Bevirimat

Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies^[1][2][3][4]. In Vitro:Bevirimat inhibits wild-type HIV-1 replication with a mean IC₅₀ of 10.3 nM^[2].
Bevirimat (72 h) shows antiviral activity against wild type HIV1 and HIV1 harboring capsid I201V mutant protein infected in human HeLa cells, with a EC₅₀ of 0.009 and 0.29 μM^[3].
Bevirimat (48 h) shows cytotoxicity against mock-infected human MT2 cells, with a CC₅₀ of > 10 μM^[4].
Bevirimat (1 day) shows antiviral activity against HIVIIIB infected in human MT2 cells assessed as inhibition of viral replication, with a EC₅₀ of 0.0013 μM^[5].
Bevirimat (48 h) shows cytotoxicity against human MT4 cells assessed as reduction in cell viability by CytoTox-Glo cytotoxicity assay, with a CC₅₀ of > 2 μM^[6].
Bevirimat (4 days) shows antiviral activity against HIV1_NL4-3 infected in human MT4 cells assessed as p24 antigen level, with a IC₅₀ of 0.087 μM^[7].
Bevirimat (3 days) shows cytotoxicity against HIV-1-infected C8166 cells, with a mean CC₅₀ of 53.23 μM^[9].
Bevirimat (0-8 μM, 3 days) has a weak inhibitory effect on the replication of HIV-1IIIB in C8166 cells in the presence of 20% human serum^[9].
In Vivo:Bevirimat (10-100 mg/kg, p.o., twice-daily, 22 days) potently inhibits HIV-1 replication and prevents thymocyte depletion in SCID-hu Thy/Liv mice^[8].