Prevalence of non–cytochrome P450–mediated metabolism in Food and Drug Administration–approved oral and intravenous drugs: 2006–2015

MA Cerny - Drug Metabolism and Disposition, 2016 - ASPET
In recent years, claims of increased involvement of non–cytochrome P450 (non-P450)
enzymes in the metabolism of drugs have appeared in the literature. However, no temporal …

Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization

JK Yano, TT Denton, MA Cerny, X Zhang… - Journal of medicinal …, 2006 - ACS Publications
A series of 3-heteroaromatic analogues of nicotine were synthesized to delineate structural
and mechanistic requirements for selectively inhibiting human cytochrome P450 (CYP) 2A6. …

Identification of glycochenodeoxycholate 3‐O‐glucuronide and glycodeoxycholate 3‐O‐glucuronide as highly sensitive and specific OATP1B1 biomarkers

…, S Mathialagan, M Varma, MA Cerny… - Clinical …, 2021 - Wiley Online Library
The aim of this study was to investigate the sensitivity and specificity of endogenous
glycochenodeoxycholate and glycodeoxycholate 3‐O‐glucuronides (GCDCA‐3G and GDCA‐3G) …

Human absorption, distribution, metabolism, and excretion studies: origins, innovations, and importance

MA Cerny, DK Spracklin, RS Obach - Drug Metabolism and Disposition, 2023 - ASPET
Human absorption, distribution, metabolism, and excretion (hADME) studies represent one
of the most important clinical studies in terms of obtaining a comprehensive and quantitative …

G protein–coupled bile acid receptor 1 stimulation mediates arterial vasodilation through a KCa1. 1 (BKCa)–dependent mechanism

…, J Lord, S Sanyal, H Yu, C Harcken, MA Cerny… - … of Pharmacology and …, 2014 - ASPET
Bile acids (BAs) and BA receptors, including G protein–coupled bile acid receptor 1 (GPBAR1),
represent novel targets for the treatment of metabolic and inflammatory disorders. …

Static and dynamic projections of drug-drug interactions caused by cytochrome P450 3A time-dependent inhibitors measured in human liver microsomes and …

E Tseng, H Eng, J Lin, MA Cerny, DA Tess… - Drug Metabolism and …, 2021 - ASPET
Cytochrome P450 3A (CYP3A) is a frequent target for time-dependent inhibition (TDI) that can
give rise to drug-drug interactions (DDI). Yet many drugs that exhibit in vitro TDI for CYP3A …

Effective application of metabolite profiling in drug design and discovery

MA Cerny, AS Kalgutkar, RS Obach… - Journal of Medicinal …, 2020 - ACS Publications
At one time, biotransformation was a descriptive activity in pharmaceutical development,
viewed simply as structural elucidation of drug metabolites, completed only once compounds …

Leveraging of rifampicin-dosed cynomolgus monkeys to identify bile acid 3-O-sulfate conjugates as potential novel biomarkers for organic anion-transporting …

…, H Gao, RE Kosa, YA Bi, MVS Varma, MA Cerny… - Drug Metabolism and …, 2017 - ASPET
In the search for novel bile acid (BA) biomarkers of liver organic anion-transporting polypeptides
(OATPs), cynomolgus monkeys received oral rifampicin (RIF) at four dose levels (1, 3, …

Cytochrome P450 3A time-dependent inhibition assays are too sensitive for identification of drugs causing clinically significant drug-drug interactions: a comparison of …

H Eng, E Tseng, MA Cerny, TC Goosen… - Drug Metabolism and …, 2021 - ASPET
Time-dependent inhibition (TDI) of CYP3A is an important mechanism underlying numerous
drug-drug interactions (DDIs), and assays to measure this are done to support early drug …

Cytochrome P450-Catalyzed Oxidation of N-Benzyl-N-cyclopropylamine Generates Both Cyclopropanone Hydrate and 3-Hydroxypropionaldehyde via Hydrogen …

MA Cerny, RP Hanzlik - Journal of the American Chemical Society, 2006 - ACS Publications
The suicide substrate activity of N-benzyl-N-cyclopropylamine (1) and N-benzyl-N-(1‘-methylcyclopropyl)amine
(2) toward cytochrome P450 and other enzymes has been explained by …