Relebactam

Relebactam is a pivotal β‑lactamase inhibitor that restores the efficacy of carbapenem antibiotics against resistant bacterial pathogens. As a diazabicyclooctane inhibitor, Relebactam exhibits activity against a wide spectrum of β‑lactamases, including class A (ESBLs and KPC) and class C (AmpC) enzymes, making it an essential component in combination therapy for complicated urinary tract infections (cUTIs), complicated intra‑abdominal infections (cIAIs), hospital‑acquired bacterial pneumonia (HABP), and ventilator‑associated bacterial pneumonia (VABP). When co‑administered with imipenem, Relebactam protects the antibiotic from enzymatic degradation, thereby extending its antibacterial spectrum to include carbapenem‑resistant Enterobacteriaceae and Pseudomonas aeruginosa. As a high‑value pharmaceutical intermediate and reference standard, Relebactam is indispensable for analytical method development, impurity profiling, and quality control testing in the manufacture of imipenem/relebactam combination products. Additionally, Relebactam serves as a critical reference material for ANDA filings and pharmacopoeial compliance testing, supporting generic manufacturers in demonstrating bioequivalence and product quality. The compound's unique diazabicyclooctane scaffold also makes Relebactam a valuable tool compound for studying β‑lactamase inhibition mechanisms and for developing next‑generation antibiotic adjuvants.

 

Product Parameters

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Parameter	Specification
Product Name	Relebactam
CAS Number	1174018-99-5
Molecular Formula	C₁₂H₂₀N₄O₆S
Molecular Weight	348.38 g/mol
Appearance	White to light yellow solid
Melting Point	>252°C (dec.)
Density	1.59 g/cm³
Solubility	DMSO (slightly), Water (slightly)
Storage Condition	Hygroscopic, −20°C freezer, under inert atmosphere

Application

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Relebactam is a novel β-lactamase inhibitor discovered and developed by Merck & Co., exhibiting activity against a broad spectrum of β-lactamases. This cyclic urea-class drug, when combined with imipenem and ciprofloxacin, has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of complicated intra-abdominal infections (cIAIs).

 

Mechanism Of Action

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Relebactam exerts its bactericidal activity by covalently binding to the serine residue at the active site of Ambler-type A, C, and D β-lactamases, thereby increasing the concentration of drug binding to penicillin-binding proteins (PBP). This mechanism poses significant challenges for this class of antibiotics in treating infections caused by multidrug-resistant Gram-negative pathogens.

 

Synthetic Route

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Contact Us

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Securing Relebactam for your antibiotic combination therapy manufacturing campaign, impurity profiling program, or antibacterial research should be straightforward. Cosperpharm makes it simple.