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

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.
AuthorsCapital A Cyrillic L Khandazhinskaya, E A Shirokova
JournalActa naturae (Acta Naturae) Vol. 5 Issue 3 Pg. 54-61 (Jul 2013) ISSN: 2075-8251 [Print] Russia (Federation)
PMID24307936 (Publication Type: Journal Article)

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