beta-carotene is the major carotenoid occurring in the human diet and in the human organism. Besides its function as pro-vitamin A, beta-carotene has been shown to be an activator of the human pregnan X receptor (PXR). PXR is mainly expressed in the liver/intestine and an inducer of enzymes involved in phase I, II and III metabolism. This review is focused on the evaluation of physiological and nutritional relevance of beta-carotene as an inducer of phase I enzymes in the human organism via PXR-mediated mechanisms. Beneficial and detrimental effects of beta-carotene on xenobiotica metabolism and metabolism of various other derivatives will be discussed.