PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 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 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 solute carrier organic anion transporter family member 1B1 Homo sapiens 94-101 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 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 solute carrier organic anion transporter family member 1B1 Homo sapiens 87-94 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 solute carrier organic anion transporter family member 1B1 Homo sapiens 141-148 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 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 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 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 13-16 solute carrier organic anion transporter family member 1B1 Homo sapiens 51-58