We studied the elimination of sulfisoxazole in eight renal transplant patients. The patients received sulfisoxazole prophylactically for urinary tract infection commencing 7 days postoperatively. The renal elimination of sulfisoxazole (unbound renal clearance) was decreased in this patient population and was highly correlated with creatinine clearance. The unbound metabolic clearance and apparent unbound formation clearance of N4-acetyl sulfisoxazole did not differ from values found in healthy volunteers. The protein binding was marginally lower in this patient population than in healthy subjects after a single dose. The reduced binding was compatible with a reduced albumin concentration. In contrast to the situation for healthy subjects, the binding of sulfisoxazole decreased upon multiple dosing. This is probably due to a relatively higher sulfisoxazole and N4-acetyl sulfisoxazole-to-albumin ratio in this patient population than in healthy subjects. No complications of sulfisoxazole therapy were seen, although in three subjects concentration of the N4-acetyl sulfisoxazole in urine exceeded its theoretical solubility on a few occasions.