvastatin and repaglinide had a strong correlation (r2 = 0.70 and 0.63, respectively) with that of pitavastatin (a SLCO1B1 probe). repaglinide 34-45 solute carrier organic anion transporter family member 1B1 Homo sapiens 136-143 30235745-0 2018 Characteristics of repaglinide and its mechanism of action on insulin secretion in patients with newly diagnosed type-2 diabetes mellitus. repaglinide 19-30 insulin Homo sapiens 62-69 30235745-1 2018 This study aims to compare the effect of repaglinide and metformin among Chinese patients with newly diagnosed diabetes, and explore the possible mechanisms by which repaglinide alters insulin secretion.Sixty subjects with glycated hemoglobin (HbA1c) < 10.0% were randomly selected to receive repaglinide or metformin monotherapy for 15 weeks. repaglinide 166-177 insulin Homo sapiens 185-192 30213010-13 2018 After 4 months, the patient showed liver injury once again (an increase in ALT, AST, AKP, GGT and GLB) caused by repaglinide administration due to hyperglycemia. repaglinide 113-124 solute carrier family 17 member 5 Homo sapiens 80-83 30235745-1 2018 This study aims to compare the effect of repaglinide and metformin among Chinese patients with newly diagnosed diabetes, and explore the possible mechanisms by which repaglinide alters insulin secretion.Sixty subjects with glycated hemoglobin (HbA1c) < 10.0% were randomly selected to receive repaglinide or metformin monotherapy for 15 weeks. repaglinide 166-177 insulin Homo sapiens 185-192 30235745-8 2018 Insulin, PCNT, and F-actin expression in MIN-6 cells decreased after 15 minutes of stimulation with repaglinide, while no difference was observed at 2, 6, and 12 hours. repaglinide 100-111 insulin Homo sapiens 0-7 30235745-8 2018 Insulin, PCNT, and F-actin expression in MIN-6 cells decreased after 15 minutes of stimulation with repaglinide, while no difference was observed at 2, 6, and 12 hours. repaglinide 100-111 pericentrin (kendrin) Mus musculus 9-13 30235745-9 2018 The insulin levels of the cell medium in the repaglinide group remained significantly higher at all timepoints.This study manifests that repaglinide has a noninferiority effect on the glycemic parameters of Chinese patients with newly diagnosed diabetes, when compared with metformin. repaglinide 45-56 insulin Homo sapiens 4-11 30235745-10 2018 The PCNT-F-actin pathway plays an important role in the repaglinide regulation process of on-demand insulin secretion. repaglinide 56-67 pericentrin Homo sapiens 4-8 30235745-10 2018 The PCNT-F-actin pathway plays an important role in the repaglinide regulation process of on-demand insulin secretion. repaglinide 56-67 insulin Homo sapiens 100-107 29663513-0 2018 A variant of GRK5 is associated with the therapeutic efficacy of repaglinide in Chinese Han patients with type 2 diabetes mellitus. repaglinide 65-76 G protein-coupled receptor kinase 5 Homo sapiens 13-17 29381228-2 2018 We investigate, as an example, the impact of CYP3A4-CYP2C8 intercorrelation on the predicted interindividual variabilities of clearance and drug-drug interactions (DDIs) for repaglinide using physiologically based pharmacokinetic (PBPK) modelling. repaglinide 174-185 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 52-58 30121055-0 2018 Repaglinide inhibits cyclosporine A-induced renal tubular toxicityby affecting apoptosis and Baxand Bcl-2expression Background/aim: Repaglinide (RG) is a prandial glucose regulator used for the treatment of type 2 diabetes. repaglinide 0-11 BCL2, apoptosis regulator Rattus norvegicus 100-105 30121055-0 2018 Repaglinide inhibits cyclosporine A-induced renal tubular toxicityby affecting apoptosis and Baxand Bcl-2expression Background/aim: Repaglinide (RG) is a prandial glucose regulator used for the treatment of type 2 diabetes. repaglinide 132-143 BCL2, apoptosis regulator Rattus norvegicus 100-105 29748863-0 2018 Repaglinide-irbesartan drug interaction: effects of SLCO1B1 polymorphism on repaglinide pharmacokinetics and pharmacodynamics in Chinese population. repaglinide 0-11 solute carrier organic anion transporter family member 1B1 Homo sapiens 52-59 29748863-5 2018 Clinical data from single dose of repaglinide indicated SLCO1B1 c.521 T>C polymorphism influenced the PK and PD of repaglinide in healthy Chinese-Han male volunteers. repaglinide 34-45 solute carrier organic anion transporter family member 1B1 Homo sapiens 56-63 29748863-5 2018 Clinical data from single dose of repaglinide indicated SLCO1B1 c.521 T>C polymorphism influenced the PK and PD of repaglinide in healthy Chinese-Han male volunteers. repaglinide 118-129 solute carrier organic anion transporter family member 1B1 Homo sapiens 56-63 29748863-9 2018 CONCLUSION: SLCO1B1 c.521 T>C polymorphism affects the PK of repaglinide in Chinese population. repaglinide 64-75 solute carrier organic anion transporter family member 1B1 Homo sapiens 12-19 29748863-10 2018 Irbesartan increased repaglinide exposure in subjects with SLCO1B1 c.521 TT genotype, but not SLCO1B1 c.521 TC genotype. repaglinide 21-32 solute carrier organic anion transporter family member 1B1 Homo sapiens 59-66 29555503-3 2018 In the presence of glucagon-like peptide-1 (GLP-1), insulin secretion by repaglinide was augmented significantly but to lesser extent and showed different dynamics from that by glimepiride. repaglinide 73-84 glucagon Homo sapiens 19-42 29555503-3 2018 In the presence of glucagon-like peptide-1 (GLP-1), insulin secretion by repaglinide was augmented significantly but to lesser extent and showed different dynamics from that by glimepiride. repaglinide 73-84 glucagon Homo sapiens 44-49 29555503-8 2018 Our data indicate that repaglinide has characteristic properties in its effects on the dynamics of insulin secretion and intracellular Ca2+ and that the combination of repaglinide and GLP-1 stimulates insulin secretion more effectively than the combination of glimepiride and GLP-1 at a high concentration of glucose, providing a basis for its use in clinical settings. repaglinide 23-34 glucagon Homo sapiens 276-281 29663513-1 2018 Post-Market Research We aimed to investigate the impact of G protein-coupled receptor kinase 5 (GRK5) rs10886471 polymorphism on repaglinide efficacy in Chinese patients with type 2 diabetes mellitus (T2DM). repaglinide 129-140 G protein-coupled receptor kinase 5 Homo sapiens 59-94 29663513-1 2018 Post-Market Research We aimed to investigate the impact of G protein-coupled receptor kinase 5 (GRK5) rs10886471 polymorphism on repaglinide efficacy in Chinese patients with type 2 diabetes mellitus (T2DM). repaglinide 129-140 G protein-coupled receptor kinase 5 Homo sapiens 96-100 29663513-8 2018 These findings suggest that GRK5 rs10886471 polymorphism may influence the therapeutic efficacy of repaglinide in Chinese Han T2DM patients. repaglinide 99-110 G protein-coupled receptor kinase 5 Homo sapiens 28-32 28476618-8 2017 Mechanistically, repaglinide significantly reduced Bcl-2, Beclin-1 and PD-L1 expression in glioma tissues, indicating that repaglinide may exert its anti-cancer effects via apoptotic, autophagic and immune checkpoint signaling. repaglinide 123-134 beclin 1 Homo sapiens 58-66 29523177-5 2018 Using the novel object recognition test, we show that chronic administration of the DREAM-binding molecule repaglinide, or induced DREAM haplodeficiency delays onset of cognitive impairment in R6/1 mice, another HD model. repaglinide 107-118 Kv channel interacting protein 3, calsenilin Mus musculus 84-89 29523177-6 2018 The mechanism involves a notable rise in the levels of transcriptionally active ATF6 protein in the hippocampus after repaglinide administration. repaglinide 118-129 activating transcription factor 6 Mus musculus 80-84 28653847-5 2017 As interaction perpetrators with CYP2C8, glucuronides of gemfibrozil and clopidogrel showed marked clinical drug-drug interactions (e.g., with cerivastatin and repaglinide), which are more than expected from the parent drug. repaglinide 160-171 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 33-39 28479356-2 2017 Repaglinide (RPG) is transported into the liver by OATP1B1 and then is metabolized by CYP2C8 and CYP3A4. repaglinide 0-11 solute carrier organic anion transporter family member 1B1 Homo sapiens 51-58 28479356-2 2017 Repaglinide (RPG) is transported into the liver by OATP1B1 and then is metabolized by CYP2C8 and CYP3A4. repaglinide 0-11 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 86-92 28479356-2 2017 Repaglinide (RPG) is transported into the liver by OATP1B1 and then is metabolized by CYP2C8 and CYP3A4. repaglinide 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 28479356-2 2017 Repaglinide (RPG) is transported into the liver by OATP1B1 and then is metabolized by CYP2C8 and CYP3A4. repaglinide 13-16 solute carrier organic anion transporter family member 1B1 Homo sapiens 51-58 28479356-2 2017 Repaglinide (RPG) is transported into the liver by OATP1B1 and then is metabolized by CYP2C8 and CYP3A4. repaglinide 13-16 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 86-92 28479356-2 2017 Repaglinide (RPG) is transported into the liver by OATP1B1 and then is metabolized by CYP2C8 and CYP3A4. repaglinide 13-16 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 28977924-10 2017 The percentage of patients with low eGFR (i.e. <30 ml/min/1.73m2) taking either metformin or sulphonilureas/repaglinide was particularly high (i.e. 15.3% and 34.3% respectively). repaglinide 111-122 epidermal growth factor receptor Homo sapiens 36-40 28653144-8 2018 RESULTS: Simulations based on the current hypothesis reasonably describe SLCO1B1 and ABCG2 genotyped pharmacokinetic time course data for five transporter substrates (atorvastatin, pitavastatin, pravastatin, repaglinide, and rosuvastatin) in Caucasian and Asian populations. repaglinide 208-219 solute carrier organic anion transporter family member 1B1 Homo sapiens 73-80 28653144-8 2018 RESULTS: Simulations based on the current hypothesis reasonably describe SLCO1B1 and ABCG2 genotyped pharmacokinetic time course data for five transporter substrates (atorvastatin, pitavastatin, pravastatin, repaglinide, and rosuvastatin) in Caucasian and Asian populations. repaglinide 208-219 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 85-90 28238899-0 2017 Estimation of the Contribution of CYP2C8 and CYP3A4 in Repaglinide Metabolism by Human Liver Microsomes Under Various Buffer Conditions. repaglinide 55-66 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 34-40 28238899-0 2017 Estimation of the Contribution of CYP2C8 and CYP3A4 in Repaglinide Metabolism by Human Liver Microsomes