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

  title={Stampidine as a promising antiretroviral drug candidate for pre-exposure prophylaxis against sexually transmitted HIV/AIDS},
  author={Fatih M. Uckun and Pedro E. Cahn and Sanjive Qazi and Osmond J. D’cruz},
  journal={Expert Opinion on Investigational Drugs},
  pages={489 - 500}
  • F. UckunP. Cahn O. D’cruz
  • Published 13 March 2012
  • Biology, Medicine, Chemistry
  • Expert Opinion on Investigational Drugs
Introduction: 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. Areas covered: This article reviews the preclinical and early clinical activity and… 

HIV-1 CRF63_02A6 models as a tool for evaluating efficacy of developing antiretroviral drugs

The data demonstrate that CRF63_02A6 HIV-1 isolated strains and infectious molecular clones are relevant and complementary tools for assessing efficacy of developing drugs aimed at suppressing HIV- 1, including non-nucleoside-resistant virus reverse transcriptase inhibitors.

Recent advances in anogenital antiretroviral microbicides and multimodal delivery systems.

Preclinical/ clinical efficacy and safety profiles of current antiretroviral microbicides candidates are reviewed, as well as advances in multimodal microbicide delivery systems.

Preexposure chemoprophylaxis for HIV prevention in men who have sex with men.

Oral FTC-TDF provided protection against the acquisition of HIV infection among the subjects and Detectable blood levels strongly correlated with the prophylactic effect.

Advances in the development of nucleoside and nucleotide analogues for cancer and viral diseases

New nucleoside analogues and associated compounds that are currently in preclinical or clinical development for the treatment of cancer and viral infections, and that aim to provide increased response rates and reduced side effects are reviewed.

Chemopreventive efficacy of stampidine in a murine breast cancer model

Stampidine has potent chemopreventive activity and is as effective as the standard chemotherapy drug paclitaxel in the chemical carcinogenesis of DMBA-induced murine breast cancer model.

Phosphoramidates and phosphonamidates (ProTides) with antiviral activity

In this review, the seminal contribution of Chris McGuigan’s research to this field is presented and his technology proved to be extremely successful in drug discovery and has led to two Food and Drug Administration-approved antiviral agents.

1 Nucleoside Phosphate and Phosphonate Prodrug Clinical Candidates †

The different key monoph phosphate and monophosphonate nucleoside prodrugs that entered clinical development are discussed, some of which may in the future be approved to treat various human diseases.

Nucleoside Phosphate and Phosphonate Prodrug Clinical Candidates.

The different key monoph phosphate and monophosphonate nucleoside prodrugs that entered clinical development are discussed, some of which may in the future be approved to treat various human diseases.

Модели CRF63_02A6 ВИЧ-1 как инструмент для оценки эффективности разрабатываемых антиретровирусных препаратов

Highly active antiretroviral therapy (HAART) allows not only to control the infection process in a particular patient, but also to reduce the risk of spreading HIV infection in general, therefore one



Preclinical and first-in-human phase I clinical evaluation of stampidine, a potent anti-HIV pharmaceutical drug candidate.

The presented favorable preclinical and early clinical safety/activity profile of Stampidine warrants its further development as a new anti-HIV drug candidate.

Antiretroviral Pre-exposure Prophylaxis Prevents Vaginal Transmission of HIV-1 in Humanized BLT Mice

The utility of humanized mice to study intravaginal HIV-1 transmission is particularly highlighted by the demonstration that pre-exposure prophylaxis can prevent intravagsinal HIV -1 transmission in the BLT mouse model.

Oral Pre-Exposure Prophylaxis by Anti-Retrovirals Raltegravir and Maraviroc Protects against HIV-1 Vaginal Transmission in a Humanized Mouse Model

Two new classes of clinically approved drugs with different modes of action namely, an integrase inhibitor raltegravir and a CCR5 inhibitor maraviroc are evaluated as potential systemically administered chemo-prophylactics and show great promise for further development as orally administered PrEPs.

Pre-exposure prophylaxis in HIV

The PrEP has a potential to address unmet need in public health if delivered as a part of comprehensive toolkit of prevention services, including risk-reduction, correct and consistent use of condoms, and diagnosis and treatment of sexually transmitted infections.

In vitro activity of stampidine against primary clinical human immunodeficiency virus isolates.

The remarkable potency of STAMP against clinical HIV-1 isolates with N RTI- or NNRTI-resistance warrants the further development of this promising new antiviral agent.

Pre-exposure prophylaxis and antiretroviral resistance: HIV prevention at a cost?

  • C. HurtJ. EronMyron S. Cohen
  • Medicine
    Clinical infectious diseases : an official publication of the Infectious Diseases Society of America
  • 2011
The impact of signature mutations selected by PrEP, how rapidly these emerge with daily ARV exposure, and the individual-level and public health consequences of ARV resistance are discussed.

Microbicides for multidrug-resistant and multitropic HIV-1.

This review describes the discovery of potent anti-HIV-1 agents against multidrug-resistant and multitropic HIV-1 variants with implications for global microbicide development.

Oral preexposure anti-HIV prophylaxis for high-risk U.S. populations: current considerations in light of new findings.

Although TDF/FTC PrEP was generally well tolerated, side effects such as nausea, as well as mild and reversible renal abnormalities were increased among the men who received active medication, suggesting that PrEP users will need ongoing PrEP clinical monitoring.

Systemic Administration of Antiretrovirals Prior to Exposure Prevents Rectal and Intravenous HIV-1 Transmission in Humanized BLT Mice

In vivo preclinical findings provide strong experimental evidence supporting the potential clinical implementation of antiretroviral based pre-exposure prophylactic measures to prevent the spread of HIV/AIDS.

Pharmacological considerations for tenofovir and emtricitabine to prevent HIV infection.

This review identifies important cellular pharmacology considerations for tenofovir and emtricitabine, which include drug penetration into relevant tissues and cell types, race/ethnicity/pharmacogenetics, gender, cellular activation state and appropriate episodic or alternative dosing strategies based on pharmacokinetic principles.