Predicting the human hepatic clearance of acidic and zwitterionic drugs
DA Tess, H Eng, AS Kalgutkar, J Litchfield… - Journal of Medicinal …, 2020 - ACS Publications
Prospective predictions of human hepatic clearance for anionic/zwitterionic compounds,
which are oftentimes subjected to transporter-mediated uptake, are challenging in drug …
which are oftentimes subjected to transporter-mediated uptake, are challenging in drug …
Hepatic Disposition of Gemfibrozil and Its Major Metabolite Gemfibrozil 1-O-β-Glucuronide
Gemfibrozil (GEM), which decreases serum triglycerides and low density lipoprotein,
perpetrates drug–drug interactions (DDIs) with several drugs. These DDIs are primarily …
perpetrates drug–drug interactions (DDIs) with several drugs. These DDIs are primarily …
Recent advances in preclinical in vitro approaches towards quantitative prediction of hepatic clearance and drug-drug interactions involving organic anion …
Y Nozaki, S Izumi - Drug Metabolism and Pharmacokinetics, 2020 - Elsevier
Hepatic uptake mediated by organic anion transporting polypeptide (OATP) 1B1 and 1B3
can serve as a major elimination pathway for various anionic drugs and as a site of drug …
can serve as a major elimination pathway for various anionic drugs and as a site of drug …
Transporter‐enzyme interplay: deconvoluting effects of hepatic transporters and enzymes on drug disposition using static and dynamic mechanistic models
MV Varma, AF El‐Kattan - The Journal of Clinical …, 2016 - Wiley Online Library
A large body of evidence suggests hepatic uptake transporters, organic anion‐transporting
polypeptides (OATPs), are of high clinical relevance in determining the pharmacokinetics of …
polypeptides (OATPs), are of high clinical relevance in determining the pharmacokinetics of …
Effect of hepatic organic anion‐transporting polypeptide 1B inhibition and chronic kidney disease on the pharmacokinetics of a liver‐targeted glucokinase activator: a …
A Bergman, Y Bi, S Mathialagan… - Clinical …, 2019 - Wiley Online Library
PF‐04991532 ((S)‐6‐(3‐Cyclopentyl‐2‐(4‐(trifluoromethyl)‐1H‐imidazol‐1‐yl)
propanamido) nicotinic acid) is a glucokinase activator designed to achieve hepato …
propanamido) nicotinic acid) is a glucokinase activator designed to achieve hepato …
[PDF][PDF] Interindividual diversity in expression of organic anion uptake transporters in normal and cirrhotic human liver
T Taniguchi, A Zanetti‐Yabur, P Wang… - Hepatology …, 2020 - Wiley Online Library
The liver plays an essential role in removing endogenous and exogenous compounds from
the circulation. This function is mediated by specific transporters, including members of the …
the circulation. This function is mediated by specific transporters, including members of the …
A mechanistic pharmacokinetic model for liver transporter substrates under liver cirrhosis conditions
Liver cirrhosis is a disease characterized by the loss of functional liver mass. Physiologically
based pharmacokinetic (PBPK) modeling was applied to interpret and predict how the …
based pharmacokinetic (PBPK) modeling was applied to interpret and predict how the …
Transporter-enzyme interplay in the pharmacokinetics of PF-06835919, a first-in-class ketohexokinase inhibitor for metabolic disorders and nonalcoholic fatty liver …
Y Weng, KR Fonseca, Y Bi, S Mathialagan… - Drug Metabolism and …, 2022 - ASPET
Excess dietary fructose consumption promotes metabolic dysfunction, thereby increasing the
risk of obesity, type 2 diabetes, nonalcoholic steatohepatitis (NASH), and related …
risk of obesity, type 2 diabetes, nonalcoholic steatohepatitis (NASH), and related …
Comparison of in vitro to in vivo extrapolation approaches for predicting transporter-mediated hepatic uptake clearance using suspended rat hepatocytes
N Li, A Badrinarayanan, X Li, J Roberts… - Drug Metabolism and …, 2020 - ASPET
Clearance (CL) prediction remains a significant challenge in drug discovery, especially
when complex processes such as drug transporters are involved. The present work explores …
when complex processes such as drug transporters are involved. The present work explores …
In Vitro–In Vivo Extrapolation of OATP1B-Mediated Drug–Drug Interactions in Cynomolgus Monkey
A Ufuk, RE Kosa, H Gao, YA Bi, S Modi, D Gates… - … of Pharmacology and …, 2018 - ASPET
Hepatic organic anion-transporting polypeptides (OATP) 1B1 and 1B3 are clinically relevant
transporters associated with significant drug–drug interactions (DDIs) and safety concerns …
transporters associated with significant drug–drug interactions (DDIs) and safety concerns …