A fusion inhibitor (FP-21399) for the treatment of human immunodeficiency virus infection: A phase I study

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Abstract

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.

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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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