This discussion outlines the major aspects of the human pharmacology of fenofibrate, a hypolipidemic agent. In view of its short half-life, efficient absorption, and elimination, fenofibrate would not appear to accumulate in either plasma or tissues. It is extensively absorbed only in the presence of food and is transported through the bloodstream by albumin. Fenofibrate is taken up by both the liver and kidney. Except for a small percentage (about 5 percent) reduced at the ketone moiety before conjugation, most drug is excreted as a conjugate in the urine. Less than 20 percent is excreted through the bile. In normal persons, at steady state with usual doses of 100 mg three times daily, the plasma half-life approximates 30 hours. Because fenofibrate is not dialyzable, it has a markedly prolonged half life in patients with renal failure and should not be used.