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随着对人免疫缺陷病毒1型(HIV-1)的深入了解,已经研制出许多作用于病毒特异性部位的药物。叠氮脱氧胸腺嘧啶核苷(Zidovudine,AZT)仍是主要的抗HIV-1药。最近的对照研究表明,AZT应以更小剂量用于早期感染。可是对艾滋病病人延长AZT疗程常引起病毒抗药性。更新的逆转录酶抑制性核苷衍生物正投入Ⅱ~Ⅲ期临床试验。临床研究中的其他HIV-1复制的作用部位包括病毒结合和穿入、囊膜蛋白糖基化及病毒组装和释放。作用于蛋白酶、整合酶、核糖核酸酶H及调节基因(如tat等的产物)的药物正在研制中。作用于不同病毒复制部位的联合治疗可使用中毒浓度以下的各种药物,并有助于预防抗药性。
With the deep understanding of human immunodeficiency virus type 1 (HIV-1), many drugs have been developed that act on virus-specific sites. Zidovudine (AZT) remains the major anti-HIV-1 drug. Recent controlled studies have shown that AZT should be used at lower doses for early infection. However, AZT treatment of AIDS patients often lead to drug resistance. Updated reverse transcriptase inhibitory nucleoside derivatives are being put into Phase II ~ III clinical trials. The site of action for other HIV-1 replication in clinical studies includes viral binding and penetration, glycoproteinization of the envelope, and viral assembly and release. Drugs that act on proteases, integrases, ribonucleases H, and regulatory genes (products such as tat) are under development. Combined treatment of different viral replication sites can use a variety of drugs below the concentration of poisoning and help prevent drug resistance.