SLC transporters as therapeutic targets: emerging opportunities
Solute carrier (SLC) transporters—a family of more than 300 membrane-bound proteins that
facilitate the transport of a wide array of substrates across biological membranes—have …
facilitate the transport of a wide array of substrates across biological membranes—have …
The next frontier in ADME science: Predicting transporter-based drug disposition, tissue concentrations and drug-drug interactions in humans
Predicting transporter-based drug clearance (CL) and tissue concentrations (TC) in humans
is important to reduce the risk of failure during drug development. In addition, when …
is important to reduce the risk of failure during drug development. In addition, when …
Coproporphyrins in plasma and urine can be appropriate clinical biomarkers to recapitulate drug-drug interactions mediated by organic anion transporting polypeptide …
Y Lai, S Mandlekar, H Shen, VK Holenarsipur… - … of Pharmacology and …, 2016 - ASPET
In the present study, an open-label, three-treatment, three-period clinical study of
rosuvastatin (RSV) and rifampicin (RIF) when administered alone and in combination was …
rosuvastatin (RSV) and rifampicin (RIF) when administered alone and in combination was …
SLC family transporters
X Liu - Drug transporters in drug disposition, effects and …, 2019 - Springer
Solute carrier (SLC) family transporters utilize an electrochemical potential difference or an
ion gradient generated by primary active transporters for transporting their substrates across …
ion gradient generated by primary active transporters for transporting their substrates across …
Investigation of the impact of substrate selection on in vitro organic anion transporting polypeptide 1B1 inhibition profiles for the prediction of drug-drug interactions
The risk assessment of organic anion transporting polypeptide (OATP) 1B1–mediated drug-
drug interactions (DDIs) is an indispensable part of drug development. We previously …
drug interactions (DDIs) is an indispensable part of drug development. We previously …
Pitavastatin is a more sensitive and selective organic anion‐transporting polypeptide 1B clinical probe than rosuvastatin
T Prueksaritanont, X Chu, R Evers… - British journal of …, 2014 - Wiley Online Library
Aims Rosuvastatin and pitavastatin have been proposed as probe substrates for the organic
anion‐transporting polypeptide (OATP) 1 B, but clinical data on their relative sensitivity and …
anion‐transporting polypeptide (OATP) 1 B, but clinical data on their relative sensitivity and …
Organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 as important regulators of the pharmacokinetics of substrate drugs
K Maeda - Biological and Pharmaceutical Bulletin, 2015 - jstage.jst.go.jp
Nobody doubts the importance of organic anion transporting polypeptide (OATP) 1B1 and
1B3 in the clinical pharmacokinetics of substrate drugs. Based on the theory of …
1B3 in the clinical pharmacokinetics of substrate drugs. Based on the theory of …
Evaluation of ketoconazole and its alternative clinical CYP3A4/5 inhibitors as inhibitors of drug transporters: the in vitro effects of ketoconazole, ritonavir, clarithromycin …
LMM Vermeer, CD Isringhausen, BW Ogilvie… - Drug metabolism and …, 2016 - ASPET
Ketoconazole is a potent CYP3A4/5 inhibitor and, until recently, recommended by the Food
and Drug Administration (FDA) and the European Medicines Agency as a strong CYP3A4/5 …
and Drug Administration (FDA) and the European Medicines Agency as a strong CYP3A4/5 …
In vitro liver toxicity testing of chemicals: A pragmatic approach
A Tabernilla, B dos Santos Rodrigues… - International journal of …, 2021 - mdpi.com
The liver is among the most frequently targeted organs by noxious chemicals of diverse
nature. Liver toxicity testing using laboratory animals not only raises serious ethical …
nature. Liver toxicity testing using laboratory animals not only raises serious ethical …
Coproporphyrins I and III as functional markers of OATP1B activity: in vitro and in vivo evaluation in preclinical species
H Shen, J Dai, T Liu, Y Cheng, W Chen… - … of Pharmacology and …, 2016 - ASPET
Inhibition of organic anion-transporting polypeptide (OATP) 1B function can lead to serious
clinical drug-drug interactions, thus a thorough evaluation of the potential for this type of …
clinical drug-drug interactions, thus a thorough evaluation of the potential for this type of …