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Efavirenz
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Alan C. Street, Irani Thevarajan
Etravirine is a nonnucleoside agent that was first used in combination with antiretrovirals in patients who had failed initial and subsequent treatment regimens. It has limited cross-resistance with efavirenz and nevirapine (see Chapter 238, Etravirine).
Switching strategies in the recent era of antiretroviral therapy
Published in Expert Review of Clinical Pharmacology, 2019
Paula Prieto, Daniel Podzamczer
First-generation nonnucleosides such as efavirenz (EFV) and nevirapine (NEV) as well as the second-generation rilpivirine (RPV) have a low genetic barrier, and VF due to poor adherence is associated with the selection of resistant mutations in a high proportion of patients. Etravirine has a higher genetic barrier, but is given in two pills per day which are not easy to swallow, making it a poor candidate for simplification. In contrast, the recently approved drug known as doravirine (DOR) is prescribed as one pill per day, may be given in a triple fixed-dose regimen combined with tenofovir disoproxil fumarate (TDF) and lamivudine (3TC) or alone to be associated with other backbones. Recent studies have shown DOR to be effective and well tolerated in ARV-naïve patients, and the drug is currently being investigated in treatment-experienced patients and in those with transmitted resistance to nonnucleoside reverse transcriptase inhibitor (NNRTI) drugs.
Emerging therapies in Friedreich’s Ataxia
Published in Expert Review of Neurotherapeutics, 2020
Theresa A. Zesiewicz, Joshua Hancock, Shaila D. Ghanekar, Sheng-Han Kuo, Carlos A. Dohse, Joshua Vega
Etravirine is an antiviral drug that is used to treat human immunodeficiency virus (HIV). It was identified as a potential therapy for FRDA as part of a drug repositioning endeavor to identify available drugs that could increase frataxin. Subsequent early research found that etravirine increased frataxin levels in FRDA patient-derived cells; specifically, etravirine was found to establish frataxin at levels comparable to unaffected carrier cells [85]. It is hypothesized that etravirine functions to increase frataxin levels by increasing the translation rate of frataxin mRNA or preventing frataxin degradation. Further testing of the effect of etravirine in FRDA is needed to determine its true therapeutic potential [85].
Emerging drugs for the treatment of HIV/AIDS: a review of 2019/2020 phase II and III trials
Published in Expert Opinion on Emerging Drugs, 2021
Marco Piscaglia, Maria Vittoria Cossu, Matteo Passerini, Francesco Petri, Martina Gerbi, Chiara Fusetti, Amedeo Capetti, Giuliano Rizzardini
The most widely used NNRTIs are rilpivirine (RPV), doravirine (DOR), efavirenz (EFV), and nevirapine (NEV), respectively. Etravirine is mainly used in patients with drug-resistant HIV-1. They are often combined with two NRTIs, although rilpivirine may be associated with DTG in a fixed-dose combination indicated for simplification in virologically suppressed patients or for first-line therapy in naive patients with specific characteristics. Second-generation NNRTIs (RPV and DOR) have higher genetic barrier and better tolerability than EFV and NEV which are gradually being replaced due to relevant neuropsychiatric side effects and allergies, and to their low genetic barrier [27,28].