Drug Metabolism and Disposition current issue

Hepatic stellate cells (HSCs) are the major site of vitamin A (retinol) esterification and subsequent storage as retinyl esters within lipid droplets. However, retinyl esters become depleted in m...

http://dmd.aspetjournals.org/cgi/content/short/52/5/442?rss=1

Bupropion is used for treating depression, obesity, and seasonal affective disorder, and for smoking cessation. Bupropion is commonly prescribed, but has complex pharmacokinetics and interindivid...

http://dmd.aspetjournals.org/cgi/content/short/52/5/455?rss=1

In vitro time-dependent inhibition (TDI) kinetic parameters for cytochrome P450 (P450) 1A2, 2B6, 2C8, 2C9, 2C19, and 2D6 were determined in pooled human liver microsomes for 19 drugs (and two met...

http://dmd.aspetjournals.org/cgi/content/short/52/5/422?rss=1

Drug-induced liver injury (DILI) is a frequent cause of clinical trial failures during drug development. While inhibiting bile salt export pump (BSEP) is a well-documented DILI mechanism, interfe...

http://dmd.aspetjournals.org/cgi/content/short/52/5/432?rss=1

Organic anion transporting polypeptide (OATP1B) plays a key role in the hepatic clearance of a majority of high molecular weight (MW) acids and zwitterions. Here, we evaluated the role of OATP1B-...

http://dmd.aspetjournals.org/cgi/content/short/52/5/399?rss=1

Metastasis is the most common pathway of cancer death. The lack of effective predictors of breast cancer metastasis is a pressing issue in clinical practice. Therefore, exploring the mechanism of...

http://dmd.aspetjournals.org/cgi/content/short/52/5/408?rss=1

The determination of metabolic stability is critical for drug discovery programs, allowing for the optimization of chemical entities and compound prioritization. As such, it is common to perform ...

http://dmd.aspetjournals.org/cgi/content/short/52/5/377?rss=1

In vitro–in vivo extrapolation (IVIVE) allows prediction of clinical outcomes across populations from in vitro data using specific scalars tailored to the biologic characteristics of each popul...

http://dmd.aspetjournals.org/cgi/content/short/52/5/390?rss=1

Camonsertib is a novel ATR kinase inhibitor in clinical development for advanced cancers targeting sensitizing mutations. This article describes the identification and biosynthesis of an N-glucur...

http://dmd.aspetjournals.org/cgi/content/short/52/5/368?rss=1

Organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 (collectively, OATP1B) transporters encoded by the solute carrier organic anion transporter (SLCO) genes mediate uptake of multiple p...

http://dmd.aspetjournals.org/cgi/content/short/52/5/355?rss=1

It is common practice in drug discovery and development to predict in vivo hepatic clearance from in vitro incubations with liver microsomes or hepatocytes using the well-stirred model (WSM). Whe...

http://dmd.aspetjournals.org/cgi/content/short/52/5/345?rss=1

Fluorination of organic compounds plays an important role in the chemical and pharmaceutical industry and is often applied to improve physicochemical parameters or modify pharmacological properti...

http://dmd.aspetjournals.org/cgi/content/short/52/5/337?rss=1

BIIB104 (formerly PF-04958242), N-((3S,4S)-4-(4-(5-cyanothiophen-2-yl)phenoxy)tetrahydrofuran-3-yl)propane-2-sulfonamide, is an α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor pote...

http://dmd.aspetjournals.org/cgi/content/short/52/5/323?rss=1