Abstract:
The peptidic antiretroviral enfuvirtide (Fuzeon) is the first clinically approved antiviral fusion inhibitor and the first antiretroviral that must routinely be administered parenterally. Its extracellular activity results both in activity against current drug-resistant strains of HIV-1 and a low potential for systemic toxicities. As a peptide, enfuvirtide also exhibits few interactions with other antiretrovirals and concomitant medications used in HIV disease. Enfuvirtide shows potent antiretroviral activity and significantly improves medical outcomes in highly treatment-experienced patients with HIV-1 infection, but like other antiretrovirals must be given as part of a carefully selected combination regimen to minimise the risk of emergent drug resistance. Despite its subcutaneous route of administration, clinical data indicate that most patients can accept long-term enfuvirtide treatment with little difficulty or impact on daily activities. The only common adverse event associated with enfuvirtide use is injection-site reactions of generally mild-to-moderate severity, which are seldom treatment-limiting.
摘要:
肽抗逆转录病毒enfuvirtide(Fuzeon)是第一个临床批准的抗病毒融合抑制剂,也是第一个必须常规肠胃外给药的抗逆转录病毒药物。它的细胞外活性导致对HIV-1的当前耐药株的活性和系统性毒性的低可能性。作为一种肽,恩夫韦肽还表现出与其他抗逆转录病毒药物和用于HIV疾病的伴随药物的相互作用。Enfuvirtide显示出有效的抗逆转录病毒活性,并显着改善了具有高度治疗经验的HIV-1感染患者的医疗结果。但与其他抗逆转录病毒药物一样,必须作为精心选择的联合治疗方案的一部分,以最大程度地降低出现耐药性的风险。尽管其皮下给药途径,临床数据表明,大多数患者可以接受长期恩夫韦肽治疗,几乎没有困难或对日常活动的影响。与恩夫韦肽使用相关的唯一常见不良事件是注射部位反应,一般为轻度至中度。很少限制治疗。