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-Reference-Cited by-同舟云学术

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

Published:2022-04-19 Issue:4 Volume:66 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Moore Katy¹^ORCID,Thakkar Nilay²^ORCID,Magee Mindy²,Sevinsky Heather³,Vakkalagadda Blisse³,Lubin Susan³,Llamoso Cyril⁴,Ackerman Peter⁴

Affiliation:

1. ViiV Healthcare, Research Triangle Park, North Carolina, USA

2. GlaxoSmithKline, Upper Providence, Pennsylvania, USA

3. Bristol-Myers Squibb, Hopewell, New Jersey, USA

4. ViiV Healthcare, Branford, Connecticut, USA

Abstract

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.

Funder

ViiV Healthcare

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/aac.02251-21

Reference23 articles.

1. Triple-Class Virologic Failure in HIV-Infected Patients Undergoing Antiretroviral Therapy for Up to 10 Years

2. Calendar Time Trends in the Incidence and Prevalence of Triple-Class Virologic Failure in Antiretroviral Drug-Experienced People With HIV in Europe

3. Efficacy of Initial Antiretroviral Therapy for HIV-1 Infection in Adults: A Systematic Review and Meta-Analysis of 114 Studies with up to 144 Weeks' Follow-Up

4. Homology models of the HIV-1 attachment inhibitor BMS-626529 bound to gp120 suggest a unique mechanism of action

5. Compartmental Absorption Modeling and Site of Absorption Studies to Determine Feasibility of an Extended-Release Formulation of an HIV-1 Attachment Inhibitor Phosphate Ester Prodrug

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