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Preclinical Profile of the HIV-1 Maturation Inhibitor VH3739937
Brian McAuliffe1, Paul Falk1, Jie Chen2
1ViiV Healthcare, 36 East Industrial Road, Branford, CT 06405, USA.
Viruses
|October 26, 2024
Summary
The novel HIV-1 maturation inhibitor VH3739937 (VH-937) shows potent antiviral activity against diverse HIV-1 strains. Its efficacy and resistance profile support its potential as a once-weekly oral HIV-1 treatment.
Area of Science:
- Virology
- Drug Discovery
- Antiviral Research
Background:
- HIV-1 maturation inhibitors (MIs) are crucial for antiretroviral therapy.
- VH3739937 (VH-937) is a novel MI targeting capsid-spacer peptide 1 cleavage.
- VH-937 demonstrates an oral half-life suitable for once-weekly dosing.
Purpose of the Study:
- To characterize the antiviral properties of VH-937 against HIV-1.
- To evaluate VH-937's activity against various HIV-1 strains and resistant variants.
- To assess the resistance development potential of VH-937.
Main Methods:
- Antiviral activity assessed using multiple-cycle and single-cycle assays.
- Half-maximal effective concentration (EC50) and maximal percent inhibition (MPI) determined.
- Resistance selection cultures and VLP dissociation rate measurements employed.
Main Results:
- VH-937 exhibited potent antiviral activity (EC50 ≤ 5.0 nM) against all tested HIV-1 strains.
- Effective inhibition of viruses with reduced susceptibility to other MIs (EC50 ≤ 8.0 nM, MPI ≥ 92%).
- Emergence of resistance mutations observed in single-cycle assays, with re-engineered viruses showing reduced function.
Conclusions:
- VH-937 demonstrates broad-spectrum antiviral activity against HIV-1 in vitro.
- The drug shows promise against strains less susceptible to existing MIs.
- Further development of VH-937 as an HIV-1 treatment is warranted based on its in vitro profile.
