Atazanavir (DB01072): A Comprehensive Pharmacological and Clinical Monograph

Introduction: Atazanavir in the HIV Treatment Armamentarium

Atazanavir is an azapeptide antiretroviral agent belonging to the protease inhibitor (PI) class, developed by Bristol-Myers Squibb and licensed from Novartis.[1] It is indicated for the treatment of Human Immunodeficiency Virus Type 1 (HIV-1) infection, always as a component of combination antiretroviral therapy (cART) with other agents.[2]

Upon its initial approval by the U.S. Food and Drug Administration (FDA) in 2003, Atazanavir represented a significant advancement in the PI class.[2] It was distinguished from its predecessors by two clinically important features that addressed major challenges in long-term HIV management. First, its pharmacokinetic profile permitted a once-daily dosing schedule, a marked improvement over the multiple daily doses required for older PIs, which enhanced patient convenience and was expected to improve treatment adherence.[2] Second, and perhaps more importantly, it demonstrated a more favorable metabolic profile, particularly its lesser impact on serum lipids, including total cholesterol and triglycerides.[2] This characteristic made it a particularly attractive option for patients with, or at high risk for, cardiovascular disease and other metabolic complications, which were becoming increasingly prevalent as people with HIV lived longer.[7]