PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 28535976-6 2017 Epigallocatechin gallate, cyclosporin A, rifampicin, and telmisartan inhibited cilostazol uptake in OATP1B1/1B3-HEK293 cells with Ki values close to their clinical plasma concentration, which suggested possible drug-drug interactions in humans via OATP1B1/1B3. Cyclosporine 26-39 solute carrier organic anion transporter family member 1B1 Homo sapiens 100-107 35241487-0 2022 Experimental and modeling evidence supporting the trans-inhibition mechanism for preincubation time-dependent, long-lasting inhibition of organic anion transporting polypeptide (OATP) 1B1 by cyclosporine A. Cyclosporine 191-205 solute carrier organic anion transporter family member 1B1 Homo sapiens 138-187 35241487-1 2022 Cyclosporine A (CsA) and rifampin are potent inhibitors of organic anion transporting polypeptide (OATP) 1B1 and are widely used to assess the risk for drug-drug interactions. Cyclosporine 0-14 solute carrier organic anion transporter family member 1B1 Homo sapiens 59-108 35241487-1 2022 Cyclosporine A (CsA) and rifampin are potent inhibitors of organic anion transporting polypeptide (OATP) 1B1 and are widely used to assess the risk for drug-drug interactions. Cyclosporine 16-19 solute carrier organic anion transporter family member 1B1 Homo sapiens 59-108 35241487-2 2022 CsA displays preincubation time-dependent, long-lasting inhibition of OATP1B1 in vitro and in rats in vivo, and a proposed mechanism is the trans-inhibition by which CsA inhibits OATP1B1 from the inside of cells. Cyclosporine 0-3 solute carrier organic anion transporter family member 1B1 Homo sapiens 70-77 35241487-2 2022 CsA displays preincubation time-dependent, long-lasting inhibition of OATP1B1 in vitro and in rats in vivo, and a proposed mechanism is the trans-inhibition by which CsA inhibits OATP1B1 from the inside of cells. Cyclosporine 0-3 solute carrier organic anion transporter family member 1B1 Homo sapiens 179-186 35241487-2 2022 CsA displays preincubation time-dependent, long-lasting inhibition of OATP1B1 in vitro and in rats in vivo, and a proposed mechanism is the trans-inhibition by which CsA inhibits OATP1B1 from the inside of cells. Cyclosporine 166-169 solute carrier organic anion transporter family member 1B1 Homo sapiens 70-77 35241487-2 2022 CsA displays preincubation time-dependent, long-lasting inhibition of OATP1B1 in vitro and in rats in vivo, and a proposed mechanism is the trans-inhibition by which CsA inhibits OATP1B1 from the inside of cells. Cyclosporine 166-169 solute carrier organic anion transporter family member 1B1 Homo sapiens 179-186 35241487-6 2022 When the OATP1B1-mediated uptake of (3H)estradiol-17beta-glucuronide was measured following preincubation with CsA for 5 to 120 min, apparent Ki values became lower with longer preincubation. Cyclosporine 111-114 solute carrier organic anion transporter family member 1B1 Homo sapiens 9-16 35241487-10 2022 Significance Statement In vitro data and kinetic modeling support that preincubation time-dependent, long-lasting inhibition of OATP1B1 by CsA can be explained by the extensive intracellular binding and reversible OATP1B1 inhibition intracellularly (trans-inhibition) as well as extracellularly (cis-inhibition). Cyclosporine 139-142 solute carrier organic anion transporter family member 1B1 Homo sapiens 128-135 35241487-10 2022 Significance Statement In vitro data and kinetic modeling support that preincubation time-dependent, long-lasting inhibition of OATP1B1 by CsA can be explained by the extensive intracellular binding and reversible OATP1B1 inhibition intracellularly (trans-inhibition) as well as extracellularly (cis-inhibition). Cyclosporine 139-142 solute carrier organic anion transporter family member 1B1 Homo sapiens 214-221 29255993-6 2018 Up to 1% of the patients was exposed to a contraindicated drug-drug interaction, the most frequent drug-drug interaction involving influx-transporter (i.e., OATP1B1) interactions between simvastatin or rosuvastatin with cyclosporin. Cyclosporine 220-231 solute carrier organic anion