relebactam
Trade name: Recarbrio
Approved
Jul 16, 2019
Relebactum sodium (MK-7655) is a piperidine analog 3 that inhibits class A and C β-lactamases (in vitro). It is being investigated for use in treatment of infectious diseases, such as treatment of gram-negative bacterial infections. Its potential as an alternative to existing medicines in the treatment of drug-resistant bacterial infections is being studied. Clinical trials have been conducted and are still ongoing to evaluate the efficacy and safety of relebactum sodium in treatment of intra-abdominal infections, urinary tract infections (such as pyelonephritis), hospital-acquired and ventilator-associated bacterial pneumonias, and gram-negative bacterial infections. — NCATS
Clinical trial activity
16 trials · 11 clinical orgs · 1 marketing orgs
Earliest trial started Jan 1, 2011 (NCT01275170)
Timeline
2010s
Indications
Approved for
Studied for
- Bacterial Infections · Phase 4
- Carbapenems · Phase 4
- Communicable Diseases · Phase 1
- Critical Illness · Phase 4
- Cystic Fibrosis · Phase 4
- Gram-Negative Bacterial Infections · Phase 4
- Healthcare-Associated Pneumonia · Phase 3
- Intraabdominal Infections · Phase 2
- Lymphoma · Phase 2
- Neoplasms · Phase 2
- Obesity · Phase 4
- Pneumonia, Bacterial · Phase 4
- Pneumonia, Ventilator-Associated · Phase 3
- Pyelonephritis · Phase 2
- Sepsis · Phase 1
- Urinary Tract Infections · Phase 3
- Ventilators, Mechanical · Phase 3
Mechanism of action
Carbapenem-hydrolyzing beta-lactamase KPC inhibitor
Relebactam is used in combination with the beta-lactam antibacterial imipenem and protects imipenem from degradation by certain bacterial beta-lactamases. Relebactam itself has no antibacterial activity.
Inhibits serine beta lactamases (SHV, TEM, CTX-M type and Enterobacter cloacae P99, Pseudomonase derived cephalosporinase PDC and Klebsiella pneumoniae carbapenemase KPC). Not active against MBLs, some oxacillinases and certain GES allelles. Can restore the activity of imipenem/cilastatin combinations against KPC-producing Enterobacteriaceae and PDC-producing Pseudomonas aeruginosa.
- Beta-lactamaseINHIBITOR
Beta-lactamase inhibitor
Relebactam is used in combination with the beta-lactam antibacterial imipenem and protects imipenem from degradation by certain bacterial beta-lactamases. Relebactam itself has no antibacterial activity.
Inhibits serine beta lactamases (SHV, TEM, CTX-M type and Enterobacter cloacae P99, Pseudomonase derived cephalosporinase PDC and Klebsiella pneumoniae carbapenemase KPC). Not active against MBLs, some oxacillinases and certain GES allelles. Can restore the activity of imipenem/cilastatin combinations against KPC-producing Enterobacteriaceae and PDC-producing Pseudomonas aeruginosa.
- Beta-lactamaseINHIBITOR
Beta-lactamase inhibitor
Relebactam is used in combination with the beta-lactam antibacterial imipenem and protects imipenem from degradation by certain bacterial beta-lactamases. Relebactam itself has no antibacterial activity.
Inhibits serine beta lactamases (SHV, TEM, CTX-M type and Enterobacter cloacae P99, Pseudomonase derived cephalosporinase PDC and Klebsiella pneumoniae carbapenemase KPC). Not active against MBLs, some oxacillinases and certain GES allelles. Can restore the activity of imipenem/cilastatin combinations against KPC-producing Enterobacteriaceae and PDC-producing Pseudomonas aeruginosa.
- Beta-lactamase SHV-1INHIBITOR
Beta-lactamase SHV-1 inhibitor
Relebactam is used in combination with the beta-lactam antibacterial imipenem and protects imipenem from degradation by certain bacterial beta-lactamases. Relebactam itself has no antibacterial activity.
Inhibits serine beta lactamases (SHV, TEM, CTX-M type and Enterobacter cloacae P99, Pseudomonase derived cephalosporinase PDC and Klebsiella pneumoniae carbapenemase KPC). Not active against MBLs, some oxacillinases and certain GES allelles. Can restore the activity of imipenem/cilastatin combinations against KPC-producing Enterobacteriaceae and PDC-producing Pseudomonas aeruginosa.
- Beta-lactamase CTX-MINHIBITOR
Beta-lactamase CTX-M inhibitor
Relebactam is used in combination with the beta-lactam antibacterial imipenem and protects imipenem from degradation by certain bacterial beta-lactamases. Relebactam itself has no antibacterial activity.
