Tenofovir Plasma Concentration from Preexposure Prophylaxis at the Time of Potential HIV Exposure: a Population Pharmacokinetic Modeling and Simulation Study Involving Serodiscordant Couples in East Africa

Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00446-19. doi: 10.1128/AAC.00446-19. Print 2019 Aug.

Abstract

The Partners Demonstration Project was a prospective, open-label, implementation science-driven study of preexposure prophylaxis (PrEP) among heterosexual HIV serodiscordant couples in Kenya and Uganda. Adherence data were collected using the Medication Event Monitoring System (MEMS), and time of sexual activity was collected using the mobile phone short message service (SMS). Two plasma samples were collected at a single study visit. We integrated adherence, pharmacokinetics, and SMS data using a population pharmacokinetic (PopPK) model to simulate tenofovir plasma concentrations from PrEP at the time of sexual activity. In the first stage of this analysis, we used data from the current study to update a prior PopPK model of tenofovir (TFV) developed with data from the Partners PrEP Study (a phase III clinical trial). The second stage involved simulating plasma concentrations at the time of sexual activity using empirical Bayes estimates (EBEs) derived from the final model. In addition, EBEs from a previously published parent metabolite model of TFV (MTN-001, an open-label 3-way crossover study in healthy women) was used to simulate tenofovir diphosphate (TFV-DP) concentrations. We estimated percent PrEP "coverage" as the number of reported sexual events during which simulated concentrations were above an a priori threshold concentrations associated with a high degree of protection from HIV infection: plasma TFV of >40 ng/ml and peripheral blood mononuclear cell (PBMC) TFV-DP concentration of >36 fmol/million cells. The levels of coverage were 72% for TFV and 81% for TFV-DP. These levels are consistent with a high degree of protection against HIV acquisition in this study of a pragmatic delivery model for antiretroviral-based HIV prevention.

Keywords: PrEP; population pharmacokinetics; preexposure prophylaxis; tenofovir.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Adenine / analogs & derivatives
  • Adenine / blood
  • Adenine / pharmacokinetics
  • Adenine / therapeutic use
  • Anti-HIV Agents / blood
  • Anti-HIV Agents / pharmacokinetics*
  • Anti-HIV Agents / therapeutic use*
  • Bayes Theorem
  • Cross-Over Studies
  • Female
  • HIV / drug effects*
  • HIV Infections / blood*
  • HIV Infections / drug therapy*
  • Humans
  • Kenya
  • Leukocytes, Mononuclear / virology
  • Male
  • Organophosphates / blood
  • Organophosphates / pharmacokinetics
  • Organophosphates / therapeutic use
  • Pre-Exposure Prophylaxis / methods
  • Prospective Studies
  • Sexual Partners
  • Tenofovir / blood
  • Tenofovir / pharmacokinetics*
  • Tenofovir / therapeutic use*
  • Uganda

Substances

  • Anti-HIV Agents
  • Organophosphates
  • tenofovir diphosphate
  • Tenofovir
  • Adenine