ABCB1/P-glycoprotein (P-gp) is an ATP-dependant transmembrane efflux protein widely expressed in human organs and plays a protective role against endogenous and exogenous substances. It is involved in drug pharmacokinetics affecting drug absorption, disposition and elimination. At the BBB level, due to its luminal localisation, ABCB1 limits drug transport and is important in central detoxification. Inter-individual variability has been described in ABCB1 expression and functionality. Recent work suggests that variability may play a role in the pathogenesis of neurological diseases. Furthermore, ABCB1 expression and/or functionality may modify drug efficacy or increase central adverse events. This paper reviews ABCB1 implication in the pathophysiology of Parkinson's disease and its role in the cerebral distribution of drugs.