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- Title
Clinical Pharmacokinetics and Pharmacodynamics of Etravirine: An Updated Review.
- Authors
Havens, Joshua P.; Podany, Anthony T.; Scarsi, Kimberly K.; Fletcher, Courtney V.
- Abstract
Etravirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of human immunodeficiency virus type 1 infection. It is a potent inhibitor of HIV reverse transcriptase and retains activity against wild-type and most NNRTI-resistant HIV. The pharmacokinetic profile of etravirine and clinical data support twice-daily dosing, although once-daily dosing has been investigated in treatment-naïve and treatment-experienced persons. Despite similar pharmacokinetic and pharmacodynamic results compared with twice-daily dosing, larger studies are needed to fully support once-daily etravirine dosing in treatment-naïve individuals. Etravirine is reserved for use in third- or fourth-line antiretroviral treatment regimens, as recommended, for example, in treatment guidelines by the US Department of Health and Human Services-Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents Living with HIV. Etravirine exhibits the potential for bi-directional drug-drug interactions with other antiretrovirals and concomitant medications through its interactions with cytochrome P450 (CYP) isozymes: CYP3A4, CYP2C9, and CYP2C19. This review summarizes the pharmacokinetic and pharmacodynamic parameters of etravirine, with particular attention to information on drug-drug interactions and use in special patient populations, including children/adolescents, women, persons with organ dysfunction, and during pregnancy.
- Subjects
NON-nucleoside reverse transcriptase inhibitors; REVERSE transcriptase inhibitors; INSULIN aspart; PHARMACOKINETICS; ANTIRETROVIRAL agents; PHARMACODYNAMICS; REVERSE transcriptase; HIV infections; PHARMACOGENOMICS; HETEROCYCLIC compounds; BIOAVAILABILITY; ORGANIC compounds; MULTIPLE organ failure; DRUG interactions; RESEARCH funding; OXIDOREDUCTASES; HIV; HEMOPROTEINS
- Publication
Clinical Pharmacokinetics, 2020, Vol 59, Issue 2, p137
- ISSN
0312-5963
- Publication type
journal article
- DOI
10.1007/s40262-019-00830-9