Ligand id: 5166

Name: cilastatin

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 7
Hydrogen bond donors 4
Rotatable bonds 12
Topological polar surface area 155.02
Molecular weight 358.16
XLogP -0.52
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
This inhibitor of dehydropeptidase-1 is administered in fixed-dose formulations with the antibiotic imipenem in order to increase its effectiveness. Commonly used formulations are Primaxin® and Tienam®.
Mechanism Of Action and Pharmacodynamic Effects
Cilastatin inhibits dehydropeptidase-I-induced hydrolysis of the antibiotic imipenem, thereby increasing its bioactivity and prolongs its antibacterial effect. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4. It has been reported to be a bacterial beta-lactamase inhibitor [2].