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

Antimicrobial Agents and Chemotherapy - Tập 64 Số 8 - 2020
Rajith K. R. Rajoli1, Zach R. Demkovich2, Charles Flexner3, Andrew Owen1, Marco Siccardi1
1Department of Molecular and Clinical Pharmacology, University of Liverpool, Liverpool, United Kingdom
2RTI International, Durham, North Carolina, USA
3Johns Hopkins University School of Medicine and Bloomberg School of Public Health, Baltimore, Maryland, USA

Tóm tắt

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).

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