Gewurz Benjamin E, Jacobs Mark, Proper Jo Ann, Dahl Thomas A, Fujiwara Tamio, Dezube Bruce J
Beth Israel Deaconess Medical Center, 330 Brookline Avenue, Boston, MA 02215, USA.
J Infect Dis. 2004 Dec 1;190(11):1957-61. doi: 10.1086/425581. Epub 2004 Oct 27.
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.
卡普瑞韦是一种具有独特耐药谱的非核苷类逆转录酶抑制剂（NNRTI）。虽然单个突变可导致对已有的NNRTIs产生耐药性，但人类免疫缺陷病毒（HIV）-1必须发生多个突变才能对卡普瑞韦产生耐药性。在当前的1期研究中，对55名CD4 + T淋巴细胞计数为50 - 500个细胞/微升的HIV-1感染个体口服给予卡普瑞韦，持续28天。最常见的不良事件为腹泻（5%）和恶心（4%），未观察到与药物相关的皮疹。接受25 mg/kg/天治疗的患者在第15天HIV-1载量中位数（平均值）下降了1.34（1.45）log(10)拷贝/毫升。卡普瑞韦即使在有抗逆转录病毒治疗经验的患者中也表现出强效的抗病毒活性。
