Evaluating emtricitabine + rilpivirine + tenofovir alafenamide in combination for the treatment of HIV-infection

ABSTRACT

Introduction: Antiretroviral therapy (ART) is recommended for all people who are living with HIV to suppress viral load and to stop the progression and transmission of HIV-1. Fixed-dose combinations of antiretrovirals largely reduce pill burden.

Areas covered: The authors first provide an overview of the use of non-nucleoside reverse transcriptase inhibitor (NNRTI) based therapy in HIV care. They then summarize the properties of each drug in the fixed-dose combination of tenofovir alafenamide/emtricitabine/rilpivirine/(TAF/FTC/RPV). The efficacy and safety of each component and the combination as a whole are reviewed: FTC is non-inferior to lamivudine (3TC) at assessed dosages; TAF was non-inferior to tenofovir disoproxil fumarate (TDF); the viral efficacy of RPV is non-inferior with EFV at the assessed dosage; TAF/FTC/RPV is non-inferior in efficacy but shows less of a decline in bone mineral density and renal function compared to TDF/FTC/RPV. Finally, adverse effects and drug–drug interaction data with FTC/RPV/TAF are discussed.

Expert opinion: TAF/FTC/RPV can be used as an initial regimen for people living with HIV whose HIV RNA <100,000 copies/ml and CD4 cell count > 200 cells/mm³ when INSTI-based regimens are not a treatment option. Future antiretroviral therapy development may focus on dual therapy-based regimens containing RPV, particularly as long-acting formulations.

KEYWORDS:

• Antiretroviral therapy
• emtricitabine
• rilpivirine
• tenofovir alafenamide

Acknowledgments

We wish to thank Dr. Wei Li for providing ChemDraw software, and Hanxuan Li for assistance with using the ChemDraw software.

Declaration of interest

The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

One referee declares that they worked on the development of tenofovir. Another referee of this manuscript is an employee and stockholder of Gilead Sciences. Peer reviewers on this manuscript have no other relevant financial relationships or otherwise to disclose.

Additional information

Funding

This work was supported by National Institute on Drug Abuse (NIDA/NIAID) Grants R01DA047178 (to TJ Cory), and K23AI134307 (to AT Podany).