Under Various Buffer Conditions. repaglinide 55-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 28238899-2 2017 In the present study, therefore, the possibility of buffer condition dependence of the fraction metabolized by CYP2C8 (fm2C8) for repaglinide, a dual substrate of CYP2C8 and CYP3A4, was estimated using human liver microsomes under various buffer conditions. repaglinide 130-141 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 111-117 28238899-2 2017 In the present study, therefore, the possibility of buffer condition dependence of the fraction metabolized by CYP2C8 (fm2C8) for repaglinide, a dual substrate of CYP2C8 and CYP3A4, was estimated using human liver microsomes under various buffer conditions. repaglinide 130-141 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 163-169 28238899-2 2017 In the present study, therefore, the possibility of buffer condition dependence of the fraction metabolized by CYP2C8 (fm2C8) for repaglinide, a dual substrate of CYP2C8 and CYP3A4, was estimated using human liver microsomes under various buffer conditions. repaglinide 130-141 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 28238899-5 2017 Based on these results, the contribution of CYP2C8 in repaglinide metabolism was estimated to be larger than that of CYP3A4 under each buffer condition, and the fm2C8 value of 0.760, estimated in 50 mM phosphate buffer, was the closest to the value (0.801) estimated in our previous modeling analysis based on its concentration increase in a clinical drug interaction study. repaglinide 54-65 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 44-50 28476618-8 2017 Mechanistically, repaglinide significantly reduced Bcl-2, Beclin-1 and PD-L1 expression in glioma tissues, indicating that repaglinide may exert its anti-cancer effects via apoptotic, autophagic and immune checkpoint signaling. repaglinide 17-28 BCL2 apoptosis regulator Homo sapiens 51-56 28476618-8 2017 Mechanistically, repaglinide significantly reduced Bcl-2, Beclin-1 and PD-L1 expression in glioma tissues, indicating that repaglinide may exert its anti-cancer effects via apoptotic, autophagic and immune checkpoint signaling. repaglinide 17-28 beclin 1 Homo sapiens 58-66 28476618-8 2017 Mechanistically, repaglinide significantly reduced Bcl-2, Beclin-1 and PD-L1 expression in glioma tissues, indicating that repaglinide may exert its anti-cancer effects via apoptotic, autophagic and immune checkpoint signaling. repaglinide 17-28 CD274 molecule Homo sapiens 71-76 28476618-8 2017 Mechanistically, repaglinide significantly reduced Bcl-2, Beclin-1 and PD-L1 expression in glioma tissues, indicating that repaglinide may exert its anti-cancer effects via apoptotic, autophagic and immune checkpoint signaling. repaglinide 123-134 BCL2 apoptosis regulator Homo sapiens 51-56 28476618-8 2017 Mechanistically, repaglinide significantly reduced Bcl-2, Beclin-1 and PD-L1 expression in glioma tissues, indicating that repaglinide may exert its anti-cancer effects via apoptotic, autophagic and immune checkpoint signaling. repaglinide 123-134 CD274 molecule Homo sapiens 71-76 27599706-4 2017 METHODS: This study predicted the magnitude of the DDI between efavirenz, an inducer of CYP3A4 and inhibitor of CYP2C8, and dual CYP3A4/CYP2C8 substrates (repaglinide, montelukast, pioglitazone, paclitaxel) using a physiologically based pharmacokinetic (PBPK) modeling approach integrating concurrent effects on CYPs. repaglinide 155-166 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 31149163-7 2017 Focusing on 4 patients who received DPP-4 inhibitor monotherapy at enrolment, switching to repaglinide also significantly improved HbA1c levels. repaglinide 91-102 dipeptidyl peptidase 4 Homo sapiens 36-41 31149163-10 2017 In case that DPP-4 inhibitors are not enough to achieve targeted range of glycemic control, repaglinide is another good candidate. repaglinide 92-103 dipeptidyl peptidase 4 Homo sapiens 13-18 27599706-4 2017 METHODS: This study predicted the magnitude of the DDI between efavirenz, an inducer of CYP3A4 and inhibitor of CYP2C8, and dual CYP3A4/CYP2C8 substrates (repaglinide, montelukast, pioglitazone, paclitaxel) using a physiologically based pharmacokinetic (PBPK) modeling approach integrating concurrent effects on CYPs. repaglinide 155-166 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 136-142 27543206-8 2016 Finally, incorporation of protein expression of OATP1B1 in alcoholic cirrhosis into the Simcyp physiologically based pharmacokinetics cirrhosis module improved prediction of the disposition of repaglinide in liver cirrhosis patients. repaglinide 193-204 solute carrier organic anion transporter family member 1B1 Homo sapiens 48-55 27967230-10 2017 Noninsulin antidiabetes agents like dipeptidyl peptidase 4 inhibitors, repaglinide, and glipizide in appropriate doses and reduction of insulin doses up to 50% may help decrease hypoglycemia. repaglinide 71-82 insulin Homo sapiens 3-10 27273149-0 2017 Pharmacokinetic Effects of Isavuconazole Coadministration With the Cytochrome P450 Enzyme Substrates Bupropion, Repaglinide, Caffeine, Dextromethorphan, and Methadone in Healthy Subjects. repaglinide 112-123 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 67-82 27857189-0 2016 A variation in KCNQ1 gene is associated with repaglinide efficacy on insulin resistance in Chinese Type 2 Diabetes Mellitus Patients. repaglinide 45-56 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 15-20 27857189-0 2016 A variation in KCNQ1 gene is associated with repaglinide efficacy on insulin resistance in Chinese Type 2 Diabetes Mellitus Patients. repaglinide 45-56 insulin Homo sapiens 69-76 27857189-1 2016 Repaglinide is an insulin secretagogue that often exhibits considerable interindividual variability in therapeutic efficacy. repaglinide 0-11 insulin Homo sapiens 18-25 27857189-2 2016 The current study was designed to investigate the impact of KCNQ1 genetic polymorphism on the efficacy of repaglinide and furthermore to identify the potential mechanism of action in patients with type 2 diabetes. repaglinide 106-117 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 60-65 27857189-7 2016 The KCNQ1 inhibitor enhanced repaglinide efficacy on insulin resistance, with IRS-2/PI(3)K/Akt signaling being up-regulated markedly. repaglinide 29-40 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 4-9 27857189-7 2016 The KCNQ1 inhibitor enhanced repaglinide efficacy on insulin resistance, with IRS-2/PI(3)K/Akt signaling being up-regulated markedly. repaglinide 29-40 insulin Homo sapiens 53-60 27857189-8 2016 As in our clinical experiment, these data strongly suggest that KCNQ1 genetic polymorphism influences repaglinide response due to the pivotal role of KCNQ1 in regulating insulin resistance through the IRS-2/PI(3)K/Akt signaling pathway. repaglinide 102-113 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 64-69 27857189-8 2016 As in our clinical experiment, these data strongly suggest that KCNQ1 genetic polymorphism influences repaglinide response due to the pivotal role of KCNQ1 in regulating insulin resistance through the IRS-2/PI(3)K/Akt signaling pathway. repaglinide 102-113 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 150-155 27857189-8 2016 As in our clinical experiment, these data strongly suggest that KCNQ1 genetic polymorphism influences repaglinide response due to the pivotal role of KCNQ1 in regulating insulin resistance through the IRS-2/PI(3)K/Akt signaling pathway. repaglinide 102-113 insulin Homo sapiens 170-177 27857189-8 2016 As in our clinical experiment, these data strongly suggest that KCNQ1 genetic polymorphism influences repaglinide response due to the pivotal role of KCNQ1 in regulating insulin resistance through the IRS-2/PI(3)K/Akt signaling pathway. repaglinide 102-113 insulin receptor substrate 2 Homo sapiens 201-206 27857189-8 2016 As in our clinical experiment, these data strongly suggest that KCNQ1 genetic polymorphism influences repaglinide response due to the pivotal role of KCNQ1 in regulating insulin resistance through the IRS-2/PI(3)K/Akt signaling pathway. repaglinide 102-113 AKT serine/threonine kinase 1 Homo sapiens 214-217 27435474-10 2016 Based on these results, we conclude that repaglinide induces vasorelaxation via activation of adenylyl cyclase/PKA and guanylyl cyclase/PKG signaling pathways independently of the endothelium, K(+) channels, Ca(2+) channels, and intracellular Ca(2+) ([Ca(2+)]i). repaglinide 41-52 protein kinase cGMP-dependent 1 Homo sapiens 136-139 27457785-6 2016 The predicted AUCRs using the mechanism-based inhibition of CYP2C8 by clopidogrel acyl-beta-glucuronide were similar to the observed AUCRs, and the predicted AUCR (1.1) of repaglinide using only the inhibition of OATP1B1 did not reach the observed AUCR (3.1). repaglinide 172-183 solute carrier organic anion transporter family member 1B1 Homo sapiens 213-220 27457785-8 2016 Clopidogrel is expected to have an effect not only on CYP2C8 substrates, but also dual CYP2C8/OATP1B1 substrates as seen in the case of repaglinide. repaglinide 136-147 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 87-93 27457785-8 2016 Clopidogrel is expected to have an effect not only on CYP2C8 substrates, but also dual CYP2C8/OATP1B1 substrates as seen in the case of repaglinide. repaglinide 136-147 solute carrier organic anion transporter family member 1B1 Homo sapiens 94-101 27435474-0 2016 The anti-diabetic drug repaglinide induces vasorelaxation via activation of PKA and PKG in aortic smooth muscle. repaglinide 23-34 protein kinase cGMP-dependent 1 Homo sapiens 84-87 27435474-6 2016 Also, pretreatment with a guanylyl cyclase inhibitor (ODQ) or a PKG inhibitor (KT 5823) inhibited repaglinide-induced vasorelaxation. repaglinide 98-109 protein kinase cGMP-dependent 1 Homo sapiens 64-67 27042279-1 2016 AIMS/INTRODUCTION: The aim of the present study was to evaluate the long-term efficacy and safety of adding repaglinide in patients with type 2 diabetes mellitus whose blood glucose levels were not sufficiently controlled by treatment with a dipeptidyl peptidase-4 inhibitor, sitagliptin, in addition to diet and exercise therapies. repaglinide 108-119 dipeptidyl peptidase 4 Homo sapiens 242-264 27259818-0 2016 CYP2C8-mediated interaction between repaglinide and steviol acyl glucuronide: In vitro investigations using rat and human matrices and in vivo pharmacokinetic evaluation in rats. repaglinide 36-47 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 0-6 27259818-4 2016 SVAG was also capable of inhibiting CYP2C8-mediated repaglinide 3"-hydroxylation