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A combination antiretroviral therapy (cART) regimen consisting of the HIV-1 protease inhibitors atazanavir, saquinavir, and ritonavir. This specific regimen was evaluated by the Kirby Institute in the ASK-500 study (Saquinavir 500mg Formulation Study), which investigated the pharmacokinetics and long-term durability of a once-daily dosing schedule. The study specifically utilized a 500 mg tablet formulation of saquinavir to reduce pill burden compared to the standard 200 mg capsules. Atazanavir and saquinavir function by binding to the active site of the HIV-1 protease, preventing the cleavage of viral polyproteins and resulting in the production of immature, non-infectious virions. Ritonavir is included at a low dose as a pharmacokinetic enhancer; it potently inhibits the cytochrome P450 3A4 (CYP3A4) enzyme, thereby increasing the systemic exposure and half-life of the other protease inhibitors.
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