Relebactam is a beta-lactamase inhibitor used to prevent hydrolysis of beta-lactam antibiotics, leading to increased effectiveness. Relebactam is a diazabicyclooctane beta-lactamase inhibitor, similar in structure to avibactam.
- Mechanism
- Curator reviewed · 4 references
Relebactam is a beta-lactamase inhibitor known to inhibit many types of beta-lactamases including Ambler class A and Ambler class C enzymes, helping to prevent imipenem from degrading in the body. Similar to the structurally-related avibactam, first, relebactam binds non-covalently to a beta-lactamase binding site, then, it covalently acylates the serine residue in the active site of the enzyme. In contrast to some other beta-lactamase inhibitors, once relebactam de-acylates from the active site, it can reform it's 5 membered ring and is capable of rebinding to target enzymes.
- Primary indication
- Relebactam is indicated in combination with imipenem and cilastatin for the treatment of complicated urinary tract infections (including pyelonephritis), and complicated intra-abdominal infections caused by susceptible organisms in adults.Curator reviewed · 3 structured indications
- Formula / weight
- C12H20N4O6S · 348.37 g/mol (avg)
- First approval
- Canada, 2026 · United States, 2020 · European Union, 2020
- Code names
- MK-7655
- Brand names
Resolves to
SMOBCLHAZXOKDQ-ZJUUUORDSA-NSMILESOS(=O)(=O)ON1[C@H]2C[N@]([C@@H](CC2)C(=O)NC2CCNCC2)C1=OWhat you can answer from here — as of August 30, 2026
Which drugs share a target with Relebactam, and which of those have an active Phase 3 trial?
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