in human liver microsomes and recombinant human CYP2C8, with Ki values of 15.8 muM and 11.6 muM, respectively. repaglinide 52-63 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 36-42 26883446-6 2016 Repaglinide also had some positive influence on HUVEC function elevating NO production in the presence of VEGF. repaglinide 0-11 vascular endothelial growth factor A Homo sapiens 106-110 26752648-6 2016 Repaglinide blocked this interaction and enhanced ATF6 processing and nuclear accumulation of transcriptionally active ATF6, improving prosurvival UPR function in striatal neurons. repaglinide 0-11 activating transcription factor 6 Mus musculus 50-54 26752648-6 2016 Repaglinide blocked this interaction and enhanced ATF6 processing and nuclear accumulation of transcriptionally active ATF6, improving prosurvival UPR function in striatal neurons. repaglinide 0-11 activating transcription factor 6 Mus musculus 119-123 26548081-4 2015 In the present study, we explored the binding interactions of antidiabetic drugs i.e., sulfonylurea drugs (glimepiride, glipizide, glyburide) and rapid acting insulin secretagogues viz., nateglinide, repaglinide and rosiglitazone; and Pgp inhibitors i.e., Generation I (verapamil and tamoxifen), III (tetradrine and tariquidar), and natural inhibitors (fumagillin and piperine) in mouse Pgp model. repaglinide 200-211 insulin Homo sapiens 159-166 26296069-1 2015 PURPOSE: Repaglinide and pioglitazone are both CYP2C8 and CYP3A4 substrates. repaglinide 9-20 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 47-53 26296069-1 2015 PURPOSE: Repaglinide and pioglitazone are both CYP2C8 and CYP3A4 substrates. repaglinide 9-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-64 25862064-9 2015 A photo-induced cross-linking-based oligomerization assay demonstrated that repaglinide supressed the formation of hIAPP oligomers, whereas glyburide and troglitazone were ineffective in inhibiting oligomerization. repaglinide 76-87 islet amyloid polypeptide Homo sapiens 115-120 26692235-1 2016 CONTEXT: Repaglinide is a short-acting insulin secretagogue with high interindividual variability in pharmacokinetics due to genetic polymorphisms. repaglinide 9-20 insulin Homo sapiens 39-46 26721703-3 2016 CYP2C8 substrate drugs include amodiaquine, cerivastatin, dasabuvir, enzalutamide, imatinib, loperamide, montelukast, paclitaxel, pioglitazone, repaglinide, and rosiglitazone, and the number is increasing. repaglinide 144-155 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 0-6 25595597-6 2015 Other inhibitors of CYP2C8 (gemfibrozil, montelukast, clopidogrel glucuronide, repaglinide, and cerivastatin) also caused extensive inhibition of 3-hydroxydesloratadine formation (73%-100%). repaglinide 79-90 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 20-26 26013675-4 2015 RESULTS: Increased risks of HCC were found for use of insulin (odds ratio [OR] = 3.73, 95% confidence interval [CI] 2.52-5.51), sulfonylureas (OR = 1.39, 95%CI 0.98-1.99), and repaglinide (OR = 2.12, 95%CI 1.38-3.26), while a reduced risk was found for use of metformin (OR = 0.57, 95%CI 0.41-0.79). repaglinide 176-187 insulin Homo sapiens 54-61 26013675-5 2015 The risk of HCC increased with increasing duration of insulin use (OR = 2.52 for <1 year, 5.41 for 1-2 years, and 6.01 for >=2 years; p for trend < 0.001), while no clear pattern with duration was observed for sulfonylureas, repaglinide, and metformin. repaglinide 234-245 insulin Homo sapiens 54-61 26024304-7 2015 In the repaglinide cohort, rs831571 was significantly associated with decreased HbA1c levels after 24 weeks of treatment, the homeostatic model assessment of insulin resistance and fasting insulin level after 48 weeks of treatment with repaglinide (P = 0.0096, 0235 and 0.0212, respectively). repaglinide 7-18 insulin Homo sapiens 189-196 26024304-7 2015 In the repaglinide cohort, rs831571 was significantly associated with decreased HbA1c levels after 24 weeks of treatment, the homeostatic model assessment of insulin resistance and fasting insulin level after 48 weeks of treatment with repaglinide (P = 0.0096, 0235 and 0.0212, respectively). repaglinide 236-247 insulin Homo sapiens 189-196 26024304-8 2015 In conclusion, we observed that the PSMD6 variant rs831571 might be associated with the therapeutic effects of rosiglitazone and repaglinide in Chinese T2DM patients. repaglinide 129-140 proteasome 26S subunit, non-ATPase 6 Homo sapiens 36-41 24704461-0 2014 Effects of nateglinide and repaglinide administered intracerebroventricularly on the CA3 hippocampal neuronal cell death and hyperglycemia induced by kainic acid in mice. repaglinide 27-38 carbonic anhydrase 3 Mus musculus 85-88 24971633-1 2014 Cerivastatin and repaglinide are substrates of cytochrome P450 (CYP)2C8, CYP3A4, and organic anion-transporting polypeptide (OATP)1B1. repaglinide 17-28 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 47-71 24971633-1 2014 Cerivastatin and repaglinide are substrates of cytochrome P450 (CYP)2C8, CYP3A4, and organic anion-transporting polypeptide (OATP)1B1. repaglinide 17-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-79 24971633-1 2014 Cerivastatin and repaglinide are substrates of cytochrome P450 (CYP)2C8, CYP3A4, and organic anion-transporting polypeptide (OATP)1B1. repaglinide 17-28 solute carrier organic anion transporter family member 1B1 Homo sapiens 85-133 24843385-10 2014 The levels of plasminogen activator inhibitor-1, high sensitivity C-reactive protein, and urinary 8-hydoroxydeoxyguanosine were reduced significantly by repaglinide treatment. repaglinide 153-164 serpin family E member 1 Homo sapiens 14-47 24843385-10 2014 The levels of plasminogen activator inhibitor-1, high sensitivity C-reactive protein, and urinary 8-hydoroxydeoxyguanosine were reduced significantly by repaglinide treatment. repaglinide 153-164 C-reactive protein Homo sapiens 66-84 25311380-0 2015 PPARD rs2016520 polymorphism affects repaglinide response in Chinese Han patients with type 2 diabetes mellitus. repaglinide 37-48 peroxisome proliferator activated receptor delta Homo sapiens 0-5 25311380-1 2015 Repaglinide is a short-acting insulin secretagogue, which often results in considerable interindividual variability in therapeutic efficacy when widely used in a clinical setting. repaglinide 0-11 insulin Homo sapiens 30-37 25311380-4 2015 However, little is known about the impacts of PPARD genetic polymorphism on the efficacy of repaglinide. repaglinide 92-103 peroxisome proliferator activated receptor delta Homo sapiens 46-51 25311380-5 2015 Therefore, the current study was designed to investigate the associations of PPARD rs2016520 polymorphism with type 2 diabetes mellitus (T2DM) susceptibility and repaglinide therapeutic efficacy in Chinese Han T2DM patients. repaglinide 162-173 peroxisome proliferator activated receptor delta Homo sapiens 77-82 25311380-11 2015 These findings suggest that PPARD rs2016520 polymorphism might influence the therapeutic effect of repaglinide rather than T2DM susceptibility in Chinese Han T2DM patients. repaglinide 99-110 peroxisome proliferator activated receptor delta Homo sapiens 28-33 25560470-1 2015 Glinides, including repaglinide, nateglinide and mitiglinide, are a type of fasting insulin secretagogue that could help to mimic early-phase insulin release, thus providing improved control of the postprandial glucose levels. repaglinide 20-31 insulin Homo sapiens 84-91 25560470-1 2015 Glinides, including repaglinide, nateglinide and mitiglinide, are a type of fasting insulin secretagogue that could help to mimic early-phase insulin release, thus providing improved control of the postprandial glucose levels. repaglinide 20-31 insulin Homo sapiens 142-149 24623479-1 2014 PURPOSE: To investigate the effect of OATP1B1 genotype as a covariate on repaglinide pharmacokinetics and drug-drug interaction (DDIs) risk using a reduced physiologically-based pharmacokinetic (PBPK) model. repaglinide 73-84 solute carrier organic anion transporter family member 1B1 Homo sapiens 38-45 24623479-3 2014 RESULTS: Estimated repaglinide CLuptake corresponded to 217 and 113 muL/min/10(6) cells for SLCO1B1 c.521TT/TC and CC, respectively. repaglinide 19-30 solute carrier organic anion transporter family member 1B1 Homo sapiens 92-99 24623479-6 2014 Propagation of this uncertainty had a marginal effect on the prediction of repaglinide OATP1B1-mediated DDI with cyclosporine; however, sensitivity of the predicted magnitude of repaglinide metabolic DDI was high. repaglinide 75-86 solute carrier organic anion transporter family member 1B1 Homo sapiens 87-94 24623479-7 2014 In addition, the reduced PBPK model was used to assess the effect of both CYP2C8*3 and SLCO1B1 c.521T>C on repaglinide exposure by simulations; power calculations were performed to guide prospective DDI and pharmacogenetic studies. repaglinide 110-121 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 74-80 24623479-7 2014 In addition, the reduced PBPK model was used to assess the effect of both CYP2C8*3 and SLCO1B1 c.521T>C on repaglinide exposure by simulations; power calculations were performed to guide prospective DDI and pharmacogenetic studies. repaglinide 110-121 solute carrier organic anion transporter family member 1B1 Homo sapiens 87-94 24704461-8 2014 pretreatment with repaglinide attenuated the KA-induced neuronal cell death in CA3 region of the hippocampus and hyperglycemia. repaglinide 18-29 carbonic anhydrase 3 Mus musculus 79-82 24704461-18 2014 Our results suggest that supraspinally administered repaglinide, but not nateglinide, exerts a protective effect against the KA-induced neuronal cells death in CA3 region of the hippocampus. repaglinide 52-63 carbonic anhydrase 3 Mus musculus 160-163 24338736-0 2014 Effects of NOS1AP rs12742393 polymorphism on repaglinide response in Chinese patients with type 2 diabetes mellitus. repaglinide 45-56 nitric oxide synthase 1 adaptor protein Homo sapiens 11-17 24567025-11 2014 After the HNF1A-MODY diagnosis, treatment was changed to repaglinide. repaglinide 57-68 HNF1 homeobox A Homo sapiens 10-15 24338736-11 2014 The effects of repaglinide treatment on FPG (p<0.01), FINS (p<0.05) and HOMA-IR (p<0.001) were reduced in patients with T2DM carrying the NOS1AP rs12742393 risk C allele compared with the AA genotype carriers. repaglinide 15-26 nitric oxide synthase 1 adaptor protein Homo sapiens 147-153 24338736-12 2014 CONCLUSION: The NOS1AP rs12742393 polymorphism is associated with therapeutic efficacy of repaglinide in Chinese T2DM patients. repaglinide 90-101 nitric oxide synthase 1 adaptor