Pharmacological and clinical evidence of nevirapine immediate- and extended-release formulations

Abstract

We reviewed the current information available on nevirapine immediate- and extended-release formulations and its role in single-dose and combination antiretroviral therapy. Nevirapine was approved in 1996 and was the first non-nucleoside reverse-transcriptase inhibitor available for the treatment of HIV-1 infection. Nevirapine has demonstrated good efficacy and a well-characterized safety profile. A major drawback is the low genetic barrier, allowing the emergence of resistance in the presence of single mutations in the reverse-transcriptase gene. This shortcoming is particularly relevant when nevirapine is administered in a single dose to prevent mother-to-child transmission of HIV-1 infection, compromising the efficacy of future non-nucleoside reverse transcriptase–inhibitor regimens. Studies published recently have probed the noninferiority of nevirapine compared to ritonavir-boosted atazanavir with both tenofovir disoproxil fumarate and emtricitabine in antiretroviral treatment–naïve patients. In 2011, a new formulation of nevirapine (nevirapine extended release) that allowed once-daily dosing was approved by the Food and Drug Administration and by the European Medicines Agency. VERxVe, a study comparing nevirapine extended release with nevirapine immediate release in antiretroviral treatment–naïve patients, and TRANxITION, a study carried out in antiretroviral treatment–experienced patients who switched therapy from nevirapine immediate release to nevirapine extended release, provided data on the noninferiority of the new formulation of nevirapine compared with nevirapine immediate release in terms of efficacy and safety. Nevirapine extended release will further increase the durability and persistence of nevirapine-containing antiretroviral therapy, allowing once-daily dosing regimens.

Keywords:

• nevirapine extended release
• efficacy
• safety
• resistance
• clinical practice

Disclosure

Javier Ena received honoraria from Bristol-Myers Squibb, Gilead, Abbott, and Boehringer Ingelheim as clinical advisor in 2011–2012. Concepción Amador received honoraria from Abbott, Boehringer Ingelheim, Bristol-Myers Squibb, Gilead, Janssen-Cilag, and MSD as clinical advisor in 2011–2012. Conxa Benito received honoraria from Bristol-Myers Squibb, Gilead, Janssen-Cilag, and Boehringer Ingelheim as clinical advisor in 2011–2012. Francisco Pasquau received honoraria from Abbott, Boehringer Ingelheim, Bristol-Myers Squibb, Gilead, Janssen-Cilag, and MSD as clinical advisor in 2011–2012. Boehringer-Ingelheim had no role in the preparation, review, or approval of the manuscript.