Vittecoq D, Woerle R, Barre-Sinoussi F, Chermann J C
Department of Immunology, Hôpital Necker, Paris, France.
Biomed Pharmacother. 1988;42(1):35-9.
Ammonium tungsto antimoniate (HPA 23) is a potent inhibitor of nucleic acid polymerases and reverse transcriptases of retroviruses. Its in vivo activity as an HIV inhibitor was previously published. However, its clinical use is limited by pharmacological parameters (short half-life and intravenous administration) and significant side effects (thrombocytopenia). In order to evaluate the place of this drug in the therapeutic strategy of HIV-infected patients, we administered 1.5 mg/kg of HPA 23 in 15 infected patients at various stages of the disease twice a day during 14 days. A significant decrease of reverse transcriptase activity (less than 15% of the initial value) was noticed in 13 patients. This activity remained low at least 6 weeks after the end of the treatment in 8 patients. Thrombocytopenia was the only significant side effect reported and was always transient. This study suggests that HPA 23 can be used as an induction treatment in patients infected by HIV. A maintenance treatment has to be defined, as well as the association to other drugs.
钨锑酸铵(HPA 23)是逆转录病毒核酸聚合酶和逆转录酶的有效抑制剂。其作为HIV抑制剂的体内活性此前已有报道。然而,其临床应用受到药理学参数(半衰期短和静脉给药)以及显著副作用(血小板减少症)的限制。为了评估该药物在HIV感染患者治疗策略中的地位,我们对15例处于疾病不同阶段的感染患者,每天两次给予1.5 mg/kg的HPA 23,持续14天。13例患者的逆转录酶活性显著降低(低于初始值的15%)。8例患者在治疗结束后至少6周,该活性仍保持较低水平。血小板减少症是唯一报告的显著副作用,且总是短暂的。本研究表明,HPA 23可作为HIV感染患者的诱导治疗药物。必须确定维持治疗方案以及与其他药物的联合使用方案。