protein Homo sapiens 16-22 24338736-1 2014 STUDY OBJECTIVE: To investigate the associations of NOS1AP rs12742393 polymorphism with the risk of type 2 diabetes mellitus (T2DM) and repaglinide therapeutic efficacy in Chinese patients with T2DM. repaglinide 136-147 nitric oxide synthase 1 adaptor protein Homo sapiens 52-58 23807564-0 2013 PXR polymorphisms and their impact on pharmacokinetics/pharmacodynamics of repaglinide in healthy Chinese volunteers. repaglinide 75-86 nuclear receptor subfamily 1 group I member 2 Homo sapiens 0-3 23807564-5 2013 Thus, a clinical study in healthy Chinese subjects was conducted to investigate the impact of PXR polymorphisms on repaglinide (an endogenous marker for CYP3A4 activity) pharmacokinetics used alone or in combination with a PXR inducer, flucloxacillin. repaglinide 115-126 nuclear receptor subfamily 1 group I member 2 Homo sapiens 94-97 23807564-5 2013 Thus, a clinical study in healthy Chinese subjects was conducted to investigate the impact of PXR polymorphisms on repaglinide (an endogenous marker for CYP3A4 activity) pharmacokinetics used alone or in combination with a PXR inducer, flucloxacillin. repaglinide 115-126 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 153-159 23807564-13 2013 CONCLUSION: Our study results demonstrated for the first time the impact of genetic polymorphisms of PXR on the PK and PD of repaglinide, and showed that subjects with genotype of -298G/G and 11193C/C in PXR has a decreased elimination rate of 3A4/2C8. repaglinide 125-136 nuclear receptor subfamily 1 group I member 2 Homo sapiens 101-104 23807564-13 2013 CONCLUSION: Our study results demonstrated for the first time the impact of genetic polymorphisms of PXR on the PK and PD of repaglinide, and showed that subjects with genotype of -298G/G and 11193C/C in PXR has a decreased elimination rate of 3A4/2C8. repaglinide 125-136 nuclear receptor subfamily 1 group I member 2 Homo sapiens 204-207 24399740-11 2013 CONCLUSION: Nifedipine enhanced the oral bioavailability of repaglinide, which may be mainly attributable to inhibition of CYP3A4-mediated metabolism of repaglinide in the small intestine and/or in the liver and to inhibition of the P-gp efflux transporter in the small intestine and/or reduction of total body clearance by nifedipine. repaglinide 60-71 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 233-237 23536207-1 2013 CYP2C8 plays an important role in the metabolism of various drugs, such as paclitaxel, repaglinide and ibuprofen. repaglinide 87-98 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 0-6 23536207-2 2013 Polymorphisms in the CYP2C8 gene were shown to influence interindividual differences in the pharmacokinetics of paclitaxel, repaglinide and ibuprofen enantiomers. repaglinide 124-135 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 21-27 23536207-6 2013 The CLint values of CYP2C8.2 and CYP2C8.4 for repaglinide were 77.9% and 80.2% of that of CYP2C8.1 (p<0.05), respectively, while the CLint value of CYP2C8.3 was 1.31-fold higher than that of CYP2C8.1 (p<0.05). repaglinide 46-57 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 20-26 23536207-6 2013 The CLint values of CYP2C8.2 and CYP2C8.4 for repaglinide were 77.9% and 80.2% of that of CYP2C8.1 (p<0.05), respectively, while the CLint value of CYP2C8.3 was 1.31-fold higher than that of CYP2C8.1 (p<0.05). repaglinide 46-57 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 33-39 23536207-6 2013 The CLint values of CYP2C8.2 and CYP2C8.4 for repaglinide were 77.9% and 80.2% of that of CYP2C8.1 (p<0.05), respectively, while the CLint value of CYP2C8.3 was 1.31-fold higher than that of CYP2C8.1 (p<0.05). repaglinide 46-57 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 90-98 23536207-6 2013 The CLint values of CYP2C8.2 and CYP2C8.4 for repaglinide were 77.9% and 80.2% of that of CYP2C8.1 (p<0.05), respectively, while the CLint value of CYP2C8.3 was 1.31-fold higher than that of CYP2C8.1 (p<0.05). repaglinide 46-57 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 33-39 23536207-6 2013 The CLint values of CYP2C8.2 and CYP2C8.4 for repaglinide were 77.9% and 80.2% of that of CYP2C8.1 (p<0.05), respectively, while the CLint value of CYP2C8.3 was 1.31-fold higher than that of CYP2C8.1 (p<0.05). repaglinide 46-57 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 194-202 23536207-8 2013 Comparing hydroxylation by CYP2C8.1 and CYP2C8.3 resulted in higher and lower intrinsic clearance of repaglinide and ibuprofen enantiomers, respectively. repaglinide 101-112 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 27-35 23536207-8 2013 Comparing hydroxylation by CYP2C8.1 and CYP2C8.3 resulted in higher and lower intrinsic clearance of repaglinide and ibuprofen enantiomers, respectively. repaglinide 101-112 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 27-33 23393219-0 2013 Quantitative prediction of repaglinide-rifampicin complex drug interactions using dynamic and static mechanistic models: delineating differential CYP3A4 induction and OATP1B1 inhibition potential of rifampicin. repaglinide 27-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-152 23393219-1 2013 Repaglinide is mainly metabolized by cytochrome P450 enzymes CYP2C8 and CYP3A4, and it is also a substrate to a hepatic uptake transporter, organic anion transporting polypeptide (OATP)1B1. repaglinide 0-11 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 61-67 23393219-1 2013 Repaglinide is mainly metabolized by cytochrome P450 enzymes CYP2C8 and CYP3A4, and it is also a substrate to a hepatic uptake transporter, organic anion transporting polypeptide (OATP)1B1. repaglinide 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 23393219-1 2013 Repaglinide is mainly metabolized by cytochrome P450 enzymes CYP2C8 and CYP3A4, and it is also a substrate to a hepatic uptake transporter, organic anion transporting polypeptide (OATP)1B1. repaglinide 0-11 solute carrier organic anion transporter family member 1B1 Homo sapiens 180-188 23625433-1 2013 The effect of pitavastatin and SLCO1B1 genetic background on the pharmacokinetic and pharmacodynamic properties of repaglinide was investigated. repaglinide 115-126 solute carrier organic anion transporter family member 1B1 Homo sapiens 31-38 23625433-4 2013 Treatment with pitavastatin significantly increased the peak plasma concentration (Cmax) of repaglinide (P=0.003) in SLCO1B1*1b homozygotes (P=0.015) and SLCO1B1*15 carriers (P=0.031). repaglinide 92-103 solute carrier organic anion transporter family member 1B1 Homo sapiens 117-124 23625433-7 2013 Pitavastatin increased the Cmax of the plasma concentration of repaglinide in an SLCO1B1 genotype dependent manner, but had no apparent effect on the pharmacodynamics of repaglinide in healthy volunteers. repaglinide 63-74 solute carrier organic anion transporter family member 1B1 Homo sapiens 81-88 23526382-13 2013 This study showed the usefulness of CGMS not only as a diagnostic but also as an educational and therapeutic tool that in combination with Repaglinide (with the lowest effective dose and duration) can significantly reduce FBG and glycemic excursions in DM2 patients and hypoglycemic events are low. repaglinide 139-150 immunoglobulin heavy diversity 1-14 (non-functional) Homo sapiens 253-256 23536207-0 2013 Influence of CYP2C8 polymorphisms on the hydroxylation metabolism of paclitaxel, repaglinide and ibuprofen enantiomers in vitro. repaglinide 81-92 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 13-19 23776402-13 2013 Fluvastatin enhanced the oral BA of repaglinide, which may be mainly attributable to the inhibition of the CYP3A4-mediated metabolism of repaglinide in the small intestine and/or liver, to the inhibition of the P-gp efflux transporter in the small intestine and/or to the reduction of TBC of repaglinide by fluvastatin. repaglinide 36-47 phosphoglycolate phosphatase Rattus norvegicus 211-215 22451699-1 2012 Repaglinide is presently recommended by the U.S. Food and Drug Administration as a clinical CYP2C8 probe, yet current in vitro and clinical data are inconsistent concerning the role of this enzyme in repaglinide elimination. repaglinide 0-11 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 92-98 22296034-0 2012 NeuroD1 A45T and PAX4 R121W polymorphisms are associated with plasma glucose level of repaglinide monotherapy in Chinese patients with type 2 diabetes. repaglinide 86-97 neuronal differentiation 1 Homo sapiens 0-7 22296034-0 2012 NeuroD1 A45T and PAX4 R121W polymorphisms are associated with plasma glucose level of repaglinide monotherapy in Chinese patients with type 2 diabetes. repaglinide 86-97 paired box 4 Homo sapiens 17-21 22296034-1 2012 AIMS: We aimed to determine whether NeuroD1/BETA2 and PAX4 polymorphisms were associated with the therapeutic efficacy of repaglinide in Chinese type 2 diabetes mellitus (T2DM) patients. repaglinide 122-133 neuronal differentiation 1 Homo sapiens 36-43 22296034-1 2012 AIMS: We aimed to determine whether NeuroD1/BETA2 and PAX4 polymorphisms were associated with the therapeutic efficacy of repaglinide in Chinese type 2 diabetes mellitus (T2DM) patients. repaglinide 122-133 neuronal differentiation 1 Homo sapiens 44-49 22296034-1 2012 AIMS: We aimed to determine whether NeuroD1/BETA2 and PAX4 polymorphisms were associated with the therapeutic efficacy of repaglinide in Chinese type 2 diabetes mellitus (T2DM) patients. repaglinide 122-133 paired box 4 Homo sapiens 54-58 22296034-10 2012 CONCLUSIONS: The NeuroD1/BETA2 and PAX4 polymorphisms were substantially associated with plasma glucose level after repaglinide monotherapy. repaglinide 116-127 neuronal differentiation 1 Homo sapiens 17-24 22296034-10 2012 CONCLUSIONS: The NeuroD1/BETA2 and PAX4 polymorphisms were substantially associated with plasma glucose level after repaglinide monotherapy. repaglinide 116-127 neuronal differentiation 1 Homo sapiens 25-30 22296034-10 2012 CONCLUSIONS: The NeuroD1/BETA2 and PAX4 polymorphisms were substantially associated with plasma glucose level after repaglinide monotherapy. repaglinide 116-127 paired box 4 Homo sapiens 35-39 23153186-8 2012 The strong CYP2C8 and OATP1B1 inhibitor gemfibrozil increases substantially the plasma concentrations of repaglinide and TZDs. repaglinide 105-116 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 11-17 23153186-8 2012 The strong CYP2C8 and OATP1B1 inhibitor gemfibrozil increases substantially the plasma concentrations of repaglinide and TZDs. repaglinide 105-116 solute carrier organic anion transporter family member 1B1 Homo sapiens 22-29 22966882-0 2012 KCNQ1 variants and response to repaglinide treatment in patients with Type 2 diabetes. repaglinide 31-42 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 0-5 22451699-9 2012 This systematic analysis revealed a comparable in vitro contribution from CYP2C8 and CYP3A4 to the metabolism of repaglinide (<50%), whereas the contribution of glucuronidation ranged from 2 to 20%, depending on the in vitro system used. repaglinide 113-124 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 74-80 22451699-9 2012 This systematic analysis revealed a comparable in vitro contribution from CYP2C8 and CYP3A4 to the metabolism of repaglinide (<50%), whereas the contribution of glucuronidation ranged from 2 to 20%, depending on the in vitro system used. repaglinide 113-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 22451699-10 2012 The repaglinide M4 metabolic pathway is proposed as a specific CYP2C8 probe for the assessment of drug-drug interactions. repaglinide 4-15 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 63-69 22414228-0 2012 KCNQ1 gene polymorphisms are associated with the therapeutic efficacy of repaglinide in Chinese type 2 diabetic patients. repaglinide 73-84 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 0-5 24843581-1 2012 UNLABELLED: Aims/Introduction: Repaglinide is a short-acting insulin secretagogue. repaglinide 32-43 insulin Homo sapiens 62-69 24843581-7 2012 The target HbA1c values of <6.9% were achieved by 75.0% of the repaglinide group vs 59.1% for nateglinide. repaglinide 66-77 hemoglobin subunit alpha 1 Homo sapiens 11-15 22414228-1 2012 The present study evaluated the effects of KCNQ1 rs2237892 and rs2237895 polymorphisms on repaglinide efficacy in Chinese patients with type 2 diabetes mellitus (T2DM). repaglinide 90-101 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 43-48 22414228-9 2012 In conclusion, KCNQ1 rs2237892 and rs2237895 polymorphisms were found to be associated with the therapeutic efficacy of repaglinide in Chinese T2DM patients. repaglinide 120-131 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 15-20 22344703-3 2012 In this study, we have assessed the predictability of human PK for seven organic anion-transporting polypeptide (OATP) substrates (pravastatin, cerivastatin, bosentan, fluvastatin, rosuvastatin, valsartan, and repaglinide) for which clinical intravenous data were available. repaglinide 210-221 solute carrier organic anion transporter family member 1A2 Homo sapiens 113-117 22083559-0 2012 Importance of the Kir6.2 N-terminus for the interaction of glibenclamide and repaglinide with the pancreatic K(ATP) channel. repaglinide 77-88 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 18-24 22083559-6 2012 Kir and SUR were transiently coexpressed in HEK cells and [(3)H]glibenclamide binding and patch-clamp experiments were performed in whole cells at 37 C and in isolated inside/out patches at 22 C. Truncation of the first 5 N-terminal amino acids abolished most of the affinity increase for glibenclamide and repaglinide that is produced by the association of Kir6.2 with SUR1. repaglinide 307-318 killer cell immunoglobulin like receptor, two Ig domains and long cytoplasmic tail 4 Homo sapiens 0-3 22424623-1 2012 OBJECTIVE: To investigate a potential relationship between Solute carrier family 30 (zinc transporter) member 8 (SLC30A8) rs13266634 variant and efficacy of rosiglitazone or repaglinide in treating newly diagnosed Chinese type 2 diabetes patients. repaglinide 174-185 solute carrier family 30 member 8 Homo sapiens 59-111 22424623-1 2012 OBJECTIVE: To investigate a potential relationship between Solute carrier family 30 (zinc transporter) member 8 (SLC30A8) rs13266634 variant and efficacy of rosiglitazone or repaglinide in treating newly diagnosed Chinese type 2 diabetes patients. repaglinide 174-185 solute carrier family 30 member 8 Homo sapiens 113-120 22424623-0 2012 Association of a SLC30A8 genetic variant with monotherapy of repaglinide and rosiglitazone effect in newly diagnosed type 2 diabetes patients in China. repaglinide 61-72 solute carrier family 30 member 8 Homo sapiens 17-24 22393835-0 2012 Effect of genetic polymorphism of UCP2-866 G/A on repaglinide response in Chinese patients with type 2 diabetes. repaglinide 50-61 uncoupling protein 2 Homo sapiens 34-38 21923736-12 2012 Tolbutamide and repaglinide may have partial pancreatic receptor selectivity because IC(50) values for SUR1 and SUR2A/SUR2B overlapped somewhat, with the C(SS) in the midst of these values. repaglinide 16-27 ATP binding cassette subfamily C member 8 Homo sapiens 103-107 22210483-9 2012 Present study has raised the awareness of potential drug interactions by concomitant use of efonidipine with repaglinide, since efonidipine may alter the absorption and/or elimination of repaglinide by the inhibition of CYP3A4 and P-gp efflux pump. repaglinide 109-120 phosphoglycolate phosphatase Rattus norvegicus 231-235 22393835-1 2012 The aim of the present study was to evaluate the impact of the UCP2-866 G/A polymorphism on the efficacy of repaglinide in treating patients with diabetes mellitus type 2 (T2DM). repaglinide 108-119 uncoupling protein 2 Homo sapiens 63-67 22393835-3 2012 16 patients with GG genotype, 14 with GA genotype and 11 with AA genotype of UCP2-866 G/A underwent an 8-week repaglinide treatment regimen. repaglinide 110-121 uncoupling protein 2 Homo sapiens 77-81 22393835-6 2012 After repaglinide treatment for 8 consecutive weeks, we found that A allele carriers of UCP2 in the T2DM patients had smaller decrease in FPG (P < 0.05) and HbA1c (P < 0.05), and smaller increase in 30-min postload plasma insulin (P < 0.01) compared with GG genotypes. repaglinide 6-17 uncoupling protein 2 Homo sapiens 88-92 22393835-7 2012 We demonstrated that UCP2-866 G/A polymorphism is associated with the therapeutic efficacy of repaglinide in Chinese T2DM patients. repaglinide 94-105 uncoupling protein 2 Homo sapiens 21-25 22398664-0 2012 The Influence of MDR1 G2677T/a genetic polymorphisms on the pharmacokinetics of repaglinide in healthy Chinese volunteers. repaglinide 80-91 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 22398664-5 2012 RESULTS: The area under the plasma concentration-time curve from time 0 to infinity (AUC((0-inf))) of repaglinide was significantly higher in subjects possessing the MDR1 2677GT and 2677TT alleles than in those with the MDR1 2677GG and 2677TA alleles (p = 0.007). repaglinide 102-113 ATP binding cassette subfamily B member 1 Homo sapiens 166-170 22398664-5 2012 RESULTS: The area under the plasma concentration-time curve from time 0 to infinity (AUC((0-inf))) of repaglinide was significantly higher in subjects possessing the MDR1 2677GT and 2677TT alleles than in those with the MDR1 2677GG and 2677TA alleles (p = 0.007). repaglinide 102-113 ATP binding cassette subfamily B member 1 Homo sapiens 220-224 22398664-8 2012 CONCLUSION: This study shows that the genetic polymorphisms of MDR1 G2677T/A might explain the variability in the pharmacokinetics of repaglinide in the Chinese population. repaglinide 134-145 ATP binding cassette subfamily B member 1 Homo sapiens 63-67 21835486-6 2011 Repaglinide was also associated with an increase in the AUC(60) and AUC(120) for insulin (+56%, +61%) and C-peptide (+41%, +36%). repaglinide 0-11 insulin Homo sapiens 81-88 21835486-6 2011 Repaglinide was also associated with an increase in the AUC(60) and AUC(120) for insulin (+56%, +61%) and C-peptide (+41%, +36%). repaglinide 0-11 insulin Homo sapiens 106-115 21835486-9 2011 CONCLUSION: Repaglinide is associated with improved postprandial glycaemic control via insulin and C-peptide release. repaglinide 12-23 insulin Homo sapiens 87-94 21835486-9 2011 CONCLUSION: Repaglinide is associated with improved postprandial glycaemic control via insulin and C-peptide release. repaglinide 12-23 insulin Homo sapiens 99-108 21778352-0 2011 Dose-dependent interaction between gemfibrozil and repaglinide in humans: strong inhibition of CYP2C8 with subtherapeutic gemfibrozil doses. repaglinide 51-62 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 95-101 20598356-8 2011 SUR1 is selectively expressed in rat taste buds, and its distribution pattern may be functionally relevant, suggesting that the rapid insulin secretion-promoting effect of repaglinide may be exerted through the cephalic-phase secretion pathway mediated by taste buds. repaglinide 172-183 ATP binding cassette subfamily C member 8 Rattus norvegicus 0-4 21477042-13 2011 Repaglinide had no effect on adipogenesis, although it causes insulin liberation like SUs. repaglinide 0-11 insulin Homo sapiens 62-69 21631570-0 2011 NAMPT -3186C/T polymorphism affects repaglinide response in Chinese patients with Type 2 diabetes mellitus. repaglinide 36-47 nicotinamide phosphoribosyltransferase Homo sapiens 0-5 21631570-11 2011 The data suggest that the NAMPT -3186C>T polymorphism is significantly associated with plasma levels of PINS and CHO in Chinese T2DM patients with repaglinide monotherapy. repaglinide 150-161 nicotinamide phosphoribosyltransferase Homo sapiens 26-31 21590629-8 2011 Patients with MODY 3 were changed from insulin to repaglinide, those with MODY 2 were recommended discontinuing insulin treatment. repaglinide 50-61 HNF1 homeobox A Homo sapiens 14-20 21327909-0 2011 Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers. repaglinide 81-92 solute carrier organic anion transporter family member 1B1 Homo sapiens 11-18 21327909-2 2011 The objective of this research was to study the effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers. repaglinide 129-140 solute carrier organic anion transporter family member 1B1 Homo sapiens 59-66 21327909-9 2011 CONCLUSIONS: SLCO1B1*1B/*1B genotype is associated with reduced pharmacokinetic exposure after a single dose oral administration of 2 mg repaglinide, including decreased AUC(0- ) and increased clearance of repaglinide. repaglinide 137-148 solute carrier organic anion transporter family member 1B1 Homo sapiens 13-20 21327909-9 2011 CONCLUSIONS: SLCO1B1*1B/*1B genotype is associated with reduced pharmacokinetic exposure after a single dose oral administration of 2 mg repaglinide, including decreased AUC(0- ) and increased clearance of repaglinide. repaglinide 206-217 solute carrier organic anion transporter family member 1B1 Homo sapiens 13-20 21327909-10 2011 Moreover, this polymorphism of SLCO1B1 has significant influence on the pharmacokinetics of repaglinide, but no effects on its pharmacodynamics. repaglinide 92-103 solute carrier organic anion transporter family member 1B1 Homo sapiens 31-38 