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 …

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 …

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…

Mechanism-based inactivation of human cytochrome p450 enzymes and the prediction of drug-drug interactions

RS Obach, RL Walsky, K Venkatakrishnan - Drug metabolism and …, 2007 - ASPET
The ability to use vitro inactivation kinetic parameters in scaling to in vivo drug-drug interactions
(DDIs) for mechanism-based inactivators of human cytochrome P450 (P450) enzymes …

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 …

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 …

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. …

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

…, S Noell, RS Obach, MN O'Brien, R O'Connor… - 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 …

Inhibition of human cytochrome P450 enzymes by constituents of St. John's Wort, an herbal preparation used in the treatment of depression

RS Obach - Journal of Pharmacology and Experimental …, 2000 - ASPET
Commercially available St. John's wort (Hypericum perforatum) extracts, preparations that
are used in the treatment of depression, were examined for the potential to inhibit human …

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. …