Kempf Dale J, King Martin S, Bernstein Barry, Cernohous Paul, Bauer Eric, Moseley Jennifer, Gu Kai, Hsu Ann, Brun Scott, Sun Eugene
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois, USA.
J Infect Dis. 2004 Jan 1;189(1):51-60. doi: 10.1086/380509. Epub 2003 Dec 31.
Study M98-863 was a double-blind, randomized, phase 3 study that compared lopinavir/ritonavir with nelfinavir, each coadministered with stavudine and lamivudine, in 653 antiretroviral therapy-naive human immunodeficiency virus (HIV) type 1-infected subjects. The incidence of HIV drug resistance was analyzed using baseline and rebound virus isolates from subjects with plasma HIV RNA >400 copies/mL from weeks 24 to 108 of therapy. No evidence of genotypic or phenotypic resistance to lopinavir/ritonavir, defined as any active site or primary mutation in HIV protease, was detected in virus isolates from 51 lopinavir/ritonavir-treated subjects with available genotypes. Primary mutations related to nelfinavir resistance (D30N and/or L90M) were observed in 43 (45%) of 96 nelfinavir-treated subjects. Resistance to lamivudine and stavudine was also significantly higher in nelfinavir-treated versus lopinavir/ritonavir-treated subjects. These differences suggest substantially different genetic and pharmacological barriers to resistance for these 2 protease inhibitors and may have implications for strategies for initiating antiretroviral therapy.
M98 - 863研究是一项双盲、随机、3期研究,在653例初治的1型人类免疫缺陷病毒(HIV)感染受试者中,比较了洛匹那韦/利托那韦与奈非那韦,二者均与司他夫定和拉米夫定联合使用。使用治疗第24周至108周血浆HIV RNA>400拷贝/mL受试者的基线和反弹病毒分离株分析HIV耐药性发生率。在51例有可用基因型的接受洛匹那韦/利托那韦治疗的受试者的病毒分离株中,未检测到对洛匹那韦/利托那韦的基因型或表型耐药证据,定义为HIV蛋白酶中的任何活性位点或主要突变。在96例接受奈非那韦治疗的受试者中,43例(45%)观察到与奈非那韦耐药相关的主要突变(D30N和/或L90M)。与接受洛匹那韦/利托那韦治疗的受试者相比,接受奈非那韦治疗的受试者对拉米夫定和司他夫定的耐药性也显著更高。这些差异表明这两种蛋白酶抑制剂在耐药性方面存在显著不同的遗传和药理学屏障,可能对启动抗逆转录病毒治疗的策略有影响。