21362360-1 2011 BACKGROUND: Both repaglinide and gliclazide are insulin secretagogues widely used in the treatment of type 2 diabetes. repaglinide 17-28 insulin Homo sapiens 48-55 21270106-1 2011 The pharmacokinetics of repaglinide shows pronounced interindividual variability, for which several reasons have been considered, including interactions with drugs inhibiting CYP2C8 and CYP2C8 genetic polymorphism. repaglinide 24-35 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 186-192 21270106-3 2011 We studied the effect of CYP2C8*3 on the pharmacokinetics and pharmacodynamics of repaglinide in 29 healthy whites carrying CYP2C8*3/*3 (n = 4), CYP2C8*1/*3 (n = 13), or CYP2C8*1/*1 (n = 12). repaglinide 82-93 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 25-31 21289621-5 2011 Our results indicated that KCNQ1 polymorphisms are associated with repaglinide efficacy, and might also be associated with rosiglitazone response, in Chinese patients with type 2 diabetes. repaglinide 67-78 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 27-32 21175273-0 2011 Effect of repaglinide versus glyburide on postprandial glucose and insulin values in elderly patients with type 2 diabetes. repaglinide 10-21 insulin Homo sapiens 67-74 21175273-1 2011 BACKGROUND: studies in younger patients with diabetes have shown that insulin profiles are more physiologic and postprandial glucose levels are lower with repaglinide than with glyburide. repaglinide 155-166 insulin Homo sapiens 70-77 21175273-5 2011 RESULTS: the 0-30 min area under the curve (AUC) for insulin was higher (glyburide, 294 +- 37 pM; repaglinide, 382 +- 39 pM) (P < 0.01), and the 180-240 min AUC for insulin was lower (glyburide, 325 +- 50 pM; repaglinide, 196 +- 20 pM) (P < 0.01) with repaglinide. repaglinide 100-111 insulin Homo sapiens 53-60 21175273-5 2011 RESULTS: the 0-30 min area under the curve (AUC) for insulin was higher (glyburide, 294 +- 37 pM; repaglinide, 382 +- 39 pM) (P < 0.01), and the 180-240 min AUC for insulin was lower (glyburide, 325 +- 50 pM; repaglinide, 196 +- 20 pM) (P < 0.01) with repaglinide. repaglinide 218-229 insulin Homo sapiens 53-60 21175273-5 2011 RESULTS: the 0-30 min area under the curve (AUC) for insulin was higher (glyburide, 294 +- 37 pM; repaglinide, 382 +- 39 pM) (P < 0.01), and the 180-240 min AUC for insulin was lower (glyburide, 325 +- 50 pM; repaglinide, 196 +- 20 pM) (P < 0.01) with repaglinide. repaglinide 218-229 insulin Homo sapiens 53-60 21175273-8 2011 CONCLUSIONS: we conclude that repaglinide results in a more physiologic insulin profile and less frequent hypoglycemia than glyburide in the elderly. repaglinide 30-41 insulin Homo sapiens 72-79 21270106-0 2011 Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide. repaglinide 78-89 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 14-20 21270106-1 2011 The pharmacokinetics of repaglinide shows pronounced interindividual variability, for which several reasons have been considered, including interactions with drugs inhibiting CYP2C8 and CYP2C8 genetic polymorphism. repaglinide 24-35 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 175-181 21362360-9 2011 The maximum insulin concentration occurred earlier in the repaglinide group than that in the gliclazide group. repaglinide 58-69 insulin Homo sapiens 12-19 30861688-3 2010 Repaglinide, a rapidly acting insulin secretagog, stimulates insulin secretion via closure of ATP-dependent potassium channels on the cell membrane of beta-cells. repaglinide 0-11 insulin Homo sapiens 30-37 21548456-1 2011 Meglitinides (repaglinide and nateglinide) are insulin secretagogues used to treat diabetes mellitus. repaglinide 14-25 insulin Homo sapiens 47-54 22086064-9 2011 In mice challenged systemically or intratracheally with LPS, repaglinide significantly decreased serum tumor necrosis factor alpha level and bronchial alveolar lavage fluid MCP-1 levels, respectively. repaglinide 61-72 tumor necrosis factor Mus musculus 103-130 22086064-9 2011 In mice challenged systemically or intratracheally with LPS, repaglinide significantly decreased serum tumor necrosis factor alpha level and bronchial alveolar lavage fluid MCP-1 levels, respectively. repaglinide 61-72 mast cell protease 1 Mus musculus 173-178 22041697-3 2011 Organic anion transporting polypeptide 1B1 (OATP1B1, gene SLCO1B1) is expressed on the basolateral membrane of hepatocytes and can facilitate hepatic uptake of certain clinically relevant drugs such as statins except for fluvastatin, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, antidiabetic drug (repaglinide) and anticancer drugs (SN-38 and methotrexate). repaglinide 332-343 solute carrier organic anion transporter family member 1B1 Homo sapiens 0-42 22041697-3 2011 Organic anion transporting polypeptide 1B1 (OATP1B1, gene SLCO1B1) is expressed on the basolateral membrane of hepatocytes and can facilitate hepatic uptake of certain clinically relevant drugs such as statins except for fluvastatin, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, antidiabetic drug (repaglinide) and anticancer drugs (SN-38 and methotrexate). repaglinide 332-343 solute carrier organic anion transporter family member 1B1 Homo sapiens 44-51 22041697-3 2011 Organic anion transporting polypeptide 1B1 (OATP1B1, gene SLCO1B1) is expressed on the basolateral membrane of hepatocytes and can facilitate hepatic uptake of certain clinically relevant drugs such as statins except for fluvastatin, angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, antidiabetic drug (repaglinide) and anticancer drugs (SN-38 and methotrexate). repaglinide 332-343 solute carrier organic anion transporter family member 1B1 Homo sapiens 58-65 20809084-0 2010 Association analysis of SLC30A8 rs13266634 and rs16889462 polymorphisms with type 2 diabetes mellitus and repaglinide response in Chinese patients. repaglinide 106-117 solute carrier family 30 member 8 Homo sapiens 24-31 20809084-2 2010 This study aimed to investigate whether the SLC30A8 rs13266634 and rs16889462 polymorphisms were associated with T2DM susceptibility and repaglinide therapeutic efficacy in Chinese T2DM patients. repaglinide 137-148 solute carrier family 30 member 8 Homo sapiens 44-51 20809084-9 2010 CONCLUSIONS: SLC30A8 rs13266634 and rs16889462 polymorphisms were associated with repaglinide therapeutic efficacy in Chinese T2DM patients. repaglinide 82-93 solute carrier family 30 member 8 Homo sapiens 13-20 20406215-5 2010 The SLCO1B1 c.521CC genotype has been associated with an about 60-190% increased, and the SLCO1B1*1B/*1B genotype with an about 30% decreased area under the plasma concentration-time curve of repaglinide. repaglinide 192-203 solute carrier organic anion transporter family member 1B1 Homo sapiens 4-11 20406215-5 2010 The SLCO1B1 c.521CC genotype has been associated with an about 60-190% increased, and the SLCO1B1*1B/*1B genotype with an about 30% decreased area under the plasma concentration-time curve of repaglinide. repaglinide 192-203 solute carrier organic anion transporter family member 1B1 Homo sapiens 90-97 20406215-6 2010 Moreover, SLCO1B1 polymorphism can affect the extent of interaction between OATP1B1 inhibitors and repaglinide. repaglinide 99-110 solute carrier organic anion transporter family member 1B1 Homo sapiens 10-17 20406215-6 2010 Moreover, SLCO1B1 polymorphism can affect the extent of interaction between OATP1B1 inhibitors and repaglinide. repaglinide 99-110 solute carrier organic anion transporter family member 1B1 Homo sapiens 76-83 20406215-7 2010 Accordingly, SLCO1B1 genotyping may help in choosing the optimal starting dose of repaglinide. repaglinide 82-93 solute carrier organic anion transporter family member 1B1 Homo sapiens 13-20 21175442-4 2010 Finally, a panel of human liver microsomes (genotyped for UGT1A1*28 allele status) was used to determine the importance of UGT1A1 in the direct glucuronidation of repaglinide. repaglinide 163-174 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 123-129 21175442-10 2010 UGT1A1 plays a significant role in the glucuronidation of repaglinide. repaglinide 58-69 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 0-6 21175442-12 2010 CONCLUSIONS: Inhibition of UGT enzymes, especially UGT1A1, by gemfibrozil and its glucuronide is an additional mechanism to consider when rationalizing the interaction between repaglinide and gemfibrozil. repaglinide 176-187 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 27-30 21175442-12 2010 CONCLUSIONS: Inhibition of UGT enzymes, especially UGT1A1, by gemfibrozil and its glucuronide is an additional mechanism to consider when rationalizing the interaction between repaglinide and gemfibrozil. repaglinide 176-187 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 51-57 20523342-0 2010 IGF2BP2 variations influence repaglinide response and risk of type 2 diabetes in Chinese population. repaglinide 29-40 insulin like growth factor 2 mRNA binding protein 2 Homo sapiens 0-7 20523342-8 2010 CONCLUSION: The IGF2BP2 rs1470579 and rs4402960 polymorphisms may be associated with the development of T2DM, and these polymorphisms may affect the therapeutic efficacy of repaglinide in Chinese T2DM patients. repaglinide 173-184 insulin like growth factor 2 mRNA binding protein 2 Homo sapiens 16-23 30861688-3 2010 Repaglinide, a rapidly acting insulin secretagog, stimulates insulin secretion via closure of ATP-dependent potassium channels on the cell membrane of beta-cells. repaglinide 0-11 insulin Homo sapiens 61-68 20305679-0 2010 A variation in NOS1AP gene is associated with repaglinide efficacy on insulin resistance in type 2 diabetes of Chinese. repaglinide 46-57 nitric oxide synthase 1 adaptor protein Homo sapiens 15-21 20305679-0 2010 A variation in NOS1AP gene is associated with repaglinide efficacy on insulin resistance in type 2 diabetes of Chinese. repaglinide 46-57 insulin Homo sapiens 70-77 20305679-1 2010 AIM: To investigate a potential association between SNP rs10494366 in the neural nitric oxide synthase adaptor protein (NOS1AP) and efficacy of repaglinide (an insulin secretagogue) in newly diagnosed Shanghai Chinese type 2 diabetes patients. repaglinide 144-155 nitric oxide synthase 1 adaptor protein Homo sapiens 120-126 20305679-1 2010 AIM: To investigate a potential association between SNP rs10494366 in the neural nitric oxide synthase adaptor protein (NOS1AP) and efficacy of repaglinide (an insulin secretagogue) in newly diagnosed Shanghai Chinese type 2 diabetes patients. repaglinide 144-155 insulin Homo sapiens 160-167 20305679-7 2010 After 24-week repaglinide monotherapy, the Delta