Lersivirine - a new drug for HIV infection therapy.

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.
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.
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.
AuthorsMartin Platten, Gerd Fätkenheuer
JournalExpert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 22 Issue 12 Pg. 1687-94 (Dec 2013) ISSN: 1744-7658 [Electronic] England
PMID24128277 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References
  • Anti-HIV Agents
  • Nitriles
  • Pyrazoles
  • Reverse Transcriptase Inhibitors
  • UK 453,061
  • Animals
  • Anti-HIV Agents (pharmacology, therapeutic use)
  • Drug Resistance, Viral
  • HIV Infections (drug therapy)
  • Humans
  • Nitriles (pharmacology, therapeutic use)
  • Pyrazoles (pharmacology, therapeutic use)
  • Reverse Transcriptase Inhibitors (pharmacology, therapeutic use)

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