Description: Cilastatin is an inhibitor of dipeptidase (dehydropeptidase I), a renal dipeptidase. It inhibits human renal dipeptidase (Ki = 0.7 M), porcine dipeptidase (IC50 = 0.11 M), and bacterial metallo-lactamase CphA from A. hydrophila (IC50 = 178 M). Cilastatin (200 g/ml) protects primary porcine renal proximal tubular epithelial cells from nephrotoxicity and apoptosis induced by vancomycin (Item No. 15327). In a mouse model of systemic infection, cilastatin in combination with imipenem (Item No. 16039) protects mice from S. aureus, E. coli, and P. aeruginosa infection. Cilastatin was designed to inhibit renal metabolism of imipenem and prolong its half-life. Formulations containing cilastatin in combination with imipenem have been used to treat susceptible bacterial infections.
Cilastatin is used for treating diseases caused by polyresistant Gram-negative microorganisms and serious complex infections, including infection of S. aureus. Because of its strong activity against anaerobic bacteria, cilastatin is effective in monotherapy of intraabdominal infections. It is used for infectious diseases of the lower respiratory tract, urinarytract, gynecological infections, bacterial septicemia, and infections of the bones, skin, and so on.