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https://www.readbyqxmd.com/read/29476044/antiretroviral-drug-metabolism-in-humanized-pxr-car-cyp3a-nog-mice
#1
JoEllyn M McMillan, Denise A Cobb, Zhiyi Lin, Mary G Banoub, Raghubendra S Dagur, Amanda A Branch Woods, Weimin Wang, Edward Makarov, Ted Kocher, Poonam S Joshi, Rolen M Quadros, Donald W Harms, Samuel M Cohen, Howard E Gendelman, Channabasavaiah B Gurumurthy, Santhi Gorantla, Larisa Y Poluektova
Antiretroviral drug (ARV) metabolism is linked largely to hepatic cytochrome P450 activity. One ARV drug class known to be metabolized by intestinal and hepatic CYP3A are the protease inhibitors (PIs). Plasma drug concentrations are boosted by CYP3A inhibitors such as cobisistat and ritonavir (RTV). Studies of such drug-drug interactions are limited since the enzyme pathways are human specific. While immune-deficient mice reconstituted with human cells are an excellent model to study ARVs during human immunodeficiency virus type 1 (HIV-1) infection, they cannot reflect human drug metabolism...
May 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27798496/how-recent-findings-on-the-pharmacokinetics-and-pharmacodynamics-of-integrase-inhibitors-can-inform-clinical-use
#2
REVIEW
Emilie Elliot, Mimie Chirwa, Marta Boffito
PURPOSE OF REVIEW: This review of recent published literature and data presented at scientific meetings on integrase stand transfer inhibitors (InSTIs) examines how these findings may impact on their future clinical use. RECENT FINDINGS: Elvitegravir (EVG), raltegravir (RAL) and dolutegravir (DTG) are InSTIs recommended as first-line options for treatment naive patients by the European AIDS Clinical Society, British HIV Association, International AIDS Society-USA and DHHS...
February 2017: Current Opinion in Infectious Diseases
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