Cilastatin

Cilastatin is a renal dehydropeptidase-I inhibitor. Its main function is to protect β-lactam antibiotics such as imipenem from renal metabolism and inactivation, so it is used almost exclusively in combination with imipenem. Dehydropeptidase-I is an enzyme located on the brush border of the renal proximal tubule and can hydrolyze antibiotics containing a β-lactam ring, especially imipenem. When imipenem is given alone, a substantial portion is degraded and inactivated in the kidney by dehydropeptidase-I. Cilastatin reversibly inhibits dehydropeptidase-I activity, allowing imipenem to retain its therapeutic effect.