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Updated: Oct 11, 2025

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A High-throughput Cre-Lox Activated Viral Membrane Fusion Assay to Identify Inhibitors of HIV-1 Viral Membrane Fusion
Published on: August 14, 2018
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Fostemsavir: a first-in-class HIV-1 attachment inhibitor
Philip M Grant1, Michael J Kozal
1Stanford University 300 Pasteur Drive, Stanford, California, USA.
Current Opinion in HIV and AIDS
|December 6, 2021
Summary
Fostemsavir, a new HIV-1 attachment inhibitor, is effective and well-tolerated for multidrug-resistant HIV-1. It helps heavily treatment-experienced patients achieve virologic suppression with optimal background therapy.
Area of Science:
- Virology
- Pharmacology
- Immunology
Background:
- Human Immunodeficiency Virus type 1 (HIV-1) infection remains a global health challenge.
- Multidrug-resistant HIV-1 strains necessitate novel therapeutic strategies.
- Antiretroviral therapy has significantly improved outcomes but faces challenges with resistance.
Purpose of the Study:
- To review the pharmacology, efficacy, tolerability, and resistance profile of fostemsavir.
- To evaluate fostemsavir's role in treating multidrug-resistant HIV-1.
- To discuss the implications of fostemsavir's approval for patient care.
Main Methods:
- Review of published literature on fostemsavir.
- Analysis of clinical trial data regarding fostemsavir's efficacy and safety.
- Examination of in vitro studies on fostemsavir's mechanism of action and resistance.
Main Results:
- Fostemsavir is an HIV-1 attachment inhibitor targeting gp120, preventing viral entry.
- It is well-tolerated and maintains virologic activity in patients with multidrug-resistant HIV-1.
- A majority of heavily treatment-experienced participants achieved virologic suppression with fostemsavir and optimal background therapy.
Conclusions:
- Fostemsavir's approval is a significant advancement for multidrug-resistant HIV-1 treatment.
- Its novel mechanism offers an option with no cross-resistance to existing antiretrovirals.
- Further research is needed to define the role of resistance testing and fostemsavir's use beyond salvage therapy.
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