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

J. Zeuli, S. Rizza, R. Bhatia, Z. Temesgen

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)669-682
Number of pages14
JournalDrugs of Today
Issue number11
StatePublished - 2019


  • Anti-HIV agents
  • Antiretroviral drugs
  • Bictegravir
  • Emtricitabine
  • Fixed combination
  • HIV infection
  • HIV integrase inhibitors
  • Tenofovir alafenamide

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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