Delavirdine (DB00705): A Comprehensive Pharmacological and Clinical Monograph of a Second-Generation NNRTI

Introduction: Delavirdine in the Context of Antiretroviral Therapy

Delavirdine, marketed under the brand name Rescriptor, is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that was approved by the U.S. Food and Drug Administration (FDA) in 1997 for the treatment of Human Immunodeficiency Virus Type 1 (HIV-1) infection.[1] As a component of the early Highly Active Antiretroviral Therapy (HAART) regimens, it represented a significant advancement by offering a mechanism of action distinct from the foundational nucleoside reverse transcriptase inhibitors (NRTIs). However, the clinical history of Delavirdine is defined by a central paradox: its unique pharmacological profile as a potent inhibitor of the cytochrome P450 (CYP) metabolic enzyme system created both therapeutic opportunities and profound clinical challenges. This dual nature as both an antiviral agent and a significant metabolic modulator ultimately dictated its limited clinical utility and eventual obsolescence in the face of more effective, tolerable, and pharmacologically simpler agents.[1]