value of fasting insulin (P=0.019) and HOMA-IR (P=0.011) were significantly different. repaglinide 14-25 insulin Homo sapiens 66-73 20305679-10 2010 CONCLUSION: A common variant in rs10494366 is associated with repaglinide monotherapy efficacy on insulin resistance in newly diagnosed Shanghai Chinese type 2 diabetes patients. repaglinide 62-73 insulin Homo sapiens 98-105 19900993-1 2009 OBJECTIVES: To study the effect of insulin treatment in combination with metformin or an insulin secretagogue, repaglinide, on glycaemic regulation in non-obese patients with type 2 diabetes. repaglinide 111-122 insulin Homo sapiens 89-96 19940232-7 2010 Def erasirox caused increases in repaglinide plasma C(max) and AUC of 1.5-fold to over 2-fold, respectively, with little change in blood glucose measures. repaglinide 33-44 UTP25 small subunit processome component Homo sapiens 0-3 20197475-8 2010 Trimethoprim induced CYP2C8 inhibition, thus increasing the plasma concentration of repaglinide. repaglinide 84-95 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 21-27 20197475-14 2010 CONCLUSIONS: This interaction between TMP/SMX and repaglinide may have involved inhibition of CYP2C8 by trimethoprim. repaglinide 50-61 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 94-100 20054294-0 2010 KCNJ11 Lys23Glu and TCF7L2 rs290487(C/T) polymorphisms affect therapeutic efficacy of repaglinide in Chinese patients with type 2 diabetes. repaglinide 86-97 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 0-6 20054294-0 2010 KCNJ11 Lys23Glu and TCF7L2 rs290487(C/T) polymorphisms affect therapeutic efficacy of repaglinide in Chinese patients with type 2 diabetes. repaglinide 86-97 transcription factor 7 like 2 Homo sapiens 20-26 20054294-9 2010 The KCNJ11 and TCF7L2 polymorphisms were associated with repaglinide efficacy. repaglinide 57-68 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 4-10 20054294-9 2010 The KCNJ11 and TCF7L2 polymorphisms were associated with repaglinide efficacy. repaglinide 57-68 transcription factor 7 like 2 Homo sapiens 15-21 20523106-0 2010 CYP3A4 genetic polymorphism influences repaglinide"s pharmacokinetics. repaglinide 39-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 20523106-1 2010 AIM: To investigate the effects of CYP3A4 and CYP2C8 enzymes on repaglinide"s pharmacokinetics in healthy Malaysian subjects. repaglinide 64-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-41 20523106-1 2010 AIM: To investigate the effects of CYP3A4 and CYP2C8 enzymes on repaglinide"s pharmacokinetics in healthy Malaysian subjects. repaglinide 64-75 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 46-52 20523106-8 2010 However, the CYP3A4 genotype significantly influenced some of repaglinide"s pharmacokinetics, where the mean elimination rate constant was 44.0% lower (p = 0.04) and the mean half-life was 33.8% higher (p = 0.04) in subjects with the CYP3A4*1/*18 genotype as compared to those with the normal CYP3A4*1/*1 genotype. repaglinide 62-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-19 20523106-8 2010 However, the CYP3A4 genotype significantly influenced some of repaglinide"s pharmacokinetics, where the mean elimination rate constant was 44.0% lower (p = 0.04) and the mean half-life was 33.8% higher (p = 0.04) in subjects with the CYP3A4*1/*18 genotype as compared to those with the normal CYP3A4*1/*1 genotype. repaglinide 62-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 234-240 20523106-8 2010 However, the CYP3A4 genotype significantly influenced some of repaglinide"s pharmacokinetics, where the mean elimination rate constant was 44.0% lower (p = 0.04) and the mean half-life was 33.8% higher (p = 0.04) in subjects with the CYP3A4*1/*18 genotype as compared to those with the normal CYP3A4*1/*1 genotype. repaglinide 62-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 234-240 20523106-9 2010 This result confirms that CYP3A4 plays a large role in metabolizing repaglinide. repaglinide 68-79 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 20523106-10 2010 CONCLUSION: Genetic polymorphisms of CYP3A4, specifically CYP3A4*18, play a major role in contributing to the interindividual variability in repaglinide"s pharmacokinetics. repaglinide 141-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 20523106-10 2010 CONCLUSION: Genetic polymorphisms of CYP3A4, specifically CYP3A4*18, play a major role in contributing to the interindividual variability in repaglinide"s pharmacokinetics. repaglinide 141-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-64 19761371-5 2009 Contrary to in vitro data, clinical data suggest that the CYP2C8*3 allele is associated with increased metabolism of the CYP2C8 substrates, rosiglitazone, pioglitazone and repaglinide. repaglinide 172-183 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 58-64 19785645-9 2009 SLCO1B1 polymorphism also affects the pharmacokinetics of many other, but not all (fluvastatin), statins and that of the antidiabetic drug repaglinide, the antihistamine fexofenadine and the endothelin A receptor antagonist atrasentan. repaglinide 139-150 solute carrier organic anion transporter family member 1B1 Homo sapiens 0-7 19531054-1 2009 AIM: To assess the efficacy and safety of a new repaglinide/metformin fixed-dose combination (FDC) tablet administered either twice a day (BID) or three times a day (TID) for the management of type 2 diabetes. repaglinide 48-59 BH3 interacting domain death agonist Homo sapiens 139-142 19761371-5 2009 Contrary to in vitro data, clinical data suggest that the CYP2C8*3 allele is associated with increased metabolism of the CYP2C8 substrates, rosiglitazone, pioglitazone and repaglinide. repaglinide 172-183 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 121-127 19476470-6 2009 Reductions in HbA1c values became apparent at earlier times for repaglinide/metformin FDC BID treatment than rosiglitazone/metformin FDC BID, and final changes in HbA1c were not significantly different between treatment arms (p = 0.8186); thus, the predefined statistical criterion for non-inferiority was met. repaglinide 64-75 BH3 interacting domain death agonist Homo sapiens 90-93 19476470-9 2009 Thus, repaglinide/metformin FDC BID is a clinically feasible alternative to rosiglitazone/metformin FDC BID. repaglinide 6-17 BH3 interacting domain death agonist Homo sapiens 32-35 19754390-9 2009 Glinides (repaglinide and nateglinide) have also been documented to improve endothelial function and lipid profile, to reduce oxidative stress, platelet activity and inflammatory markers, and to diminish the progression of CIMT. repaglinide 10-21 CIMT Homo sapiens 223-227 21437123-3 2009 Repaglinide, a rapid-acting insulin secretagogue, targets PPG, and metformin, an insulin sensitizer, targets FBG. repaglinide 0-11 insulin Homo sapiens 28-35 18777156-6 2009 During the repaglinide treatment, the meal related peaks of C-peptide and free human insulin were about twofold higher than during treatment with insulin aspart. repaglinide 11-22 insulin Homo sapiens 60-69 18777156-6 2009 During the repaglinide treatment, the meal related peaks of C-peptide and free human insulin were about twofold higher than during treatment with insulin aspart. repaglinide 11-22 insulin Homo sapiens 85-92 18777156-6 2009 During the repaglinide treatment, the meal related peaks of C-peptide and free human insulin were about twofold higher than during treatment with insulin aspart. repaglinide 11-22 insulin Homo sapiens 146-153 18777156-7 2009 Proinsulin, GHBP were higher and IAPP levels tended to be higher during repaglinide compared to insulin aspart. repaglinide 72-83 islet amyloid polypeptide Homo sapiens 33-37 18777156-8 2009 Postprandial plasma total cholesterol, triglycerides and apolipoprotein B concentrations were higher on repaglinide than on insulin aspart treatment. repaglinide 104-115 apolipoprotein B Homo sapiens 57-73 18777156-9 2009 Our results show that, at the same glycemic control, treatment with exogenous insulin aspart in comparison with the insulin secretagogue repaglinide result in a lower endogenous insulin secretion, and a tendency towards a less atherogenic postprandial lipid profile. repaglinide 137-148 insulin Homo sapiens 116-123 18777156-1 2009 Our aim was to study, at the same glycemic control, how treatment with either the insulin secretagogue repaglinide or exogenous insulin aspart affects endogenous insulin secretion, plasma insulin and IAPP (islet amyloid polypeptide) levels, GH-IGF (growth hormone-insulin-like growth factor) axis and plasma lipoprotein concentrations in patients with type 2 diabetes. repaglinide 103-114 insulin Homo sapiens 82-89 18777156-1 2009 Our aim was to study, at the same glycemic control, how treatment with either the insulin secretagogue repaglinide or exogenous insulin aspart affects endogenous insulin secretion, plasma insulin and IAPP (islet amyloid polypeptide) levels, GH-IGF (growth hormone-insulin-like growth factor) axis and plasma lipoprotein concentrations in patients with type 2 diabetes. repaglinide 103-114 islet amyloid polypeptide Homo sapiens 200-204 19232035-2 2009 The primary endpoint of the study was to evaluate which add-on treatment between acarbose and repaglinide is more efficacious in reducing PPG. repaglinide 94-105 serglycin Homo sapiens 138-141 19232035-8 2009 After 15 weeks of therapy, the repaglinide-treated patients experienced a significant decrease in HbA(1c) (-1.1%, p < 0.05), FPG (-9.5%, p < 0.05), and PPG (-14.9%, p < 0.05), when compared to the baseline values. repaglinide 31-42 serglycin Homo sapiens 158-161 18844675-0 2008 Reversible binding of antidiabetic drugs, repaglinide and gliclazide, with human serum albumin. repaglinide 42-53 albumin Homo sapiens 81-94 18854776-0 2008 Effects of the SLCO1B1*1B haplotype on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide. repaglinide 84-95 solute carrier organic anion transporter family member 1B1 Homo sapiens 15-22 18854776-2 2008 The aim of this study was to investigate whether the SLCO1B1*1B haplotype affects the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide. repaglinide 127-138 solute carrier organic anion transporter family member 1B1 Homo sapiens 53-60 18854776-4 2008 Plasma repaglinide and nateglinide and blood glucose concentrations were measured for 7 h. RESULTS: The AUC(0-infinity) and Cmax of repaglinide were 32% (P=0.007) and 24% lower (P=0.056) in the individuals with the SLCO1B1*1B/*1B genotype than in those with the SLCO1B1*1A/*1A genotype. repaglinide 132-143 solute carrier organic anion transporter family member 1B1 Homo sapiens 