Cilastatin

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{{drugbox | IUPAC_name = (Z)-7-[(2S)-2-amino-3-hydroxy-3-oxopropyl]sulfanyl-2-{[(1S)-
2,2-dimethylcyclopropanecarbonyl]amino}hept-2-enoic acid | image = Cilastatin.svg | CAS_number = 82009-34-5 | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 5280454 | DrugBank = EXPT00918 | C=16|H=26|N=2|O=5|S=1 | molecular_weight = 358.454 g/mol | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_UK = | legal_US = | legal_status = | routes_of_administration = }} Cilastatin is a chemical compound which inhibits the human enzyme dehydropeptidase. [1]

Dehydropeptidase is found in the kidney and is responsible for degrading 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.

References

  1. Keynan S, Hooper NM, Felici A, Amicosante G, Turner AJ (1995). "The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterial metallo-beta-lactamase enzyme CphA". Antimicrob. Agents Chemother. 39 (7): 1629–31. PMID 7492120.

See also


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