Frampton James E, Croom Katherine F
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 2006;66(11):1501-12; discussion 1513-4. doi: 10.2165/00003495-200666110-00012.
A new formulation combining fixed doses of the nucleoside reverse transcriptase inhibitors emtricitabine (200mg) and tenofovir disoproxil fumarate (tenofovir DF; 300 mg) with the non-nucleoside reverse transcriptase inhibitor efavirenz (600 mg) represents the first once-daily, one-tablet antiretroviral regimen. Co-formulated efavirenz/emtricitabine/tenofovir DF demonstrated bioequivalence to concomitant administration of the individual agents in a pharmacokinetic trial in healthy volunteers (n = 48). Co-formulated efavirenz/emtricitabine/tenofovir DF has not been evaluated in clinical trials. However, a once-daily regimen of efavirenz, emtricitabine and tenofovir DF (administered as individual agents) was superior to once-daily efavirenz plus twice-daily co-formulated lamivudine/zidovudine in terms of virological suppression, immunological recovery and adverse events resulting in discontinuation of the study medications in a randomised, multicentre, noninferiority study in treatment-naive patients with HIV infection (n = 517). Both regimens are currently recommended as initial antiretroviral therapy. Preliminary data suggest that co-formulated efavirenz/emtricitabine/tenofovir DF, like the individual agents in combination with other antiretroviral drugs, is generally well tolerated. CNS adverse events, primarily headache and dizziness, were the most common treatment-emergent, drug-related adverse events in the pharmacokinetic study involving the co-formulation.
一种新的配方，将固定剂量的核苷类逆转录酶抑制剂恩曲他滨（200毫克）和替诺福韦酯富马酸盐（替诺福韦DF；300毫克）与非核苷类逆转录酶抑制剂依非韦伦（600毫克）联合，代表了首个每日一次、一片剂的抗逆转录病毒治疗方案。在一项针对健康志愿者（n = 48）的药代动力学试验中，联合配方的依非韦伦/恩曲他滨/替诺福韦DF显示出与单独给药各药物具有生物等效性。联合配方的依非韦伦/恩曲他滨/替诺福韦DF尚未在临床试验中进行评估。然而，在一项针对初治HIV感染患者（n = 517）的随机、多中心、非劣效性研究中，依非韦伦、恩曲他滨和替诺福韦DF每日一次的治疗方案（单独给药）在病毒学抑制、免疫恢复以及导致研究药物停用的不良事件方面优于每日一次的依非韦伦加每日两次的联合配方拉米夫定/齐多夫定。目前这两种治疗方案均被推荐作为初始抗逆转录病毒治疗。初步数据表明，联合配方的依非韦伦/恩曲他滨/替诺福韦DF，与单独药物联合其他抗逆转录病毒药物一样，总体耐受性良好。中枢神经系统不良事件，主要是头痛和头晕，是涉及联合配方的药代动力学研究中最常见的治疗中出现的、与药物相关的不良事件。
