P-glicoproteina e terapia antiretrovirale

Objective: P-glycoprotein (P-gp), a transmembrane protein capable of transporting different substrates, has been identified among farmacologic variables that can modify the availability of antiretroviral drugs. P-gp has similar tissue distribution and similar substrates of cytochrome P450 subfamily 3A4, an enzyme system responsible for biotransformation of endogenous and exogenous substances. Methods: The aim of the paper is to analyse the role of P-gp as far as the pharmacokinetic of antiretroviral drugs is concerned and to evaluate possible strategies to overcome the interactions with these compounds. Results and conclusions: The therapeutic strategies that imply the modulation of P-gp may be clinically useful. Nevertheless, the usage of P-gp inhibitors in human beings should be addressed within clinical trials as higher concentrations of drugs in sanctuaries, usually protected by P-gp, might give rise to relevant toxicity.