Capravirine, a nonnucleoside reverse-transcriptase inhibitor in patients infected with HIV-1: a phase 1 study.
Capravirine is a nonnucleoside reverse-transcriptase inhibitor (NNRTI) with a unique resistance profile. Although single mutations allow resistance to established NNRTIs, 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/microL. The most frequent adverse events were diarrhea (5%) and nausea (4%), with no drug-related rashes observed. The day 15 median (mean) HIV-1 load decreased by 1.34 (1.45) log(10) copies/mL in the patients receiving 25 mg/kg/day. Capravirine demonstrated potent antiviral activity, even in antiretroviral-experienced patients.
Gewurz
Benjamin E
BE
Beth Israel Deaconess Medical Center, 330 Brookline Avenue, Boston, MA 02215, USA.
Jacobs
Mark
M
Proper
Jo Ann
JA
Dahl
Thomas A
TA
Fujiwara
Tamio
T
Dezube
Bruce J
BJ
D000284:Administration, Oral; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D018791:CD4 Lymphocyte Count; D003967:Diarrhea / Q000139:chemically induced; D005260:Female; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1; D006801:Humans; D007093:Imidazoles; D008297:Male; D009325:Nausea / Q000139:chemically induced; D018894:Reverse Transcriptase Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013457:Sulfur Compounds; D019562:Viral Load
D019380:Anti-HIV Agents; D007093:Imidazoles; D018894:Reverse Transcriptase Inhibitors; D013457:Sulfur Compounds; C433874:capravirine