Cilastatin sodium

Cilastatin is a dipeptidase inhibitor that specifically inhibits DPEP1 (dehydrodipeptidase I), a renal membrane-bound glycoprotein involved in the hydrolytic metabolism of penem and carbapenem β-lactam antibiotics. Cilastatin has been shown to inhibit leukotriene D4 hydrolase in porcine kidney microvillar membranes which inhibits the conversion of leukotriene D4 to leukotriene E4. Also, Cilastatin has been used to maintain the antibiotic activity of imipenem through inhibiting dipeptidase activity. It has been reported that Cilastatin exhibits nephroprotective effects in cyclosporine A-induced nephrotoxicity in kidney proximal tubule epithelial cells and inhibits the bacterial metallo-β-lactamase, an enzyme responsible for bacterial resistance to β-lactam antibiotics.