General
Preferred name
CILASTATIN
Synonyms
MK0791 ()
Cilastatin (sodium) ()
MK0791 (sodium) ()
CILASTATIN SODIUM ()
Primaxin ()
Cilastatine ()
Cilastatina ()
Cilastatin sodium component of primaxin ()
Cilastatin sodium component of recarbrio ()
Cilastatin sodium salt ()
MK-791 ()
Cilastatin sodium component of mk-7655a ()
Cilastatin-15N-d3 ()
P&D ID
PD009460
CAS
82009-34-5
81129-83-1
2738376-83-3
Tags
available
drug
Approved by
PMDA
FDA
First approval
1985
Drug indication
infection
Bacterial infection
Drug Status
approved
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS
Cilastatin is a chemical compound which inhibits the human enzyme dehydropeptidase. Renal Dehydropeptidase degrades the antibiotic imipenem. Cilastatin is therefore combined intravenously with imipenem in order to protect it from dehydropeptidase and prolong its antibacterial effect. However, cilastatin in and of itself does not have any antibacterial activity.
DESCRIPTION
Cilastatin (sodium) is an adjunct to treatment with the antibacterial imipenem (PubChem CID 104838). Functions as a dipeptidase inhibitor.
(GtoPdb)
DESCRIPTION
Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 ¦ÌM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 ¦ÌM. Cilastatin is an antibacterial adjunct[1][2][3].
PRICE
33
DESCRIPTION
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. 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.
(Enamine Bioactive Compounds)
DESCRIPTION
Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase 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 increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
27
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Mcule NIBR MoA Box Subset
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
63
Molecular Weight
358.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
4
Rotatable Bonds
11
Ring Count
1
Aromatic Ring Count
0
cLogP
1.43
TPSA
129.72
Fraction CSP3
0.69
Chiral centers
2.0
Largest ring
3.0
QED
0.32
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
MOA
renal dipeptidase inhibitor
Proteasome inhibitor
Dehydropeptidase I Inhibitors
dehydropeptidase inhibitor
Target
Renal dipeptidase
antibiotic
Bacterial
Dipeptidase 1
DPEP1
Member status
member
Pathway
Microbiology/virology
Proteases/Proteasome
Ubiquitination
Anti-infection
Therapeutic Class
Antibiotics
Source data
