A comprehensive listing of bioactivation pathways of organic functional groups

AS Kalgutkar, I Gardner, RS Obach… - Current drug …, 2005 - ingentaconnect.com
The occurrence of idiosyncratic adverse drug reactions during late clinical trials or after a
drug has been released can lead to a severe restriction in its use and even in its withdrawal. …

Biotransformation reactions of five-membered aromatic heterocyclic rings

…, SC Khojasteh-Bakht, RS Obach… - Chemical research in …, 2002 - ACS Publications
Organic compounds containing five-membered aromatic heterocyclic rings are widely
distributed in nature and often play an important role in various biochemical processes. …

Managing the challenge of chemically reactive metabolites in drug development

…, S Nelson, DA Nicoll-Griffith, RS Obach… - Nature Reviews Drug …, 2011 - nature.com
The normal metabolism of drugs can generate metabolites that have intrinsic chemical reactivity
towards cellular molecules, and therefore have the potential to alter biological function …

An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

…, W Liu, SW Mason, S Noell, JJ Novak, RS Obach… - Science, 2021 - science.org
The worldwide outbreak of COVID-19 caused by severe acute respiratory syndrome
coronavirus 2 (SARS-CoV-2) has become a global pandemic. Alongside vaccines, antiviral …

Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: an examination of in vitro half-life approach and nonspecific …

RS Obach - Drug Metabolism and Disposition, 1999 - ASPET
Twenty-nine drugs of disparate structures and physicochemical properties were used in an
examination of the capability of human liver microsomal lability data (“in vitroT 1/2 ” approach…

The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data

RS Obach, JG Baxter, TE Liston, BM Silber… - … of Pharmacology and …, 1997 - ASPET
We describe a comprehensive retrospective analysis in which the abilities of several
methods by which human pharmacokinetic parameters are predicted from preclinical …

Impact of different dietary lipid sources on growth, lipid digestibility, tissue fatty acid composition and histology of rainbow trout, Oncorhynchus mykiss

MJ Caballero, A Obach, G Rosenlund, D Montero… - Aquaculture, 2002 - Elsevier
The aim of the present study was to determine the impact of replacing at least 50% of the
fish oil by alternative lipid sources in diets for rainbow trout on growth, lipid digestibility, fatty …

The conduct of in vitro and in vivo drug-drug interaction studies: a Pharmaceutical Research and Manufacturers of America (PhRMA) perspective

…, G Miwa, L Ni, G Kumar, J McLeod, RS Obach… - Drug metabolism and …, 2003 - ASPET
Current regulatory guidances do not address specific study designs for in vitro and in vivo
drug-drug interaction studies. There is a common desire by regulatory authorities and by …

Validated assays for human cytochrome P450 activities

RL Walsky, RS Obach - Drug metabolism and disposition, 2004 - ASPET
The measurement of the effect of new chemical entities on human cytochrome P450 marker
activities using in vitro experimentation represents an important experimental approach in …

Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19

…, SW Mason, ME McGrath, S Noell, RS Obach… - Nature …, 2021 - nature.com
COVID-19 caused by the SARS-CoV-2 virus has become a global pandemic. 3CL protease
is a virally encoded protein that is essential across a broad spectrum of coronaviruses with …