Open AccessPharmacokinetics of Temsavir, the Active Moiety of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir, Coadministered with Cobicistat, Etravirine, Darunavir/Cobicistat, or Darunavir/Ritonavir with or without Etravirine in Healthy Participants
Author(s) -
Katy Moore,
Nilay Thakkar,
Mindy Magee,
Heather Sevinsky,
Blisse Vakkalagadda,
Susan Lubin,
Cyril Llamoso,
Peter Ackerman
Publication year - 2022
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.02251-21
Subject(s) - etravirine , darunavir , cobicistat , cmax , ritonavir , pharmacology , cmin , pharmacokinetics , maraviroc , medicine , chemistry , viral load , virology , human immunodeficiency virus (hiv) , antiretroviral therapy
Fostemsavir is a prodrug of temsavir, a first-in-class attachment inhibitor that binds directly to HIV-1 gp120, preventing initial viral attachment and entry into host CD4+ T cells with demonstrated efficacy in phase 2 and 3. Temsavir is a P-glycoprotein and breast cancer resistance protein (BCRP) substrate; its metabolism is mediated by esterase and CYP3A4 enzymes.