Contribution of organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 to hepatic uptake of nateglinide, and the prediction of drug-drug interactions via these transporters

2011 ◽  
Vol 64 (2) ◽  
pp. 199-206 ◽  
Author(s):  
Toshiyuki Takanohashi ◽  
Satoru Kubo ◽  
Harumi Arisaka ◽  
Kenji Shinkai ◽  
Kazuyuki Ubukata
Keyword(s):  
Drug Interactions ◽  
Organic Anion ◽  
Hepatic Uptake ◽  
Organic Anion Transporting Polypeptide

scholarly journals Characterization of Organic Anion Transporting Polypeptide 1b2-null Mice: Essential Role in Hepatic Uptake/Toxicity of Phalloidin and Microcystin-LR

2008 ◽  
Vol 103 (1) ◽  
pp. 35-45 ◽  
Author(s):  
Hong Lu ◽  
Supratim Choudhuri ◽  
Kenichiro Ogura ◽  
Iván L. Csanaky ◽  
Xiaohong Lei ◽  
...  
Keyword(s):  
Essential Role ◽  
Organic Anion ◽  
Hepatic Uptake ◽  
Organic Anion Transporting Polypeptide

Fentanyl Pharmacokinetics is not Dependent on Hepatic Uptake by Organic Anion-Transporting Polypeptide 1B1 in Human Beings

2013 ◽  
Vol 113 (1) ◽  
pp. 43-48 ◽  
Author(s):  
Victoria C. Ziesenitz ◽  
Sonja K. König ◽  
Nina Mahlke ◽  
Ricarda Jantos ◽  
Gisela Skopp ◽  
...  
Keyword(s):  
Organic Anion ◽  
Hepatic Uptake ◽  
Human Beings ◽  
Organic Anion Transporting Polypeptide

Pitavastatin as an In Vivo Probe for Studying Hepatic Organic Anion Transporting Polypeptide-Mediated Drug–Drug Interactions in Cynomolgus Monkeys

2013 ◽  
Vol 41 (10) ◽  
pp. 1875-1882 ◽  
Author(s):  
Tsuyoshi Takahashi ◽  
Tatsuyuki Ohtsuka ◽  
Takahiro Yoshikawa ◽  
Ichiro Tatekawa ◽  
Yasuhiro Uno ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Organic Anion ◽  
Cynomolgus Monkeys ◽  
Organic Anion Transporting Polypeptide

scholarly journals Raltegravir Has a Low Propensity To Cause Clinical Drug Interactions through Inhibition of Major Drug Transporters: anIn VitroEvaluation

2013 ◽  
Vol 58 (3) ◽  
pp. 1294-1301 ◽  
Author(s):  
Matthew L. Rizk ◽  
Robert Houle ◽  
Grace Hoyee Chan ◽  
Mike Hafey ◽  
Elizabeth G. Rhee ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Organic Cation ◽  
Drug Transporters ◽  
Organic Anion ◽  
Organic Cation Transporter ◽  
Hepatic Uptake ◽  
Efflux Transporters ◽  
Renal Uptake ◽  
No Inhibition ◽  
Uptake Transporters

ABSTRACTRaltegravir (RAL) is a human immunodeficiency virus type 1 (HIV-1) integrase inhibitor approved to treat HIV infection in adults in combination with other antiretrovirals. The potential of RAL to cause transporter-related drug-drug interactions (DDIs) as an inhibitor has not been well described to date. In this study, a series ofin vitroexperiments were conducted to assess the inhibitory effects of RAL on major human drug transporters known to be involved in clinically relevant drug interactions, including hepatic and renal uptake transporters and efflux transporters. For hepatic uptake transporters, RAL showed no inhibition of organic anion-transporting polypeptide 1B1 (OATP1B1), weak inhibition of OATP1B3 (40% inhibition at 100 μM), and no inhibition of organic cation transporter 1 (OCT1). Studies of renal uptake transporters showed that RAL inhibited organic anion transporters 1 and 3 (OAT1 and OAT3) with 50% inhibitory concentrations (IC50s) (108 μM and 18.8 μM, respectively) well above the maximum concentration of drug in plasma (Cmax) at the clinical 400-mg dose and did not inhibit organic cation transporter 2 (OCT2). As for efflux transporters, RAL did not inhibit breast cancer resistance protein (BCRP) and showed weak inhibition of multidrug and toxin extrusion protein 1 (MATE1) (52% inhibition at 100 μM) and MATE2-K (29% inhibition at 100 μM). These studies indicate that at clinically relevant exposures, RAL does not inhibit or only weakly inhibits hepatic uptake transporters OATP1B1, OATP1B3, and OCT1, renal uptake transporters OCT2, OAT1, and OAT3, as well as efflux transporters BCRP, MATE1, and MATE2-K. The propensity for RAL to cause DDIs via inhibition of these transporters is therefore considered low.

scholarly journals Glycyrrhizin has a high likelihood to be a victim of drug-drug interactions mediated by hepatic organic anion-transporting polypeptide 1B1/1B3

2018 ◽  
Vol 175 (17) ◽  
pp. 3486-3503 ◽  
Author(s):  
Jiajia Dong ◽  
Olajide E Olaleye ◽  
Rongrong Jiang ◽  
Jing Li ◽  
Chuang Lu ◽  
...  
Keyword(s):  
Drug Interactions ◽  
Organic Anion ◽  
High Likelihood ◽  
Organic Anion Transporting Polypeptide
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