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Benjamin E. Gewurz, Mark Jacobs, Jo Ann Proper, Thomas A. Dahl, Tamio Fujiwara, Bruce J. Dezube, Capravirine, a Nonnucleoside Reverse-Transcriptase Inhibitor in Patients Infected with HIV-1: A Phase 1 Study, The Journal of Infectious Diseases, Volume 190, Issue 11, 1 December 2004, Pages 1957–1961, https://doi.org/10.1086/425581
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Abstract
Capravirine is a nonnucleoside reverse-transcriptase inhibitor (NNRTI) with a unique resistance profile. Although single mutations allow resistance to establishedNNRTIs, human immunodeficiency virus (HIV)-1 must undergo multiple mutations to achieve resistance to capravirine. In the present phase 1 study, capravirine was administered orally for up to 28 days to 55 HIV-1-infected individuals with CD4+ T lymphocyte counts of 50–500 cells/εL. The most frequent adverse events were diarrhea (5%) and nausea (4%), with no drugrelated rashes observed. The day 15 median (mean) HIV-1 load decreased by 1.34 (1.45) log10 copies/mL in the patients receiving 25 mg/kg/day. Capravirine demonstrated potent antiviral activity, even in antiretroviral-experienced patients.