Switching to bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC/TAF) plus darunavir/cobicistat in heavily antiretroviral-experienced, virologically suppressed HIV-infected adults receiving complex regimens

J Antimicrob Chemother. 2023 Nov 6;78(11):2696-2701. doi: 10.1093/jac/dkad285.

Abstract

Objectives: To evaluate the efficacy and safety of the two-pill regimen bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC/TAF) plus darunavir/cobicistat as a switching strategy in heavily treatment-experienced people living with HIV (PLWH).

Methods: Multicentre, prospective, single-arm pilot clinical trial. Participants were virologically suppressed adults receiving a stable antiretroviral regimen of at least three pills from at least three drug families due to previous virological failures and/or toxicities with no documented resistance to integrase strand transfer inhibitors or darunavir (≥15 points, Stanford). Clinical and laboratory assessments were performed at 0, 4, 12, 24, 36 and 48 weeks. HIV-1 proviral DNA was amplified and sequenced by Illumina at baseline. Plasma bictegravir concentrations were determined in 22 patients using UHPLC-MS/MS. The primary study endpoint was viral load (VL)< 50 copies/mL at Week 48 (ITT).

Results: We enrolled 63 participants (92% men) with median baseline CD4 count of 515 cells/mm3 (IQR: 334.5-734.5), 24 years on ART (IQR: 15.9-27.8). The median number of pills was 4 (range: 3-10). At baseline, proviral DNA was amplified in 39 participants: 33/39 had resistance mutations. Three participants discontinued owing to toxicity. At 48 weeks, 95% had VL < 50 copies/mL by ITT and 100% by PP analysis. A modest increase was observed in the bictegravir plasma concentration, and a significant decrease in estimated glomerular filtration rate was observed only at Week 4, probably related to interaction with renal transporters.

Conclusions: Our data suggest that BIC/FTC/TAF + darunavir/cobicistat is an effective, well-tolerated regimen that may improve convenience and, potentially, long-term success in stable heavily pre-treated PLWH.

Publication types

  • Clinical Trial
  • Multicenter Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / therapeutic use
  • Adult
  • Alanine / therapeutic use
  • Anti-HIV Agents* / adverse effects
  • Anti-Retroviral Agents / therapeutic use
  • Cobicistat / therapeutic use
  • DNA / therapeutic use
  • Darunavir / therapeutic use
  • Emtricitabine / therapeutic use
  • Female
  • HIV Infections* / drug therapy
  • Humans
  • Male
  • Prospective Studies
  • Tandem Mass Spectrometry

Substances

  • Adenine
  • Alanine
  • Anti-HIV Agents
  • Anti-Retroviral Agents
  • bictegravir
  • Cobicistat
  • Darunavir
  • DNA
  • Emtricitabine
  • tenofovir alafenamide