Nevirapine (DB00238): A Comprehensive Monograph on its Pharmacology, Clinical Efficacy, and Safety Profile

1.0 Executive Summary

Nevirapine is a first-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) and was the first agent in its class to receive regulatory approval for the treatment of Human Immunodeficiency Virus Type 1 (HIV-1) infection.[1] It functions as a potent, allosteric inhibitor of the HIV-1 reverse transcriptase enzyme, a critical component of the viral replication cycle.[2] Nevirapine is indicated for use exclusively in combination with other antiretroviral (ARV) agents for the management of HIV-1 in adults and children and has also played a significant role in strategies for the prevention of mother-to-child transmission (PMTCT) of the virus.[2]

The clinical utility of Nevirapine is defined by a distinct and challenging safety profile. The drug carries a U.S. Food and Drug Administration (FDA) Boxed Warning for severe, life-threatening, and sometimes fatal hepatotoxicity and severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN).[5] The risk of hepatotoxicity is paradoxically elevated in treatment-naïve patients with more robust immune systems. Consequently, initiation of Nevirapine is not recommended in adult females with CD4+ T-cell counts greater than 250 cells/mm³ or in adult males with CD4+ T-cell counts greater than 400 cells/mm³, unless the potential benefit is determined to unequivocally outweigh the substantial risk.[2]