215-222 18854776-4 2008 Plasma repaglinide and nateglinide and blood glucose concentrations were measured for 7 h. RESULTS: The AUC(0-infinity) and Cmax of repaglinide were 32% (P=0.007) and 24% lower (P=0.056) in the individuals with the SLCO1B1*1B/*1B genotype than in those with the SLCO1B1*1A/*1A genotype. repaglinide 132-143 solute carrier organic anion transporter family member 1B1 Homo sapiens 262-269 18854776-5 2008 The mean blood glucose concentration from 0 to 7 h after repaglinide intake was 10% higher in the SLCO1B1*1B/*1B participants than in the SLCO1B1*1A/*1A participants (P=0.007). repaglinide 57-68 solute carrier organic anion transporter family member 1B1 Homo sapiens 98-105 18854776-5 2008 The mean blood glucose concentration from 0 to 7 h after repaglinide intake was 10% higher in the SLCO1B1*1B/*1B participants than in the SLCO1B1*1A/*1A participants (P=0.007). repaglinide 57-68 solute carrier organic anion transporter family member 1B1 Homo sapiens 138-145 18854776-7 2008 CONCLUSION: The SLCO1B1*1B/*1B genotype is associated with reduced plasma concentrations of repaglinide, consistent with an enhanced hepatic uptake by OATP1B1, but has limited effects on the pharmacokinetics of nateglinide. repaglinide 92-103 solute carrier organic anion transporter family member 1B1 Homo sapiens 16-23 20409940-6 2009 The sulfonylurea ligands tolbutamide and repaglinide, but not glibenclamide, increased stretch-promoted ANF secretion. repaglinide 41-52 natriuretic peptide A Rattus norvegicus 104-107 18823304-0 2008 The effect of SLCO1B1 polymorphism on repaglinide pharmacokinetics persists over a wide dose range. repaglinide 38-49 solute carrier organic anion transporter family member 1B1 Homo sapiens 14-21 18823304-3 2008 RESULTS: The mean area under the plasma concentration-time curve from time 0 to infinity (AUC(0-infinity)) of 0.25, 0.5, 1 or 2 mg repaglinide was 82% (95% confidence interval 47, 125), 72% (24, 138), 56% (24, 95) or 108% (59, 171) (P < or = 0.001) larger in participants with the SLCO1B1 c.521CC genotype than in those with the c.521TT genotype, respectively. repaglinide 131-142 solute carrier organic anion transporter family member 1B1 Homo sapiens 284-291 18823304-6 2008 CONCLUSIONS: The effect of SLCO1B1 c.521T-->C polymorphism on the pharmacokinetics of repaglinide persists throughout the clinically relevant dose range. repaglinide 89-100 solute carrier organic anion transporter family member 1B1 Homo sapiens 27-34 18844675-1 2008 Mechanism of interaction of antidiabetic drugs, repaglinide and gliclazide, to human serum albumin has been studied using fluorescence spectroscopic technique. repaglinide 48-59 albumin Homo sapiens 85-98 18844675-2 2008 Repaglinide had much higher affinity for human serum albumin when compared with gliclazide. repaglinide 0-11 albumin Homo sapiens 47-60 18844675-8 2008 Repaglinide and gliclazide are bound to site II on the human serum albumin molecule, and the aromatic ring of 411Tyr appears to be involved in binding within site II. repaglinide 0-11 albumin Homo sapiens 61-74 18187595-0 2008 Different effects of SLCO1B1 polymorphism on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide. repaglinide 90-101 solute carrier organic anion transporter family member 1B1 Homo sapiens 21-28 19238654-0 2008 Effects of gemfibrozil and atorvastatin on the pharmacokinetics of repaglinide in relation to SLCO1B1 polymorphism. repaglinide 67-78 solute carrier organic anion transporter family member 1B1 Homo sapiens 94-101 19238654-2 2008 The mean increase in the repaglinide area under the plasma concentration-time curve from 0 h to infinity (AUC(0-infinity)) produced by gemfibrozil was larger in individuals with the SLCO1B1 c.521CC genotype (n = 6) than in those with the c.521TC (n = 6) and c.521TT (n = 12) genotypes, by factors of 1.56 (P = 0.004) and 1.54 (P = 0.002), respectively. repaglinide 25-36 solute carrier organic anion transporter family member 1B1 Homo sapiens 182-189 19238654-6 2008 In conclusion, the extent of gemfibrozil-repaglinide interaction depends on SLCO1B1 genotype. repaglinide 41-52 solute carrier organic anion transporter family member 1B1 Homo sapiens 76-83 19238654-7 2008 Atorvastatin raises plasma repaglinide concentrations, probably by inhibiting organic anion transporting polypeptide 1B1 (OATP1B1). repaglinide 27-38 solute carrier organic anion transporter family member 1B1 Homo sapiens 78-120 19238654-7 2008 Atorvastatin raises plasma repaglinide concentrations, probably by inhibiting organic anion transporting polypeptide 1B1 (OATP1B1). repaglinide 27-38 solute carrier organic anion transporter family member 1B1 Homo sapiens 122-129 18664331-0 2008 Association of KCNJ11 and ABCC8 genetic polymorphisms with response to repaglinide in Chinese diabetic patients. repaglinide 71-82 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 15-21 18664331-0 2008 Association of KCNJ11 and ABCC8 genetic polymorphisms with response to repaglinide in Chinese diabetic patients. repaglinide 71-82 ATP binding cassette subfamily C member 8 Homo sapiens 26-31 18664331-1 2008 AIM: The aim of this study was to investigate the association of KCNJ11 E23K and ABCC8 exon16-3T/C with the therapeutic effect of repaglinide in patients with type 2 diabetes. repaglinide 130-141 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 65-71 18664331-1 2008 AIM: The aim of this study was to investigate the association of KCNJ11 E23K and ABCC8 exon16-3T/C with the therapeutic effect of repaglinide in patients with type 2 diabetes. repaglinide 130-141 ATP binding cassette subfamily C member 8 Homo sapiens 81-86 18664331-10 2008 CONCLUSION: The KCNJ11 E23K variant was associated with the therapeutic effect of repaglinide. repaglinide 82-93 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 16-22 18664331-11 2008 In addition, The C/C homozygotes of the ABCC8 exon16-3T/C variant responded better to repaglinide in insulin sensitivity than the T/C and T/T genotypes. repaglinide 86-97 ATP binding cassette subfamily C member 8 Homo sapiens 40-45 18664331-11 2008 In addition, The C/C homozygotes of the ABCC8 exon16-3T/C variant responded better to repaglinide in insulin sensitivity than the T/C and T/T genotypes. repaglinide 86-97 insulin Homo sapiens 101-108 17923851-0 2008 Characterization of novel CYP2C8 haplotypes and their contribution to paclitaxel and repaglinide metabolism. repaglinide 85-96 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 26-32 17923851-4 2008 In healthy white subjects, CYP2C8*3 and the two novel haplotypes significantly influenced repaglinide pharmacokinetics in SLCO1B1c.521T/C heterozygous individuals: haplotype B was associated with reduced and haplotype C with increased repaglinide AUC (0-infinity). repaglinide 90-101 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 27-33 17923851-4 2008 In healthy white subjects, CYP2C8*3 and the two novel haplotypes significantly influenced repaglinide pharmacokinetics in SLCO1B1c.521T/C heterozygous individuals: haplotype B was associated with reduced and haplotype C with increased repaglinide AUC (0-infinity). repaglinide 90-101 solute carrier organic anion transporter family member 1B1 Homo sapiens 122-129 18314419-6 2008 However, OATP-mediated BSP and pravastatin uptake and OCT1-mediated MPP(+) and metformin uptake were significantly inhibited by repaglinide (half-maximal inhibitory concentration [IC(50)] 1.6-5.6 micromol/l) and rosiglitazone (IC(50) 5.2-30.4 micromol/l). repaglinide 128-139 solute carrier organic anion transporter family member 1A2 Homo sapiens 9-13 18314419-6 2008 However, OATP-mediated BSP and pravastatin uptake and OCT1-mediated MPP(+) and metformin uptake were significantly inhibited by repaglinide (half-maximal inhibitory concentration [IC(50)] 1.6-5.6 micromol/l) and rosiglitazone (IC(50) 5.2-30.4 micromol/l). repaglinide 128-139 solute carrier family 22 member 1 Homo sapiens 54-58 18505128-6 2008 RESULTS: Similar decreases in fasting blood glucose, 2 hours postprandial blood glucose, and HbA1 c were found in both nateglinide group and repaglinide group without significant differences. repaglinide 141-152 hemoglobin subunit alpha 1 Homo sapiens 93-97 18621529-4 2008 Furthermore, (2R,3R,4S)-hydantoin stimulates the insulin secretion by 150% at 25microM compared with 4-hydroxyisoleucine and insulin secretagogue drug repaglinide. repaglinide 151-162 insulin Homo sapiens 125-132 18187595-2 2008 Participants with SLCO1B1 c.521CC genotype (n = 4) had a 59% (P = 0.001) or 72% (P < 0.001) greater mean area under the plasma repaglinide concentration-time curve (AUC(0-infinity)) than participants with c.521TC (n = 12) or c.521TT (n = 16) genotypes. repaglinide 130-141 solute carrier organic anion transporter family member 1B1 Homo sapiens 18-25 17587398-0 2007 Improvement of insulin sensitivity and beta-cell function by nateglinide and repaglinide in type 2 diabetic patients - a randomized controlled double-blind and double-dummy multicentre clinical trial. repaglinide 77-88 insulin Homo sapiens 15-22 18166815-9 2008 In contrast, fasting levels and AUC of total cholesterol, low-density lipoprotein (LDL) cholesterol, non-high-density lipoprotein (non-HDL) cholesterol and serum insulin were lower during metformin than repaglinide (mean (95% confidence intervals), LDL cholesterol difference metformin versus repaglinide: AUC: -0.17 mmol/l (-0.26; -0.08)). repaglinide 203-214 insulin Homo sapiens 162-169 18166815-9 2008 In contrast, fasting levels and AUC of total cholesterol, low-density lipoprotein (LDL) cholesterol, non-high-density lipoprotein (non-HDL) cholesterol and serum insulin were lower during metformin than repaglinide (mean (95% confidence intervals), LDL cholesterol difference metformin versus repaglinide: AUC: -0.17 mmol/l (-0.26; -0.08)). repaglinide 293-304 insulin Homo sapiens 162-169 17712875-12 2007 A mixed model analysis of variance on the 178 patients who started with combination therapy, either immediately or after a 3-6 month period on diet, showed that metformin plus gliclazide, repaglinide, or pioglitazone was associated with a gradual increase in HbA1c values. repaglinide 188-199 hemoglobin subunit alpha 1 Homo sapiens 259-263 17587398-16 2007 CONCLUSIONS: The efficacy of repaglinide and nateglinide in FBG, postprandial glucose excursion and early-phase insulin secretion is similar. repaglinide 29-40 insulin Homo sapiens 112-119 17587398-19 2007 This trial had shown that nateglinide and repaglinide could comparably improve insulin sensitivity and beta-cell function. repaglinide 42-53 insulin Homo sapiens 79-86