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Brazilian Journal of Pharmaceutical Sciences

On-line version ISSN 2175-9790


ANDRADE, Carolina Horta; FREITAS, Lenis Medeiros de  and  OLIVEIRA, Valéria de. Twenty-six years of HIV science: an overview of anti-HIV drugs metabolism. Braz. J. Pharm. Sci. [online]. 2011, vol.47, n.2, pp.209-230. ISSN 2175-9790.

From the identification of HIV as the agent causing AIDS, to the development of effective antiretroviral drugs, the scientific achievements in HIV research over the past twenty-six years have been formidable. Currently, there are twenty-five anti-HIV compounds which have been formally approved for clinical use in the treatment of AIDS. These compounds fall into six categories: nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), cell entry inhibitors or fusion inhibitors (FIs), co-receptor inhibitors (CRIs), and integrase inhibitors (INIs). Metabolism by the host organism is one of the most important determinants of the pharmacokinetic profile of a drug. Formation of active or toxic metabolites will also have an impact on the pharmacological and toxicological outcomes. Therefore, it is widely recognized that metabolism studies of a new chemical entity need to be addressed early in the drug discovery process. This paper describes an overview of the metabolism of currently available anti-HIV drugs.

Keywords : AIDS [treatment]; Drugs [anti-HIV]; Drugs [metabolism]; Antiretroviral drugs; Biotransformation.

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