Tsai C C, Follis K E, Beck T W, Sabo A, Bischofberger N, Dailey P J
Washington Regional Primate Research Center, Seattle 98195, USA.
AIDS Res Hum Retroviruses. 1997 May 20;13(8):707-12. doi: 10.1089/aid.1997.13.707.
(R)-9-(2-Phosphonylmethoxypropyl)adenine (PMPA) acts as a reverse transcriptase inhibitor of retroviruses and has been shown to be effective against acute simian immunodeficiency virus (SIV) infection in macaques. To study its efficacy at different stages of infection, we tested PMPA in cynomolgus macaques (Macaca fascicularis) that had been chronically infected with SIVMne for at least 19 weeks before treatment was begun. PMPA was administered subcutaneously in a single daily dose of either 30 or 75 mg/kg body weight for 28 days. Within < or = 2 weeks of treatment, PMPA in both dosing regimens reduced SIV levels by >99% in the plasma or peripheral blood mononuclear cells; in some macaques SIV levels were reduced to below the lower quantitation limit. At a dose of 30 mg/kg/day PMPA was well tolerated, causing no side effects while increasing the mean CD4+ cell counts in animals that received this dose. Thus PMPA seems to be a promising agent for use against retroviral infections.
（R）-9-（2-膦酰甲氧基丙基）腺嘌呤（PMPA）作为逆转录病毒的逆转录酶抑制剂，已被证明对猕猴的急性猿猴免疫缺陷病毒（SIV）感染有效。为了研究其在感染不同阶段的疗效，我们在治疗开始前已被SIVMne慢性感染至少19周的食蟹猴（猕猴）中测试了PMPA。PMPA以30或75mg/kg体重的单日剂量皮下给药，持续28天。在治疗的≤2周内，两种给药方案中的PMPA都使血浆或外周血单核细胞中的SIV水平降低了>99%；在一些猕猴中，SIV水平降至定量下限以下。在30mg/kg/天的剂量下，PMPA耐受性良好，没有引起副作用，同时增加了接受该剂量动物的平均CD4+细胞计数。因此，PMPA似乎是一种有前景的抗逆转录病毒感染药物。
