FP-21399 is a bis(disulfonaphthalene) derivative that prevents human immunodeficiency virus (HIV) infection of uninfected cells by blocking entry of the virus. FP-21399 shows an affinity for lymph nodes. In this phase I study, FP-21399 was administered intravenously over 1 h as a single dose (0.9, 1.7, 2.8, and 4.2 mg/kg) or as a once-weekly infusion (1, 2, and 3 mg/kg) for 4 consecutive weeks to 34 HIV-1 infected patients with CD4+ cell counts of 50-400 cells/μL. Concomitant antiretroviral therapy was permitted but not required. The most frequent adverse events involved the transient, dose-dependent appearance of drug- or metabolite-related color in the urine and skin. Plasma drug levels were linear with dose. The drug was cleared, with an elimination half-life of 4 h and a terminal half-life of 1.5-2 days; the terminal half-life represented redistribution and clearance from tissues. FP-21399 administered weekly for 4 weeks was well tolerated. Further studies are necessary to define the role of this fusion inhibitor in the treatment of HIV infection.
CITATION STYLE
Dezube, B. J., Dahl, T. A., Wong, T. K., Chapman, B., Ono, M., Yamaguchi, N., … Crumpacker, C. S. (2000). A fusion inhibitor (FP-21399) for the treatment of human immunodeficiency virus infection: A phase I study. Journal of Infectious Diseases, 182(2), 607–610. https://doi.org/10.1086/315703
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