Pharmacokinetics 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 | Zendy

Katy Moore | Zendy; Nilay Thakkar | Zendy; Mindy Magee | Zendy; Heather Sevinsky | Zendy; Blisse Vakkalagadda | Zendy; Susan Lubin | Zendy; Cyril Llamoso | Zendy; Peter Ackerman | Zendy

Open Access

Pharmacokinetics 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 , chemistry , maraviroc , medicine , 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.

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