Wolfe E J, Cavacini L A, Samore M H, Posner M R, Kozial C, Spino C, Trapnell C B, Ketter N, Hammer S, Gambertoglio J G
Division of Clinical Pharmacy, University of California, San Francisco 94143-0622, USA.
Clin Pharmacol Ther. 1996 Jun;59(6):662-7. doi: 10.1016/S0009-9236(96)90006-5.
F105 is a human monoclonal antibody that binds to the CD4 binding site of human immunodeficiency virus type 1 gp120 and neutralizes clinical and laboratory isolates of the human immunodeficiency virus. This phase I study investigated the disposition of the antibody in humans. F105 was administered over a 60-minute period at two dose levels, 100 and 500 mg/m2. Blood samples were obtained for up to 56 days. The clearance of the antibody was 0.33 ml/min with a corresponding half-life of approximately 13 days. Peak concentrations achieved at the higher dose level were 216.19 +/- 9.62 micrograms/ml. The disposition of the drug was linear for the doses studied. Simulations were performed to design future studies aimed at investigating the efficacy of the antibody. This study concluded that F105 can be administered as a bolus dose every 21 days.
F105是一种人源单克隆抗体，它与人类免疫缺陷病毒1型（HIV-1）gp120的CD4结合位点结合，并能中和人类免疫缺陷病毒的临床和实验室分离株。这项I期研究调查了该抗体在人体内的处置情况。F105在两个剂量水平，即100和500 mg/m²下，在60分钟内给药。采集血样长达56天。该抗体的清除率为0.33 ml/分钟，相应的半衰期约为13天。较高剂量水平下达到的峰值浓度为216.19 +/- 9.62微克/毫升。在所研究的剂量范围内，药物的处置呈线性关系。进行了模拟以设计未来旨在研究该抗体疗效的研究。该研究得出结论，F105可以每21天作为一次推注剂量给药。
