Cilastatin

Overview

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. Since the antibiotic, imipenem, is one such antibiotic that is hydrolyzed by dehydropeptidase, cilastatin is used in combination with imipenem to prevent its metabolism. The first combination product containing both drugs was approved by the FDA in November of 1985 under the trade name Primaxin, marketed by Merck & Co. A newer triple-drug product was approved in July 2019 under the trade name Recarbrio which also contains relebactam.

Background

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.

Associated Conditions

Bacterial Septicemia
Bone and Joint Infections
Complicated Intra-Abdominal Infections (cIAIs)
Complicated Urinary Tract Infection
Endocarditis caused by staphylococcus aureus
Gynecological Infection
Intraabdominal Infections
Lower respiratory tract infection bacterial
Neutropenic Fever
Pyelonephritis
Skin and Subcutaneous Tissue Bacterial Infections
Surgical Site Infections
Uncomplicated Urinary Tract Infections
Hepatic abscess

Clinical Trials

Title	Posted	Study ID	Phase	Status	Sponsor
Prevention of Nephrotoxin-Induced Acute Kidney Injury Using Cilastatin	2025/03/20	NCT06886464	Phase 2	Not yet recruiting	Matthew James
Safety, Tolerability, Efficacy and Pharmacokinetics of Imipenem/Cilastatin/Relebactam (MK-7655A) in Pediatric Participants With Gram-negative Bacterial Infection (MK-7655A-021)	2019/05/31	NCT03969901	Phase 2	Completed	Merck Sharp & Dohme LLC
Safety, Tolerability and Pharmacokinetic Profile of an Infusion of Cilastatin in Healthy Volunteers.	2018/07/23	NCT03595189	Phase 1	Completed	Spherium Biomed
Imipenem/Relebactam/Cilastatin Versus Piperacillin/Tazobactam for Treatment of Participants With Bacterial Pneumonia (MK-7655A-014)	2015/07/09	NCT02493764	Phase 3	Completed	Merck Sharp & Dohme LLC
Study Evaluating Tigecycline Versus Imipenem/Cilastatin in Hospital-Acquired Pneumonia	2004/04/07	NCT00080496	Phase 3	Completed	Wyeth is now a wholly owned subsidiary of Pfizer

FDA Drug Approvals

Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
Imipenem and Cilastatin	Fresenius Kabi USA, LLC	63323-349	INTRAVENOUS	250 mg in 20 mL	8/31/2020
PRIMAXIN IV	Merck Sharp & Dohme LLC	0006-3551	INTRAVENOUS	250 mg in 100 mL	5/24/2022
Imipenem and Cilastatin	Fresenius Kabi USA, LLC	63323-322	INTRAVENOUS	500 mg in 20 mL	8/31/2020
RECARBRIO	Merck Sharp & Dohme LLC	0006-3856	INTRAVENOUS	500 mg in 100 mL	5/5/2022
Imipenem and Cilastatin	Fresenius Kabi USA, LLC	63323-322	INTRAVENOUS	500 mg in 20 mL	11/1/2020
Imipenem and Cilastatin	Fresenius Kabi USA, LLC	63323-349	INTRAVENOUS	250 mg in 20 mL	8/31/2020
Imipenem and Cilastatin	Fresenius Kabi USA, LLC	63323-349	INTRAVENOUS	250 mg in 20 mL	11/1/2020
PRIMAXIN IV	Merck Sharp & Dohme LLC	0006-3516	INTRAVENOUS	500 mg in 100 mL	5/24/2022
Imipenem and Cilastatin	Fresenius Kabi USA, LLC	63323-322	INTRAVENOUS	500 mg in 20 mL	8/31/2020
PRIMAXIN IV	Merck Sharp & Dohme LLC	0006-3552	INTRAVENOUS	500 mg in 100 mL	5/24/2022

EMA Drug Approvals

Approved Product	Authorization Holder	Status	Issued Date
Recarbrio	Merck Sharp & Dohme B.V.,Waarderweg 39,2031 BN Haarlem,The Netherlands	Authorised	2/13/2020

HSA Drug Approvals

Approved Product	Manufacturer	Approval Number	Dosage Form	Strength	Approval Date
Imipenem + Cilastatin Mevon Powder for solution for Injection 500 mg + 500 mg	ACS DOBFAR S.p.A (Filling of Drug product sterile bulk), ACS Dobfar S.p.A. 2: Addetta Plant (Drug product bulk)	SIN14329P	INJECTION, POWDER, FOR SOLUTION	500mg	3/20/2013
IMIPENEM /CILASTATIN KABI POWDER FOR SOLUTION FOR INFUSION 500MG/500MG	ACS Dobfar S.p.A (primary and secondary packager), ACS Dobfar SpA (sterile bulk blend)	SIN14765P	INJECTION, POWDER, FOR SOLUTION	500mg/ vial	3/26/2015
Imipenem/Cilastatin Labatec IV powder for Injection 500mg/500mg	ACS Dobfar S.p.A, ACS Dobfar SpA (Intermediate)	SIN14589P	INJECTION, POWDER, FOR SOLUTION	500mg	8/13/2014
IMCIL POWDER FOR SOLUTION FOR INJECTION OR INFUSION 500MG/500MG PER VIAL	ANFARM HELLAS S.A., ACS DOBFAR S.P.A (DP INTERMEDIATE)	SIN16280P	INJECTION, POWDER, FOR SOLUTION	500mg	7/21/2021

NMPA Drug Approvals

Approved Product	Company	Approval Number	Drug Type	Dosage Form	Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product	Registration No.	Company	Licence No.	Strength	Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product	ARTG ID	Sponsor	Registration Type	Status	Registration Date
No TGA approvals found for this drug.

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