lersivirine

Lersivirine is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that was under development for the treatment of HIV-1 infection. Developed by Pfizer and later managed by ViiV Healthcare, it belongs to the pyrazole class of NNRTIs. Its mechanism of action involves binding to a specific allosteric pocket on the HIV-1 reverse transcriptase enzyme, distinct from the active site, which induces a conformational change that inhibits the enzyme's polymerase activity. Lersivirine was designed to offer an improved resistance profile against common NNRTI-resistant mutations (such as K103N and Y181C) and a better safety profile compared to first-generation NNRTIs like efavirenz. However, in 2013, ViiV Healthcare announced the discontinuation of its development following Phase II clinical trials, as it did not demonstrate a sufficient competitive advantage over existing therapies.

Other names

lersivirine