THERAPY DOSSIER · th-b688c0489b7a

Cilastatin

Drug · Renal dehydropeptidase-I inhibitor; protects imipenem from renal metabolism.

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Evidence & regulatory context

Mechanism: Renal dehydropeptidase-I inhibitor; protects imipenem from renal metabolism.
Target: CHEMBL1989 (Renal dipeptidase)
Injury models: Chemical/toxin
Reported indication: Approved only in fixed combination with imipenem (imipenem/cilastatin) - cilastatin is a renal dehydropeptidase-I inhibitor that protects imipenem from renal metabolism; the antibacterial combination treats serious bacterial infections
First approval: 1985
Development stage: Approved as imipenem adjuvant (antibiotic combination); standalone nephroprotection for AKI is investigational (PONTiAK ongoing)
ChEMBL record: CHEMBL766 ↗
ChEMBL max phase: 4 / 4 (development scale, not regulatory approval)
Synonyms: Primaxin (with imipenem)
Note: Not recorded

Clinical trials 4

1 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.

NCT06886464 ↗Injury indicationPHASE2recruiting

PONTiAK: Cilastatin to Prevent Nephrotoxin-Induced Acute Kidney Injury

Acute Kidney Injury

Enrolment: 698 · Results not recorded

NCT05561764 ↗PHASE4terminated

Imipenem/Cilastatin/Relebactam in CF Pulmonary Exacerbations

Cystic Fibrosis · Pneumonia, Bacterial

Enrolment: 4 · Results not recorded

NCT02452047 ↗PHASE3completed

Imipenem/Cilastatin/Relebactam vs Colistimethate+Imipenem/Cilastatin

Bacterial Infections

Enrolment: 50 · Results not recorded

NCT03230916 ↗PHASE1completed

MK-7655A (Imipenem/Cilastatin/Relebactam) in Pediatric Gram-neg Infections

Gram-negative Bacterial Infection

Enrolment: 47 · Results not recorded

Preclinical evidence 1

1 studies reported at therapy level; 1 evidence entries itemised.

PMID 32899204 ↗2020Reported benefit

Nephroprotective Effect of Cilastatin against Gentamicin-Induced Renal Injury In Vitro and In Vivo without Altering Its Bactericidal Efficiency.

RatChemical/toxinWistarmalen = 28 rats in 4 groups: untreated control n = 6, cilastatin n…intraperitonealCilastatin 150 mg/kg (0.5 mL/kg); gentamicin 80 mg/kg (5 mL…Cilastatin given immediately before each gentamicin dose, from the first gentam…

Model: Gentamicin-induced acute kidney injury (gentamicin 80 mg/kg), with porcine renal cells in vitro

Cilastatin decreased creatinine, blood urea nitrogen, kidney injury molecule-1 and severe morphological changes caused by gentamicin, reduced megalin expression, gentamicin uptake and myeloid body formation, and lowered apoptotic, oxidative and inflammatory markers without preventing gentamicin bac…

Extraction: extract · Supplied extraction confidence: 0.92. Machine-extracted fields require source verification.

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