transporter family member 1B1 Homo sapiens 157-164 28479356-5 2017 The time profiles of RPG and the inhibitors were analyzed by PBPK models, considering the inhibition of OATP1B1 and CYP3A4 by CsA or OATP1B1 inhibition by GEM and its glucuronide and the mechanism-based inhibition of CYP2C8 by GEM glucuronide. Cyclosporine 126-129 solute carrier organic anion transporter family member 1B1 Homo sapiens 104-111 28479356-6 2017 RPG-CsA interaction was closely predicted using a reported in vitro Ki,OATP1B1 value in the presence of CsA preincubation. Cyclosporine 4-7 solute carrier organic anion transporter family member 1B1 Homo sapiens 71-78 31901416-7 2020 The time-dependent inhibition of OATP1B1 was also noted and may be a mechanism underlying the in vitro-in vivo differences in the inhibition constant of cyclosporine A. Cyclosporine 153-167 solute carrier organic anion transporter family member 1B1 Homo sapiens 33-40 31703927-7 2019 However, the reduced OATP1B1 activity by preincubation with pazopanib was more rapidly recovered than CsA. Cyclosporine 102-105 solute carrier organic anion transporter family member 1B1 Homo sapiens 21-28 30982223-3 2019 The current study investigated the effect of OATP1B1 genotype c.521T>C (OATP1B1-Val174Ala) on the extent of interaction between cyclosporin A (CsA) and pravastatin, and associated endogenous biomarkers of the transporter (HDA, TDA, CP-I, and CP-III), in 20 healthy volunteers. Cyclosporine 131-144 solute carrier organic anion transporter family member 1B1 Homo sapiens 45-52 30982223-3 2019 The current study investigated the effect of OATP1B1 genotype c.521T>C (OATP1B1-Val174Ala) on the extent of interaction between cyclosporin A (CsA) and pravastatin, and associated endogenous biomarkers of the transporter (HDA, TDA, CP-I, and CP-III), in 20 healthy volunteers. Cyclosporine 131-144 solute carrier organic anion transporter family member 1B1 Homo sapiens 75-82 30982223-3 2019 The current study investigated the effect of OATP1B1 genotype c.521T>C (OATP1B1-Val174Ala) on the extent of interaction between cyclosporin A (CsA) and pravastatin, and associated endogenous biomarkers of the transporter (HDA, TDA, CP-I, and CP-III), in 20 healthy volunteers. Cyclosporine 146-149 solute carrier organic anion transporter family member 1B1 Homo sapiens 45-52 30982223-3 2019 The current study investigated the effect of OATP1B1 genotype c.521T>C (OATP1B1-Val174Ala) on the extent of interaction between cyclosporin A (CsA) and pravastatin, and associated endogenous biomarkers of the transporter (HDA, TDA, CP-I, and CP-III), in 20 healthy volunteers. Cyclosporine 146-149 solute carrier organic anion transporter family member 1B1 Homo sapiens 75-82 30982223-8 2019 Overall, these results suggest that OATP1B1 genotype can modulate the effects of CsA on biomarker levels; the extent of modulation differs among the biomarkers. Cyclosporine 81-84 solute carrier organic anion transporter family member 1B1 Homo sapiens 36-43 29712725-3 2018 CsA is an inhibitor of organic anion transporting polypeptide (OATP)1B1 and CYP3A4, and GEM and its glucuronide (GEM-glu) inhibit OATP1B1 and CYP2C8. Cyclosporine 0-3 solute carrier organic anion transporter family member 1B1 Homo sapiens 63-71 29712725-3 2018 CsA is an inhibitor of organic anion transporting polypeptide (OATP)1B1 and CYP3A4, and GEM and its glucuronide (GEM-glu) inhibit OATP1B1 and CYP2C8. Cyclosporine 0-3 solute carrier organic anion transporter family member 1B1 Homo sapiens 130-137 29712725-8 2018 The DDIs were then simulated using the established PBPK models with previously obtained in vitro inhibition constants of CsA or GEM/GEM-glu against the OATP1B1 and cytochrome P450s. Cyclosporine 121-124 solute carrier organic anion transporter family member 1B1 Homo sapiens 152-159 27858342-7 2017 Further analysis demonstrated that OATP1B1 inhibition by rifampin or cyclosporine in the existing inhibitor models needs to be approximately tenfold stronger to recapitulate the observed DDI with these two inhibitors. Cyclosporine 69-81 solute carrier organic anion transporter