Tebas P, Powderly W G
Division of Infectious Diseases, Washington University School of Medicine, Box 8051, St. Louis, MO 63110, USA.
Expert Opin Pharmacother. 2000 Dec;1(7):1429-40. doi: 10.1517/14656566.1.7.1429.
Nelfinavir is an inhibitor of the HIV-1 and HIV-2 protease, with good in vivo activity in HIV-infected patients. Nelfinavir is used in combination with other antiretroviral medications as part of a potent antiretroviral regimen. When used in this manner, 50-75% of patients who are naïve to antiretroviral therapy have plasma HIV RNA levels below the limit of detection (< 400 copies) after 12 months of treatment. This use of nelfinavir in combination regimens is associated with an increase of almost 200/mm3 CD4+ lymphocytes at 12 months of therapy. Initial trials and clinical experience indicate that nelfinavir is equipotent to other potent protease inhibitors (PIs). The drug is well-tolerated, with mild diarrhoea being the most common side effect in 12-20% of patients. Virologic failure of nelfinavir is associated with genotypic and phenotypic changes that have a unique pattern that may retain susceptibility to other PIs. The results of small, non-controlled trials suggest these failures can be rescued with a second protease-based regimen. Due to the above characteristics, nelfinavir has become the most frequently prescribed first line PI.
奈非那韦是一种HIV-1和HIV-2蛋白酶抑制剂，在HIV感染患者中具有良好的体内活性。奈非那韦与其他抗逆转录病毒药物联合使用，作为强效抗逆转录病毒治疗方案的一部分。以这种方式使用时，在接受12个月治疗后，50%-75%未接受过抗逆转录病毒治疗的患者血浆HIV RNA水平低于检测下限（<400拷贝）。在联合治疗方案中使用奈非那韦与治疗12个月时CD4+淋巴细胞增加近200/mm3相关。初步试验和临床经验表明，奈非那韦与其他强效蛋白酶抑制剂（PIs）效力相当。该药物耐受性良好，12%-20%的患者最常见的副作用是轻度腹泻。奈非那韦的病毒学失败与具有独特模式的基因型和表型变化相关，这些变化可能使病毒对其他PIs保持敏感性。小型非对照试验结果表明，这些失败情况可用第二种基于蛋白酶的治疗方案挽救。由于上述特点，奈非那韦已成为最常处方的一线PI。
