Atazanavir (ATV) - Once-Daily HIV Protease Inhibitor

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Atazanavir Powder Usage and Synthesis.

Azanavir is an inhibitor of azeptide HIV-1 protease. The product selectively inhibits the specific processing of viral Gag and GAG-pol polymers in HIV-1-infected cells, thereby blocking the formation of mature viruses. In vitro antiviral activity: The mean 50% inhibitory concentration (IC50) of azanavir against a large number of laboratory and clinical isolates of HIV-1 virus isolated from peripheral blood mononuclear cells, macrophages, CIM-SS cells, and MT2 cells without human serum was 2-5 nm.

Pharmacological action of Atazanavir.

Azanavir is a novel azopeptidase protease inhibitor (PI), whose activity in vitro is comparable to that of non-peptide PIs such as Nelfinavir. Azanavir is designed based on X-ray diffraction studies of enzym-azopeptidase complexes and has a C-2 symmetric chemical structure. It is a highly selective and efficient inhibitor of HIV-1 protease, which inhibits the production of viral structural proteins, reverse transcriptase, integrase and protease by blocking the cleavage of viral gap and GAP-POL precursor polymerase, so that HIV-1-infected cells release non-infectious immature viral particles. This product has stronger inhibitory activity against multiple strains of HIV-1 virus than other PIs, and the median effective concentration (EC50) in vitro medium is 2.6 ~ 5.3nmol/L, and the 90% effective concentration (EC90) is 9 ~ 15nmol/L.

In vitro study of Atazanavir.

Atazanavir has effective activity against wild-type viruses in vitro with EC50 and EC90 of 2-5 nM and 9-15 nM, respectively. Atazanavir can effectively induce endoplasmic reticulum stress response in glioma cells, and the levels of GRP78 and CHOP are increased, and caspase-4 is activated, leading to cell death.

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