AZT 5’-Phosphonates: Achievements and Trends in the Treatment and Prevention of HIV Infection

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Despite the numerous drawbacks, 3’-azido-3’-deoxythymidine (AZT, Zidovudine, Retrovir) remains one of the key drugs used in the treatment and prevention of HIV infection in both monotherapy and HAART. A strategy in searching for new effective and safe AZT agents among latent (depot) forms of AZT has yielded its first positive results. In particular, the sodium salt of AZT 5’-H-phosphonate (Nikavir, phosphazide) has demonstrated clinical advantages over parent AZT: first and foremost, lower toxicity and better tolerability. It can be effectively used for the prevention of vertical transmission from mothers to babies and as an alternative drug for HIV-infected patients with low tolerance to Zidovudine. Preclinical studies of another phosphonate, AZT 5’-aminocarbonylphosphonate, have demonstrated that it releases AZT when taken orally. Pharmacokinetic studies have shown a prolonged action potential. Based on the analysis of both toxicological and pharmacological data, AZT 5’-aminocarbonylphosphonate has been recommended for clinical trials.

About the authors

А. L. Khandazhinskaya

Engelhardt Institute of Molecular Biology, Russian Academy of Sciences

Author for correspondence.
Russian Federation

E. A. Shirokova

Engelhardt Institute of Molecular Biology, Russian Academy of Sciences

Russian Federation


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Copyright (c) 2013 Khandazhinskaya А.L., Shirokova E.A.

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