Open AccessNon‐nucleoside reverse transcriptase inhibitors: a review on pharmacokinetics, pharmacodynamics, safety and tolerability
Author(s) -
Usach Iris,
Melis Virginia,
Peris JoséEsteban
Publication year - 2013
Publication title -
journal of the international aids society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.724
H-Index - 62
ISSN - 1758-2652
DOI - 10.7448/ias.16.1.18567
Subject(s) - etravirine , efavirenz , rilpivirine , medicine , nevirapine , pharmacology , tolerability , pharmacokinetics , pharmacodynamics , virology , nucleoside reverse transcriptase inhibitor , reverse transcriptase , human immunodeficiency virus (hiv) , adverse effect , antiretroviral therapy , viral load , biology , rna , biochemistry , gene
Introduction Human immunodeficiency virus (HIV) type‐1 non‐nucleoside and nucleoside reverse transcriptase inhibitors (NNRTIs) are key drugs of highly active antiretroviral therapy (HAART) in the clinical management of acquired immune deficiency syndrome (AIDS)/HIV infection. Discussion First‐generation NNRTIs, nevirapine (NVP), delavirdine (DLV) and efavirenz (EFV) are drugs with a low genetic barrier and poor resistance profile, which has led to the development of new generations of NNRTIs. Second‐generation NNRTIs, etravirine (ETR) and rilpivirine (RPV) have been approved by the Food and Drug Administration and European Union, and the next generation of drugs is currently being clinically developed. This review describes recent clinical data, pharmacokinetics, metabolism, pharmacodynamics, safety and tolerability of commercialized NNRTIs, including the effects of sex, race and age differences on pharmacokinetics and safety. Moreover, it summarizes the characteristics of next‐generation NNRTIs: lersivirine, GSK 2248761, RDEA806, BILR 355 BS, calanolide A, MK‐4965, MK‐1439 and MK‐6186. Conclusions This review presents a wide description of NNRTIs, providing useful information for researchers interested in this field, both in clinical use and in research.