family member 1B1 Homo sapiens 35-42 27858342-8 2017 CONCLUSION: Through quantitative assessment of the effect of OATP1B1 genetic polymorphism and inhibitors of transporters and metabolizing enyzmes via PBPK modeling, we confirmed the importance of OATP1B1 in the disposition of these two statins, and explored potential causes for under-prediction of the inhibitory effect of rifampin and cyclosporine. Cyclosporine 337-349 solute carrier organic anion transporter family member 1B1 Homo sapiens 61-68 27858342-8 2017 CONCLUSION: Through quantitative assessment of the effect of OATP1B1 genetic polymorphism and inhibitors of transporters and metabolizing enyzmes via PBPK modeling, we confirmed the importance of OATP1B1 in the disposition of these two statins, and explored potential causes for under-prediction of the inhibitory effect of rifampin and cyclosporine. Cyclosporine 337-349 solute carrier organic anion transporter family member 1B1 Homo sapiens 196-203 26353895-8 2016 Cyclosporine is an inhibitor of OATP1B1/3, BCRP and P-gp, and a mild inhibitor of CYP3A; cyclosporine causes a significant increase in simeprevir plasma concentrations, and coadministration is not recommended. Cyclosporine 0-12 solute carrier organic anion transporter family member 1B1 Homo sapiens 32-41 27447836-3 2016 Of these, 12 metabolites were significantly higher in plasma samples from volunteers dosed with the OATP1B1 inhibitor, cyclosporine (CSA) vs. placebo (q-value < 0.2). Cyclosporine 119-131 solute carrier organic anion transporter family member 1B1 Homo sapiens 100-107 27447836-3 2016 Of these, 12 metabolites were significantly higher in plasma samples from volunteers dosed with the OATP1B1 inhibitor, cyclosporine (CSA) vs. placebo (q-value < 0.2). Cyclosporine 133-136 solute carrier organic anion transporter family member 1B1 Homo sapiens 100-107 26961540-8 2017 From the further evaluation with the typical inhibitors of each transporter, it was confirmed that BPS is a substrate for P-gp, BCRP, OAT3, OATP1B1, OATP1B3 and MRP2, because the typical inhibitor, cyclosporine, had no effects on BPS transport by BSEP. Cyclosporine 198-210 solute carrier organic anion transporter family member 1B1 Homo sapiens 140-147 27603548-4 2016 Pre-incubation with cyclosporine A, but not with rifampicin, decreased the apparent IC50 values on recombinant cynomolgus monkey OATP1B1- and OATP1B3-mediated pitavastatin uptake. Cyclosporine 20-34 solute carrier organic anion transporter family member 1B1 Homo sapiens 129-136 25522788-6 2015 Patients of the CASLAMB trial received CAS in combination with cyclosporine A (CsA), which leads to an increased AUC0-24h of CAS hypothetically due to an inhibition of the hepatic transport protein OATP1B1 by CsA. Cyclosporine 63-77 solute carrier organic anion transporter family member 1B1 Homo sapiens 198-205 25522788-6 2015 Patients of the CASLAMB trial received CAS in combination with cyclosporine A (CsA), which leads to an increased AUC0-24h of CAS hypothetically due to an inhibition of the hepatic transport protein OATP1B1 by CsA. Cyclosporine 79-82 solute carrier organic anion transporter family member 1B1 Homo sapiens 198-205 23886114-6 2014 OATP1B1 and OATP1B3-mediated transport of bilirubin was confirmed and inhibition was determined for atazanavir, rifampicin, indinavir, amprenavir, cyclosporine, rifamycin SV and saquinavir. Cyclosporine 147-159 solute carrier organic anion transporter family member 1B1 Homo sapiens 0-7 25414411-4 2015 Effects of cyclosporine A (CsA), rifampin, and gemfibrozil on OATP1B1-mediated uptake of 12 substrate drugs were examined in OATP1B1-expressing human embryonic kidney 293 cells. Cyclosporine 27-30 solute carrier organic anion transporter family member 1B1 Homo sapiens 62-69 25414411-7 2015 Preincubation potentiated the inhibitory effect of CsA on OATP1B1 with similar magnitude regardless of the substrates. Cyclosporine 51-54 solute carrier organic anion transporter family member 1B1 Homo sapiens 58-65 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. Cyclosporine 113-125 solute carrier