Predicting Pharmacokinetics of a Tenofovir Alafenamide Subcutaneous Implant Using Physiologically Based Pharmacokinetic Modelling

Author:

Rajoli Rajith K. R.1ORCID,Demkovich Zach R.2,Flexner Charles3,Owen Andrew1,Siccardi Marco1

Affiliation:

1. Department of Molecular and Clinical Pharmacology, University of Liverpool, Liverpool, United Kingdom

2. RTI International, Durham, North Carolina, USA

3. Johns Hopkins University School of Medicine and Bloomberg School of Public Health, Baltimore, Maryland, USA

Abstract

Long-acting (LA) administration using a subcutaneous (s.c.) implant presents opportunities to simplify administration of antiretroviral drugs, improve pharmacological profiles, and overcome suboptimal adherence associated with daily oral formulations. Tenofovir alafenamide (TAF) is a highly potent nucleoside reverse transcriptase inhibitor (NRTI) and an attractive agent for LA delivery, with a high potency and long intracellular half-life. The aim of this study was to predict minimum TAF doses required to achieve concentrations effective for HIV preexposure prophylaxis (PrEP).

Funder

HHS | NIH | National Institute of Allergy and Infectious Diseases

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Reference44 articles.

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2. UNAIDS. 2018. The youth bulge and HIV. https://www.unaids.org/sites/default/files/media_asset/the-youth-bulge-and-hiv_en.pdf. Accessed 21 January 2020.

3. Pre-exposure prophylaxis (PrEP) in an era of stalled HIV prevention: Can it change the game?

4. The Effect of PrEP on HIV Incidence Among Men Who Have Sex With Men in the Context of Condom Use, Treatment as Prevention, and Seroadaptive Practices

5. How safe is TDF/FTC as PrEP? A systematic review and meta-analysis of the risk of adverse events in 13 randomised trials of PrEP;Pilkington V;J Virus Erad,2018

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