Inhibits serine beta lactamases (SHV, TEM, CTX-M type and Enterobacter cloacae P99, Pseudomonase derived cephalosporinase PDC and Klebsiella pneumoniae carbapenemase KPC). Not active against MBLs, some oxacillinases and certain GES allelles. Can restore the activity of imipenem/cilastatin combinations against KPC-producing Enterobacteriaceae and PDC-producing Pseudomonas aeruginosa.
- Bacterial beta-lactamase TEMINHIBITOR
Bacterial beta-lactamase TEM inhibitor
Relebactam is used in combination with the beta-lactam antibacterial imipenem and protects imipenem from degradation by certain bacterial beta-lactamases. Relebactam itself has no antibacterial activity.
Inhibits serine beta lactamases (SHV, TEM, CTX-M type and Enterobacter cloacae P99, Pseudomonase derived cephalosporinase PDC and Klebsiella pneumoniae carbapenemase KPC). Not active against MBLs, some oxacillinases and certain GES allelles. Can restore the activity of imipenem/cilastatin combinations against KPC-producing Enterobacteriaceae and PDC-producing Pseudomonas aeruginosa.
- Beta-lactamaseANTAGONIST
bcl1 antagonist
Combination products
recarbrio
with cilastatin, imipenem
Also known as imipenem, cilastatin and relebactam, imipenem/cilastatin/relebactam
Approval history
- approvedPriority reviewFast trackJul 16, 2019
Chemistry & pharmacology
SMILES
O=C(NC1CCNCC1)[C@@H]1CC[C@@H]2CN1C(=O)N2OS(=O)(=O)O- Mol. weight
- 348.38 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Prescription Only
Oral
No
Parenteral
Yes
Topical
No
Sources
- ChEMBLCHEMBL3112741 ↗
- WikipediaRelebactam ↗
- NCATS1OQF7TT3PF ↗
- ChEMBLCHEMBL3301605 ↗
Also known as
- mk-7655
- mk-7655
- mk-7655
- relebactam
- relebactam
- relebactam
- relebactam
- relebactam
- relebactam anhydrous
- relebactam anhydrous
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05561764 | Phase 4 | Dec 31, 2022 | Indiana University, Merck, Q2 solutions, The University of Texas, Dallas, University of Connecticut, University of Pittsburgh |
| NCT05204563 | Phase 3 | Mar 31, 2022 | Sinovent Pty Ltd. |
| NCT05146154 | Phase 4 | Jan 31, 2022 | Merck, University of Illinois at Chicago |
| NCT04983901 | Phase 2 | Sep 14, 2021 | University of Texas at Houston |
| NCT04785924 | Phase 4 | Jun 7, 2021 | Merck, University of Florida |
| NCT04493151 | Phase 1 | Sep 1, 2020 | Hartford Hospital, Merck, University of Connecticut |
| NCT04147221 | Phase 1 | Jan 31, 2020 | Merck, University of Connecticut |
| NCT03969901 | Phase 2/Phase 3 (Phase 3) | Oct 21, 2019 | Merck |
| NCT03583333 | Phase 3 | Sep 18, 2018 | Merck |
| NCT03230916 | Phase 1 | Nov 6, 2017 | Merck |
| NCT03293485 | Phase 3 | Oct 4, 2017 | Merck |
| NCT02493764 | Phase 3 | Nov 24, 2015 | Merck |
| NCT02452047 | Phase 3 | Aug 21, 2015 | Merck |
| NCT01506271 | Phase 2 | Jun 1, 2012 | Merck |
| NCT01505634 | Phase 2 | May 1, 2012 | Merck |
| NCT01275170 | Phase 1 | Jan 1, 2011 | Merck |
Organizations
Research & Development (11)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 14 | 9 | 4 | 2011 |
| University of Connecticut | Academic/Hospital | 3 | 2 | 2 | 2020 |
| Hartford Hospital | Academic/Hospital | 1 | 1 | 1 | 2020 |
| Indiana University | Academic/Hospital | 1 | 0 | 1 | 2022 |
| Q2 solutions | For profit | 1 | 0 | 1 | 2022 |
| Sinovent Pty Ltd. | For profit | 1 | 1 | 1 | 2022 |
| The University of Texas, Dallas | Academic/Hospital | 1 | 0 | 1 | 2022 |
| University of Florida | Academic/Hospital | 1 | 1 | 1 | 2021 |
| University of Illinois at Chicago | Academic/Hospital | 1 | 1 | 1 | 2022 |
| University of Pittsburgh | Academic/Hospital | 1 | 0 | 1 | 2022 |
| University of Texas at Houston | Academic/Hospital | 1 | 1 | 1 | 2021 |