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AIDS Therapies: HIV Type 1 Protease Mutation Increases Sensitivity to Amprenavir

AIDSWEEKLY Plus; Monday, June 5, 2000
Prepared by AIDS Weekly editors from staff and other reports


NewsRx -- According to a recent study published in the Journal of Virology, the human immunodeficiency virus type 1 (HIV-1) protease inhibitor amprenavir is a good salvage therapy for patients who have had unsuccessful courses of treatment with other protease inhibitors.

It works even better in patients with HIV-1 N88S mutations, scientists say.

"Amprenavir (Agenerase, 141-W94, VX-478) is a HIV-1 protease inhibitor (PRI) recently approved for the treatment of HIV-1 infection in the United States," R. Ziermann and associates noted.

Four major protease inhibitors are presently used in antiretroviral therapy, these include saquinavir, indinavir, ritonavir, and nelfinavir. Of these four, nelfinavir and indinavir are prescribed the most often, according to the researchers. It was these two drugs that Ziermann's group investigated for viral cross-resistance with amprenavir.

"Unexpectedly, a dramatic increase in susceptibility (2.5- to 12.5-fold) was observed with 20 of 312 (6.4%) patient viruses analyzed," Ziermann et al. said.

But more interestingly, the most hypersensitivity to amprenavir was seen in patients with an HIV mutation in the N88S protease. "All viruses that carried the N88S mutation were hypersensitive to amprenavir," investigators reported ("A mutation in human immunodeficiency virus type 1 protease, N88S, that causes in vitro hypersensitivity to amprenavir," J Virol 2000 May;74(9):4414-9.

Ziermann and colleagues concluded, "The presence of the N88S mutation and associated amprenavir hypersensitivity may be useful in predicting an improved clinical response to amprenavir salvage therapy."

Search the www.NewsRx.com online database for 32 more articles about amprenevir.

The corresponding author for this study is N.T. Parkin, 270 E. Grand Avenue, South San Francisco, California 94080, USA.

Key points reported in this study are:

This article was prepared by AIDS Weekly editors from staff and other reports.

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