Bioactivation to an aldehyde metabolite--possible role in the onset of toxicity induced by the anti-HIV drug abacavir.

摘要: Aldehydes are highly reactive molecules, which can be generated during numerous physiological processes, including the biotransformation of drugs. Several non-P450 enzymes participate in their metabolism albeit alcohol dehydrogenase and aldehyde ones most frequently involved this process. Endogenous exogenous aldehydes have been strongly implicated multiple human pathologies. Their ability to react with biomacromolecules (e.g. proteins) yielding covalent adducts is suggested common primary mechanism underlying toxicity these species. Abacavir one options for combined anti-HIV therapy. Although individual susceptibilities adverse effects differ among patients, abacavir associated idiosyncratic hypersensitivity drug reactions an increased risk cardiac dysfunction. This review highlights current knowledge on discusses potential role bioactivation metabolite, capable forming protein adducts, onset abacavir-induced toxic outcomes.