mk0791

Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.

Cilastatin (MK-0791) is a potent, reversible, competitive inhibitor of renal dehydropeptidase I (DHP-I), exhibiting an IC₅₀ of 0.1 μM. By inhibiting DHP-I in the kidney, Cilastatin prevents the enzymatic degradation of β-lactam antibiotics, thereby enhancing their stability and therapeutic efficacy. In addition, Cilastatin demonstrates inhibitory activity against the bacterial metallo-β-lactamase enzyme CphA, with an IC₅₀ of 178 μM. Clinically and experimentally, Cilastatin is widely used as an antibacterial adjunct to improve antibiotic performance and reduce renal metabolism of co-administered β-lactam drugs.

Cilastatin-15N,D3 is a version of Cilastatin (T2583) that is labeled with ^15N and deuterium. Cilastatin (T2583) (MK0791) acts as a reversible competitive inhibitor of renal dehydropeptidase I, with an IC50 of 0.1 μM. It inhibits the bacterial metallo-beta-lactamase CphA with an IC50 of 178 μM. Cilastatin (T2583) is utilized as an antibacterial adjunct.