Cilastatin

Renal Dehydropeptidase Inhibitor — ANTIINFECTIVES FOR SYSTEMIC USE

Key facts

Cilastatin is an ofp drug in the Renal Dehydropeptidase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 1985. Its mechanism of action is classified as Dipeptidase Inhibitors. DrugCentral lists 2 molecular targets, including DPEP1 and DPEP1. Recorded indications include Abdominal abscess, Acute exacerbation of chronic bronchitis, Bacterial endocarditis and Bacterial infection due to Klebsiella pneumoniae.

• Approval status: ofp (first approved 1985 by the FDA).
• Drug class: Renal Dehydropeptidase Inhibitor.
• Mechanism of action: Dipeptidase Inhibitors.
• Molecular targets: DPEP1 and DPEP1 (2 listed in DrugCentral).
• Indications: Abdominal abscess, Acute exacerbation of chronic bronchitis, Bacterial endocarditis, Bacterial infection due to Klebsiella pneumoniae and Bacterial pneumonia and others.
• ATC code: J01DH51 (Carbapenems).
• Molecular formula: C16H26N2O5S; molecular weight 358.46 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (29)

• Abdominal abscess
• Acute exacerbation of chronic bronchitis
• Bacterial endocarditis
• Bacterial infection due to Klebsiella pneumoniae
• Bacterial pneumonia
• Bacterial septicemia
• Bacterial urinary infection
• Diabetic Foot Infection
• Endometritis
• Enterobacter Pneumonia
• Female genital tract infection
• Gram-Negative Aerobic Bacillary Pneumonia
• Haemophilus influenzae pneumonia
• Infection caused by Acinetobacter spp resistant to carbapenem antimicrobial drugs
• Infection caused by Citrobacter spp resistant to carbapenem antimicrobial drugs
• Infection caused by Enterococcus spp resistant to carbapenem antimicrobial drugs
• Infection caused by Escherichia coli strain resistant to carbapenem antimicrobial drugs
• Infection caused by Klebsiella spp resistant to carbapenem antimicrobial drugs
• Infection caused by Pseudomonas aeruginosa strain resistant to carbapenem antimicrobial drugs
• Infection caused by Serratia spp resistant to carbapenem antimicrobial drugs
• Infection of bone
• Infection of skin AND/OR subcutaneous tissue
• Infectious disease of abdomen
• Infectious disorder of joint
• Inflammatory Disease of Female Pelvic Organs
• Lower respiratory tract infection
• Peritonitis
• Pneumonia due to Escherichia coli
• Pneumonia due to Streptococcus

Off-label uses (10)

• Anthrax
• Clostridium Perfringens Empyema
• Cutaneous anthrax
• Gas gangrene caused by clostridium perfringens
• Gastrointestinal anthrax
• Infection by Campylobacter fetus
• Inhalational anthrax
• Melioidosis
• Pseudomonas Respiratory Tract Infection in Cystic Fibrosis
• Pyrexia of unknown origin

Contraindications (4)

• Kidney disease
• Lesion of brain
• Pseudomembranous enterocolitis
• Seizure disorder

Mechanism & targets

• Mechanism of action (MoA): Dipeptidase Inhibitors
• Established pharmacologic class: Renal Dehydropeptidase Inhibitor

Molecular targets (2)

Target	Gene	Action	Activity
Dipeptidase 1	DPEP1	unknown	Ki 6.96
Dipeptidase 1	DPEP1	inhibitor	Ki 6.96

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2021-06-23	PMDA	—	MSD K.K.
1985-11-26	FDA	—	MERCK

ATC classification

ATC code	Therapeutic hierarchy
J01DH51	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIBACTERIALS FOR SYSTEMIC USE › OTHER BETA-LACTAM ANTIBACTERIALS › Carbapenems
J01DH56	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIBACTERIALS FOR SYSTEMIC USE › OTHER BETA-LACTAM ANTIBACTERIALS › Carbapenems

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Seizure	362.7
Multiple organ dysfunction syndrome	112.3
Septic shock	108.5
Generalised tonic-clonic seizure	64.9
Renal failure	64.6
Eosinophilia	53.9
Respiratory failure	50.8
Dermatitis exfoliative	49.2
Sepsis	48.8
Pseudomonas infection	48.2
Drug reaction with eosinophilia and systemic symptoms	46.8
Toxic epidermal necrolysis	46.6

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Cilastatin is on its molecule page.

• Molecular formula: C₁₆H₂₆N₂O₅S
• Molecular weight: 358.46 g/mol
• CAS number: —
• InChIKey: DHSUYTOATWAVLW-WFVMDLQDSA-N
• PubChem CID: 6435415

CC1(C)C[C@@H]1C(=O)N\C(=C/CCCCSC[C@H](N)C(O)=O)C(O)=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Cilastatin used for?

DrugCentral lists the following indications for Cilastatin: Abdominal abscess, Acute exacerbation of chronic bronchitis, Bacterial endocarditis, Bacterial infection due to Klebsiella pneumoniae, Bacterial pneumonia, Bacterial septicemia, Bacterial urinary infection and Diabetic Foot Infection and others.

How does Cilastatin work?

Cilastatin is classified as Dipeptidase Inhibitors; its molecular targets in DrugCentral include DPEP1 and DPEP1 (inhibitor).

When was Cilastatin first approved?

Cilastatin was first approved by the FDA in 1985.

What drug class does Cilastatin belong to?

Cilastatin is in the Renal Dehydropeptidase Inhibitor class.

What is the chemical formula of Cilastatin?

Cilastatin has the molecular formula C16H26N2O5S and a molecular weight of 358.46 g/mol.

Sources

• DrugCentral drug card 640 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201057 — compound record and bioactivity
• PubChem CID 6435415 — chemical identifiers
• DrugBank DB01597 — drug record
• FDA UNII 141A6AMN38 — substance identity
• DailyMed: FDA labels for Cilastatin — current prescribing information (label search)
• UniProt P16444 (DPEP1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.