Bictegravir, a novel integrase inhibitor for the treatment of HIV infection.

• Zeuli, J ^{[1] [3]} ; Rizza, S. ^[3] ; Bhatia, R. ^[2] ; Temesgen, Z. ^[3]
  1. [1] Mayo Clinic

     Mayo Clinic

     City of Rochester, Estados Unidos

     
  2. [2] University of Illinois at Chicago

     University of Illinois at Chicago

     City of Chicago, Estados Unidos

     
  3. [3] HIV Program, Mayo Clinic and Foundation, Division of Infectious Diseases, 200 First St. SW, Rochester, MN 55905, United States

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• Localización: Medicamentos de actualidad = Drugs of today, ISSN 1699-3993, Vol. 55, Nº. 11, 2019 (Ejemplar dedicado a: Noviembre), págs. 669-682
• Idioma: inglés
• Texto completo no disponible (Saber más ...)
• Resumen

  • Bictegravir (BIC), a second-generation integrase strand transfer inhibitor (INSTI) approved for HIV treatment in fixed-dose combination with emtricitabine and tenofovir alafenamide, has potent antiviral activity in vitro to wild-type virus and strains with resistance to first-generation INSTIs. As part of combination therapy, BIC's virologic suppression rates in clinical trials are comparable to those of first-line combination antiretroviral drug regimens. BIC has demonstrated a high genetic barrier to resistance development in vitro, can be administered with or without food, and has a bioavailability of > 70%. A median plasma half-life of 18 hours allows once-daily dosing. Clearance is primarily hepatic through cytochrome P450 3A4 (CYP3A4) oxidation and UDP-glucuronosyltransferase 1A1 (UGT1A1) glucuronidation. Thus, potent inducers of UGT1A1 and CYP3A4 (e.g., rifamycins/anticonvulsants) should be avoided due to significantly decreased BIC serum exposure. Chelation with polyvalent cations can decrease absorption; otherwise, drug-drug interactions are few. BIC is well tolerated; diarrhea, nausea and headache are the main adverse effects associated with its use.