Meng T C, Fischl M A, Richman D D
University of California San Diego Treatment Center 92103.
Am J Med. 1990 May 21;88(5B):27S-30S. doi: 10.1016/0002-9343(90)90419-e.
The dideoxynucleosides 3'-azido-3'-deoxythymidine (zidovudine, AZT) and 2',3'-dideoxycytidine (ddC) are potent inhibitors of human immunodeficiency virus (HIV) in vitro and improve surrogate measures of HIV infection in vivo. Long-term administration of AZT has been associated with significant hematologic toxicity and has resulted in virus with reduced in vitro susceptibility. Although ddC does not have significant hematologic toxicity and has not shown cross-resistance with AZT in vitro, ddC has been associated with a severe dose-related peripheral neuropathy. Given the independent activity of each agent, their non-overlapping toxicity profiles, and the absence of cross-resistance, it was hypothesized that concurrent administration of AZT and ddC in low doses might be at least as active as either drug given individually at higher doses in the treatment of HIV infection. It was further hypothesized that combined low doses of both drugs would reduce the incidence of serious side effects and the development of resistance. A phase I/II dose-finding trial of six different regimens of combination AZT and ddC in persons with acquired immunodeficiency syndrome (AIDS) or advanced AIDS-related complex was initiated to test these hypotheses.
双脱氧核苷3'-叠氮-3'-脱氧胸苷(齐多夫定,AZT)和2',3'-双脱氧胞苷(ddC)在体外是人类免疫缺陷病毒(HIV)的有效抑制剂,并能改善体内HIV感染的替代指标。长期服用AZT与显著的血液学毒性有关,并导致病毒在体外的敏感性降低。虽然ddC没有显著的血液学毒性,且在体外未显示与AZT有交叉耐药性,但ddC与严重的剂量相关外周神经病变有关。鉴于每种药物的独立活性、不重叠的毒性谱以及不存在交叉耐药性,有人推测,低剂量同时服用AZT和ddC在治疗HIV感染方面可能至少与单独高剂量服用任何一种药物一样有效。进一步推测,两种药物联合低剂量使用将降低严重副作用的发生率和耐药性的产生。一项针对获得性免疫缺陷综合征(AIDS)或晚期AIDS相关综合征患者的AZT和ddC联合用药六种不同方案的I/II期剂量探索试验启动,以检验这些假设。