Stampidine as a promising antiretroviral drug candidate for pre-exposure prophylaxis against sexually transmitted HIV/AIDS

Expert Opinion on Investigational Drugs
F M UckunOsmond J D'Cruz

Abstract

Pre-exposure prophylaxis (PrEP) is an evolving new approach to prevention of sexually transmitted HIV-1 that employs antiretroviral (ARV) agents prior to potential HIV-1 exposure in an attempt to reduce the likelihood of HIV-1 infection postexposure. The identification of new ARV agents with potent activity against multidrug-resistant HIV remains an unmet and urgent challenge in the field of PrEP. This article reviews the preclinical and early clinical activity and safety profile of stampidine, a novel antiretroviral (ARV) drug candidate that exhibits remarkable subnanomolar to low nanomolar in vitro antiretroviral potency against genotypically and phenotypically nucleoside reverse transcriptase inhibitor (NRTI)-resistant primary clinical HIV isolates, non-nucleoside RT-resistant HIV-1 isolates. Stampidine has a favorable pharmacokinetic profile in mice, rats, dogs and cats with 25 or 50 mg/kg tolerable dose levels yielding micromolar plasma concentrations that are 1000-fold higher than its in vitro IC(50) value against HIV. Stampidine has a favorable, safety profile in mice, rats, dogs and cats and it showed significant in vivo ARV activity in HIV-infected Hu-PBL-SCID mice as well as FIV-infected domestic cats. Furthermore, it...Continue Reading

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Jun 1, 2013·Nature Reviews. Drug Discovery·Lars Petter JordheimCharles Dumontet
Aug 26, 2016·Journal of Medicinal Chemistry·Peter J ThorntonYoucef Mehellou
Feb 2, 2020·Expert Opinion on Therapeutic Targets·Kazim SahinFatih Mehmet Uckun
May 25, 2018·Antiviral Chemistry & Chemotherapy·Magdalena SlusarczykFabrizio Pertusati

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