Cilastatin is a renal dehydropeptidase inhibitor used to prevent degradation of imipenem. Both medications are used together to treat a variety of infections. Cilastatin is an inhibitor of renal dehydropeptidase, an enzyme responsible for both the metabolism of thienamycin beta-lactam antibiotics as well as conversion of leukotriene D4 to leukotriene E4.
- Mechanism
- Curator reviewed · 2 references
Cilastatin is a renal dehydropeptidase-I 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 block the metabolism of imipenem.
- Primary indication
- Cilastatin is indicated, in combination with imipenem with or without relebactam, for the treatment of bacterial infections including respiratory, skin, bone, gynecologic, urinary tract, and intra-abdominal as well as septicemia and endocarditis.Curator reviewed · 15 structured indications
- Formula / weight
- C16H26N2O5S · 358.453 g/mol (avg)
- First approval
- Canada, 2005 · United States, 1985 · European Union, 2020
- Brand names
Resolves to
DHSUYTOATWAVLW-WFVMDLQDSA-NSMILESCC1(C)C[C@@H]1C(=O)N\C(=C/CCCCSC[C@H](N)C(O)=O)C(O)=OWhat you can answer from here — as of September 12, 2026
Which drugs share a target with Cilastatin, and which of those have an active Phase 3 trial?
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