Twenty-six years of HIV science: an overview of anti-HIV drugs metabolism

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.