Drug intelligence / Profile preview

imipenem + cilastatin + tigecycline

Development stage
Unknown
Lead developer
Ain Shams University
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination antibiotic regimen consisting of imipenem, a broad-spectrum carbapenem; cilastatin, a renal dehydropeptidase-I inhibitor; and tigecycline, a glycylcycline. Imipenem works by inhibiting bacterial cell wall synthesis through binding to penicillin-binding proteins (PBPs). Cilastatin is co-administered with imipenem to prevent its degradation by the enzyme dehydropeptidase I in the renal tubules, thereby increasing its concentration in the urinary tract and preventing potential nephrotoxicity. Tigecycline is a protein synthesis inhibitor that binds to the 30S ribosomal subunit, blocking the entry of aminoacyl-tRNA into the A site. This combination is primarily investigated for the treatment of severe infections caused by multidrug-resistant (MDR) Gram-negative bacteria, such as carbapenem-resistant Enterobacteriaceae or *Acinetobacter baumannii*, where monotherapy is often insufficient.

Other names
imipenem/cilastatin + tigecyclineimipenem-cilastatin and tigecycline
02

Targets

Bacterial RibosomeDPEP1 (Dehydropeptidase 1)PBP (Penicillin-binding protein family)

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