organic anion transporter family member 1B1 Homo sapiens 87-94 22240838-5 2012 The pretreatment of OATP1B1- and OATP1B3-expressing cells with 0.5-10 microM CsA, but not TCR, resulted in a reduction in their activity, even after washing out CsA from the incubation media. Cyclosporine 161-164 solute carrier organic anion transporter family member 1B1 Homo sapiens 20-27 23440887-5 2013 Among them, saquinavir and ritonavir in addition to CsA exhibited long-lasting inhibitory effects on OATP1B1-mediated transport of E1 S at >= 5 and 25 muM, respectively, even after they were washed out from the incubation buffer. Cyclosporine 52-55 solute carrier organic anion transporter family member 1B1 Homo sapiens 101-108 23440887-8 2013 The present study firstly showed that saquinavir and ritonavir as well as CsA have long-lasting inhibitory effects on OATP1B1. Cyclosporine 74-77 solute carrier organic anion transporter family member 1B1 Homo sapiens 118-125 22240838-0 2012 Long-lasting inhibitory effects of cyclosporin A, but not tacrolimus, on OATP1B1- and OATP1B3-mediated uptake. Cyclosporine 35-48 solute carrier organic anion transporter family member 1B1 Homo sapiens 73-80 22240838-1 2012 Cyclosporin A (CsA) causes a number of clinically relevant drug-drug interactions (DDIs) by inhibiting OATP1B1 and OATP1B3. Cyclosporine 0-13 solute carrier organic anion transporter family member 1B1 Homo sapiens 103-110 22240838-6 2012 Preincubating the cells with CsA significantly enhanced its inhibitory effects on OATP1B1 and OATP1B3 by coincubation at 0.1-1 microM. Cyclosporine 29-32 solute carrier organic anion transporter family member 1B1 Homo sapiens 82-89 22240838-1 2012 Cyclosporin A (CsA) causes a number of clinically relevant drug-drug interactions (DDIs) by inhibiting OATP1B1 and OATP1B3. Cyclosporine 15-18 solute carrier organic anion transporter family member 1B1 Homo sapiens 103-110 22240838-7 2012 Preincubation with 1 microM CsA caused a reduction in OATP1B1 activity for at least 18 h after its removal. Cyclosporine 28-31 solute carrier organic anion transporter family member 1B1 Homo sapiens 54-61 22240838-5 2012 The pretreatment of OATP1B1- and OATP1B3-expressing cells with 0.5-10 microM CsA, but not TCR, resulted in a reduction in their activity, even after washing out CsA from the incubation media. Cyclosporine 77-80 solute carrier organic anion transporter family member 1B1 Homo sapiens 20-27 22240838-10 2012 Thus, CsA has a long-lasting inhibitory effect on OATP1B1 and OATP1B3. Cyclosporine 6-9 solute carrier organic anion transporter family member 1B1 Homo sapiens 50-57 21430235-5 2011 Finally, budesonide, cyclosporine, and rifampin were identified as inhibitors of OATP1B1-, OATP1B3-, and OATP2B1-meditated mesalazine uptake. Cyclosporine 21-33 solute carrier organic anion transporter family member 1B1 Homo sapiens 81-88 21297316-3 2011 Among these drugs, cyclosporin A markedly increases the plasma concentrations of OATP1B1 substrates. Cyclosporine 19-32 solute carrier organic anion transporter family member 1B1 Homo sapiens 81-88 20519340-1 2010 The aim of this study was to investigate the potential of calcineurin inhibitors [cyclosporine A (CsA) and tacrolimus (Tac)] to inhibit cellular uptake of atorvastatin mediated by the liver-specific organic anion-transporting polypeptide 1B1 (OATP1B1) in vitro. Cyclosporine 82-96 solute carrier organic anion transporter family member 1B1 Homo sapiens 243-250 21245207-9 2011 Certain drugs (e.g., cyclosporine) potently inhibit OATP1B1, causing clinically significant drug interactions. Cyclosporine 21-33 solute carrier organic anion transporter family member 1B1 Homo sapiens 52-59 20540932-10 2010 Molecules known to interact with OATPs, including cyclosporin A, rifampicin, and glibenclamide, each demonstrated concentration-dependent inhibition of 8-FcA transport by OATP1B1 and OATP1B3. Cyclosporine 50-63 solute carrier organic anion transporter family member 1B1 Homo sapiens 171-178 17496208-0 2007 Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Cyclosporine 132-145 solute carrier organic