Gilead Sciences, Inc., Foster City, California 94404, USA.
J Acquir Immune Defic Syndr. 2009 Oct 1;52(2):209-21. doi: 10.1097/QAI.0b013e3181b05f7c.
Study 934 was an open-label, randomized Phase III study of emtricitabine + tenofovir DF + efavirenz (FTC + TDF + EFV) compared with lamivudine + zidovudine + efavirenz (3TC + ZDV + EFV) in antiretroviral therapy-naïve HIV-1 infected subjects. Baseline genotyping revealed the presence of primary nonnucleoside reverse transcriptase inhibitor resistance (NNRTI-R) in 22 of 509 enrolled patients (4.3%, 11 subjects in each group). The 487 subjects without baseline NNRTI-R formed the primary efficacy population (modified intent-to-treat population). Through 144 weeks, 50 of 487 modified intent-to-treat subjects (FTC + TDF + EFV, n = 19; 3TC + ZDV + EFV, n = 31) were analyzed for resistance development after virologic failure. NNRTI-R, primarily the K103N mutation, was the most common form of resistance that developed in both groups. No subject on FTC + TDF + EFV developed the K65R mutation. Significantly fewer subjects on FTC + TDF + EFV compared with 3TC + ZDV + EFV developed the M184V/I mutation (two versus 10, respectively, P = 0.021). Thymidine analog mutations developed in two subjects on 3TC + ZDV + EFV. Subjects with baseline NRTI genotypic resistance (TAMs, n = 13) or non-B HIV-1 subtypes (n = 28) showed no evidence of reduced treatment responses in either group. Nine of 22 patients with baseline NNRTI-R experienced virologic failure (FTC + TDF + EFV, n = 4; 3TC + ZDV + EFV, n = 5); seven of nine developed M184V/I and/or additional NNRTI-R, but none developed K65R. Baseline NNRTI-R was significantly associated with virologic failure in both groups (P < 0.001).
研究 934 是一项开放性、随机的 III 期研究,比较了恩曲他滨+替诺福韦酯+依法韦仑(FTC+TDF+EFV)与拉米夫定+齐多夫定+依法韦仑(3TC+ZDV+EFV)在初治 HIV-1 感染患者中的疗效。基线基因分型显示,509 名入组患者中有 22 名(4.3%,每组各 11 名)存在原发性非核苷类逆转录酶抑制剂耐药(NNRTI-R)。487 名无基线 NNRTI-R 的患者构成主要疗效人群(修改后的意向治疗人群)。在 144 周时,对 487 名修改后的意向治疗患者(FTC+TDF+EFV,n=19;3TC+ZDV+EFV,n=31)中的 50 名患者进行了病毒学失败后的耐药性发展分析。NNRTI-R,主要是 K103N 突变,是两组中最常见的耐药形式。FTC+TDF+EFV 组无 K65R 突变。与 3TC+ZDV+EFV 组相比,FTC+TDF+EFV 组中 M184V/I 突变的发生率明显较低(分别为 2 例和 10 例,P=0.021)。3TC+ZDV+EFV 组中有 2 例患者出现胸苷类似物突变。基线核苷类逆转录酶抑制剂基因型耐药(TAMs,n=13)或非 B 型 HIV-1 亚型(n=28)的患者在两组中均无治疗反应降低的证据。基线 NNRTI-R 的 22 名患者中有 9 名发生病毒学失败(FTC+TDF+EFV,n=4;3TC+ZDV+EFV,n=5);其中 7 名患者出现 M184V/I 和/或其他 NNRTI-R,但均未出现 K65R。两组中基线 NNRTI-R 均与病毒学失败显著相关(P<0.001)。
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