Bictegravir in a fixed-dose tablet with emtricitabine and tenofovir alafenamide for the treatment of HIV infection: pharmacology and clinical implications

ABSTRACT

Introduction: Current antiretroviral therapy is more effective and simpler than in previous times due to the development of new drugs with improved pharmacokinetic and pharmacodynamic profiles and the advent of single pill regimens with low toxicity that facilitate long-term adherence. The recent approval of the novel potent integrase strand-transfer inhibitor bictegravir (BIC) co-formulated with emtricitabine (FTC) and tenofovir alafenamide (TAF) in a fixed daily dose pill, B/F/TAF, adds to the list of single-tablet regimens available to treat HIV infection.

Areas covered: This review provides an overview of the pharmacological and clinical information obtained from MEDLINE/PubMed publications and the latest international conferences.

Expert opinion: BIC is a potent antiretroviral with an improved resistance profile over previous integrase inhibitors. Its combination with the new tenofovir prodrug TAF and FTC creates an effective regimen B/F/TAF for treatment-naïve patients and for those switching from another successful combination. B/F/TAF’s favorable pharmacokinetic profile, simple dose, low pill burden, and few drug-drug interactions or treatment-related adverse events, will make it one of the preferred regimens in the future.

KEYWORDS:

• Bictegravir
• tenofovir alafenamide
• emtricitabine
• integrase inhibitors
• HIV treatment
• antiretroviral drug resistance

Acknowledgments

The authors thank ME Goring for his input into the composition of this manuscript.

Box 1. Drug summary box.

Declaration of interest

The authors have no other relevant affiliation or financial involvement with any organization or entity with financial interests or financial conflicts with the subject matter or materials discussed in the manuscript. Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This work was supported in part by Retrosolutions.