anion transporter family member 1B1 Homo sapiens 33-40 17901929-5 2008 Gemfibrozil and cyclosporine inhibition data obtained in human embryonic kidney cells expressing OATP1B1 and hepatic input concentration ([I]in) were used for qualitative zoning of 14 transporter-mediated DDIs. Cyclosporine 16-28 solute carrier organic anion transporter family member 1B1 Homo sapiens 97-104 18192894-1 2008 OBJECTIVE: To evaluate whether variations in the ABCB1, ABCC2, SLCO1B1, CYP3A4, CYP3A5, or NR1I2 genes are associated with the pharmacokinetics of cyclosporine in pediatric renal transplant candidates, and whether the effects of these variants are related to age. Cyclosporine 147-159 solute carrier organic anion transporter family member 1B1 Homo sapiens 63-70 14530907-7 2003 Additional inhibitors of phalloidin uptake mediated by SLC21A6 included the immunosuppressive drugs cyclosporin A, FK506, and rapamycin, whereas alpha-amanitin was only a weak inhibitor. Cyclosporine 100-113 solute carrier organic anion transporter family member 1B1 Homo sapiens 55-62 14530907-8 2003 Cyclosporin A was a most potent competitive inhibitor for SLC21A6-mediated phalloidin transport with a K(i) value of 51 nM. Cyclosporine 0-13 solute carrier organic anion transporter family member 1B1 Homo sapiens 58-65 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 0-12 solute carrier organic anion transporter family member 1B1 Homo sapiens 98-140 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 0-12 solute carrier organic anion transporter family member 1B1 Homo sapiens 142-149 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 19-30 solute carrier organic anion transporter family member 1B1 Homo sapiens 98-140 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 19-30 solute carrier organic anion transporter family member 1B1 Homo sapiens 142-149 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). Cyclosporine 14-26 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. Cyclosporine 13-25 solute carrier organic anion transporter family member 1B1 Homo sapiens 141-148 16316932-7 2005 Cyclosporin A significantly inhibited OATP1B1 and P-gp, whereas only moderate inhibition was observed on MRP2. Cyclosporine 0-13 solute carrier organic anion transporter family member 1B1 Homo sapiens 38-45 16541750-5 2005 Furthemore, recent mechanistic studies have shown organic anion transporting peptides (OATP) C to mediate the uptake of some statins and cyclosporine has been shown to inhibit the uptake via OATP-C in cultured cells. Cyclosporine 137-149 solute carrier organic anion transporter family member 1B1 Homo sapiens 191-197 15289793-16 2004 The in vitro results demonstrate that rosuvastatin is a good substrate for OATP-C-mediated hepatic uptake (association constant, 8.5 +/- 1.1 micromol/L) and that cyclosporine is an effective inhibitor of this process (50% inhibition constant, 2.2 +/- 0.4 micromol/L when the rosuvastatin concentration was 5 micromol/L). Cyclosporine 162-174 solute carrier organic anion transporter family member 1B1 Homo sapiens 75-81 15289793-18 2004 Cyclosporine inhibition of OATP-C-mediated rosuvastatin hepatic uptake may be the mechanism of the drug-drug interaction. Cyclosporine 0-12 solute carrier organic anion transporter family member 1B1 Homo sapiens 27-33 12538813-7 2003 Saturable OATP2-mediated uptake of [(14)C]CER was observed and was also inhibited by CsA, with a K(i) value of 0.2 microM. Cyclosporine 85-88 solute carrier organic anion transporter family member 1B1 Homo sapiens 10-15 12538813-8 2003 These results suggest that the DDI between CER and CsA involves the inhibition of transporter-mediated uptake of CER and, at least in part, its OATP2-mediated uptake. Cyclosporine 51-54 solute carrier organic anion transporter family member 1B1 Homo sapiens 144-149 12538813-11 2003 From these results, we conclude that the DDI between CER and CsA is mainly due to the inhibition of transporter (at least partly OATP2)-mediated uptake in the liver. Cyclosporine 61-64 solute carrier organic anion transporter family member 1B1 Homo sapiens 129-134