Universität zu Köln

Platten, Martin and Faetkenheuer, Gerd (2013). Lersivirine - a new drug for HIV infection therapy. Expert Opin. Investig. Drugs, 22 (12). S. 1687 - 1695. ABINGDON: TAYLOR & FRANCIS LTD. ISSN 1744-7658

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Abstract

Introduction: Lersivirine (UK-453,061) is a novel second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). It binds reverse transcriptase in a distinct way leading to a unique resistance profile. The development of lersivirine was recently stopped in Phase IIb clinical development. Areas covered: This article describes the background of lersivirine, its pharmacodynamic and pharmacokinetic profile and its clinical efficacy in HIV-infected patients. Moreover, the authors review its resistance profile in addition to its possible interactions with coadministered drugs and safety and tolerability. The authors' evaluation is based on the articles retrieved from a Medline in addition to abstracts from major HIV conferences and workshops addressing lersivirine. Expert opinion: The authors believe that lersivirine has therapeutic potential for HIV-infected individuals with viral strains resistant against first-line NNRTIs. However, no large, well-powered studies have been conducted so far, which assess noninferiority against established antiretroviral agents. In February 2013, the developing company behind lersivirine halted further development as it was decided that it would not provide an improvement over existing therapies; perhaps this is an opportunity missed.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Platten, Martin UNSPECIFIED UNSPECIFIED UNSPECIFIED Faetkenheuer, Gerd UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-471080
DOI:	10.1517/13543784.2013.846325
Journal or Publication Title:	Expert Opin. Investig. Drugs
Volume:	22
Number:	12
Page Range:	S. 1687 - 1695
Date:	2013
Publisher:	TAYLOR & FRANCIS LTD
Place of Publication:	ABINGDON
ISSN:	1744-7658
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language REVERSE-TRANSCRIPTASE INHIBITOR; DEVELOPMENTAL TOXICITY; PHARMACOKINETICS; UK-453,061; SAFETY; NNRTI; RESISTANCE; ACID Multiple languages Pharmacology & Pharmacy Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/47108