Drug intelligence / Profile preview

probenecid + tenofovir disoproxil fumarate + emtricitabine

Development stage
Unknown
Lead developer
Indiana University
Modality
Small Molecules
Administration
Oral
01

Overview

probenecid + tenofovir disoproxil fumarate + emtricitabine is a combination therapy being investigated by Indiana University as a novel "boosting" strategy for HIV pre-exposure prophylaxis (PrEP). The regimen combines the uricosuric agent probenecid with the standard-of-care fixed-dose combination of tenofovir disoproxil fumarate (TDF) and emtricitabine (FTC). Probenecid acts as a pharmacokinetic enhancer by inhibiting organic anion transporters 1 and 3 (OAT1/3) in the renal proximal tubules. These transporters are responsible for the active secretion of tenofovir into the urine; by blocking them, probenecid aims to reduce the intra-renal concentration of tenofovir, potentially mitigating the drug's associated nephrotoxicity and bone mineral density loss while maintaining or enhancing systemic exposure for HIV prevention.

Other names
probenecid + TDF/FTCprobenecid + Truvadaprobenecid-boosted TDF/FTC
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseSLC22A8 (Organic anion transporter 3)OAT1 (Organic anion transporter 1)

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