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Imipenem, Cilastatin and Relebactam
Imipenem inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins, cilastatin protects imipenem from renal degradation, and relebactam is a beta-lactamase inhibitor that prevents bacterial resistance.
Imipenem inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins, cilastatin protects imipenem from renal degradation, and relebactam is a beta-lactamase inhibitor that prevents bacterial resistance. Used for Complicated urinary tract infections (cUTI) including pyelonephritis, Complicated intra-abdominal infections (cIAI), Hospital-acquired bacterial pneumonia (HABP) and ventilator-associated bacterial pneumonia (VABP).
At a glance
| Generic name | Imipenem, Cilastatin and Relebactam |
|---|---|
| Also known as | Recarbrio |
| Sponsor | Joseph L. Kuti, PharmD |
| Drug class | Carbapenem antibiotic with beta-lactamase inhibitor |
| Target | Penicillin-binding proteins (PBPs); beta-lactamase inhibition |
| Modality | Small molecule |
| Therapeutic area | Infectious Disease |
| Phase | FDA-approved |
Mechanism of action
Imipenem is a broad-spectrum carbapenem antibiotic that disrupts peptidoglycan cross-linking in bacterial cell walls, leading to cell lysis and death. Cilastatin is a dehydropeptidase inhibitor that prevents renal metabolism of imipenem, increasing its bioavailability. Relebactam is a non-beta-lactam beta-lactamase inhibitor that protects imipenem from degradation by bacterial beta-lactamases, extending its spectrum to include beta-lactamase-producing organisms.
Approved indications
- Complicated urinary tract infections (cUTI) including pyelonephritis
- Complicated intra-abdominal infections (cIAI)
- Hospital-acquired bacterial pneumonia (HABP) and ventilator-associated bacterial pneumonia (VABP)
Common side effects
- Nausea
- Diarrhea
- Headache
- Phlebitis at injection site
- Seizures (rare, dose-dependent)
Key clinical trials
- Safety, Tolerability, Efficacy and Pharmacokinetics of Imipenem/Cilastatin/Relebactam (MK-7655A) in Pediatric Participants With Gram-negative Bacterial Infection (MK-7655A-021) (PHASE2, PHASE3)
- Imipenem/Cilastatin-XNW4107 Versus Imipenem/Cilastatin/Relebactam for Treatment of Participants With Bacterial Pneumonia (XNW4107-302, REITAB-2) (PHASE3)
- Imipenem/Cilastatin/Relebactam (MK-7655A) Versus Piperacillin/Tazobactam in Participants With Hospital-Acquired or Ventilator-Associated Bacterial Pneumonia (MK-7655A-016) (PHASE3)
- Imipenem/Cilastatin/Relebactam Pharmacokinetics, Safety, and Outcomes in Adults and Adolescents With Cystic Fibrosis (PHASE4)
- Impact of Obesity on the Pharmacokinetics of Imipenem-Relebactam in ICU Patients (PHASE4)
- PHASE II SINGLE-CENTER, RANDOMIZED, OPEN-LABEL, PROSPECTIVE, STUDY TO DETERMINE THE IMPACT OF SERIAL PROCALCITONIN (PHASE2)
- Imipenem/Cilastatin/Relebactam (IMI/REL) in Treatment of CRE Infections (PHASE4)
- Imipenem/Cilastatin/Relebactam PK in ECMO (PHASE1)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |