Synopsis
Synopsis
0
USDMF
0
CEP/COS
0
JDMF
0
EU WC
0
KDMF
0
VMF
0
API
0
FDF
0
Europe
0
Canada
0
Australia
0
South Africa
0
Listed Dossiers
DRUG PRODUCT COMPOSITIONS
0
EDQM
0
USP
0
JP
0
Others
0
Data Compilation #PharmaFlow
0
Stock Recap #PipelineProspector
0
Weekly News Recap #Phispers
US Medicaid
NA
Annual Reports
NA
Finished Drug Prices
NA
1. (2s,5r)-7-oxo-n-(4-piperidinyl)-6-(sulfooxy)-1,6-diazabicyclo(3.2.1)octane-2-carboxamide
2. Mk-7655
3. Mk7655
4. Relebactam Anhydrous
1. 1174018-99-5
2. Mk-7655
3. Relebactam Anhydrous
4. Relebactam [inn]
5. (-)-relebactam Anhydrous
6. 1oqf7tt3pf
7. Chembl3112741
8. Mk-7655a
9. Mk7655
10. Sulfuric Acid Mono-((2s,5r)-7-oxo-2-(piperidin-4-ylcarbamoyl)-1,6-diaza-bicyclo(3.2.1)oct-6-yl) Ester
11. (1r,2s,5r)-7-oxo-2-(piperidin-4-ylcarbamoyl)-1,6-diazabicyclo[3.2.1]octan-6-yl Hydrogen Sulfate
12. [(2s,5r)-7-oxo-2-(piperidin-4-ylcarbamoyl)-1,6-diazabicyclo[3.2.1]octan-6-yl] Hydrogen Sulfate
13. Unii-1oqf7tt3pf
14. Relebactam [mi]
15. Relebactam [who-dd]
16. Bdbm1858
17. Schembl3721178
18. Gtpl10852
19. Ex-a864
20. Sulfuric Acid Mono-[7-oxo-2-(piperidin-4-ylcarbamoyl)-1,6-diaza-bicyclo[3.2.1]oct-6-yl] Ester
21. Bdbm50447651
22. Mfcd28502833
23. Zinc43206319
24. Cs-5391
25. Db12377
26. Ac-36163
27. As-35205
28. Br163749
29. Hy-16752
30. Us8487073, 1a
31. S0074
32. J3.628.086g
33. Mk-7655;mk7655;mk 7655
34. J-690043
35. Q27252695
36. (2s,5r)-7-oxo-n-piperidin-4-yl-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide
| Molecular Weight | 348.38 g/mol |
|---|---|
| Molecular Formula | C12H20N4O6S |
| XLogP3 | -3.6 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 4 |
| Exact Mass | 348.11035554 g/mol |
| Monoisotopic Mass | 348.11035554 g/mol |
| Topological Polar Surface Area | 137 Ų |
| Heavy Atom Count | 23 |
| Formal Charge | 0 |
| Complexity | 585 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 2 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
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.
Relebactam prevents the hydrolysis of [imipenem], allowing it to exert its bactericidal effect.
beta-Lactamase Inhibitors
Endogenous substances and drugs that inhibit or block the activity of BETA-LACTAMASES. (See all compounds classified as beta-Lactamase Inhibitors.)
Absorption
Currently, relebactam is only available as an intravenous product; therefore, there is no relevant absorption data in the literature.
Route of Elimination
Approximately 90-100% of relebactam is renally eliminated.
Volume of Distribution
Relebactam has a volume of distribution of approximately 19 L with both single and steady state dosing.
Clearance
Relebactam has a reported total clearance of approximately 130-150 mL/min (8 L/h). About 30% of the total drug clearance can be attributed to active tubular secretion.
Relebactam does not undergo significant metabolism and can be found mostly unchanged in human plasma.
Relebactam has a half-life of 1.2 hours as per official FDA labeling. Values reported in pharmacokinetic studies vary from 1.35-1.8 hours.
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.
API SUPPLIERS
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]
NDC API
Fareva is a one-stop-shop for API/HPAPI, OSD & Sterile products, is USFDA, EMA and PMDA-inspected and has multiple NDA & ANDA filings.
NDC Package Code : 24823-154
Start Marketing Date : 2019-01-02
End Marketing Date : 2024-12-31
Dosage Form (Strength) : POWDER (1kg/kg)
Marketing Category : BULK INGREDIENT FOR HUMAN P...
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Listed Suppliers
About the Company : Almelo are the industry leaders in manufacturing advanced intermediates, Active Pharmaceutical Ingredients (APIs) and specialty fine chemicals. With a diverse product portfolio cou...
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Drugs in Development
Details:
FDA has approved sNDA for RECARBRIO (imipenem, cilastatin, and relebactam) for the treatment of patients 18 years of age and older with hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia (HABP/VABP).
Lead Product(s): Imipenem,Cilastatin,Relebactam
Therapeutic Area: Infections and Infectious Diseases Brand Name: Undisclosed
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable June 05, 2020
Lead Product(s) : Imipenem,Cilastatin,Relebactam
Therapeutic Area : Infections and Infectious Diseases
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : FDA has approved sNDA for RECARBRIO (imipenem, cilastatin, and relebactam) for the treatment of patients 18 years of age and older with hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia (HABP/VABP).
Brand Name : Undisclosed
Molecule Type : Small molecule
Upfront Cash : Not Applicable
June 05, 2020
Details:
The results demonstrated noninferiority of RECARBRIO compared to piperacillin and tazobactam (PIP/TAZ), in the primary and key secondary endpoints of the study.
Lead Product(s): Imipenem,Cilastatin,Relebactam
Therapeutic Area: Infections and Infectious Diseases Brand Name: Undisclosed
Study Phase: Phase IIIProduct Type: Small molecule
Sponsor: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable May 06, 2020
Lead Product(s) : Imipenem,Cilastatin,Relebactam
Therapeutic Area : Infections and Infectious Diseases
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Results of Phase 3 Trial Evaluating the Efficacy and Safety of Merck’s RECARBRIO Vs Piperacillin...
Details : The results demonstrated noninferiority of RECARBRIO compared to piperacillin and tazobactam (PIP/TAZ), in the primary and key secondary endpoints of the study.
Brand Name : Undisclosed
Molecule Type : Small molecule
Upfront Cash : Not Applicable
May 06, 2020
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]INTERMEDIATES SUPPLIERS
Tagoor's product development expertise, backed by our comprehensive understanding of the processes, helps us offer high-quality APIs.
CAS Number : 73874-95-0
End Use API : Relebactam
About The Company : Tagoor Laboratories, established in 2018, is a part of the Tagoor Group. It specializes in providing APIs, advanced intermediates and key starting materials for...
Tagoor's product development expertise, backed by our comprehensive understanding of the processes, helps us offer high-quality APIs.
CAS Number : 13035-19-3
End Use API : Relebactam
About The Company : Tagoor Laboratories, established in 2018, is a part of the Tagoor Group. It specializes in providing APIs, advanced intermediates and key starting materials for...
Tagoor's product development expertise, backed by our comprehensive understanding of the processes, helps us offer high-quality APIs.
CAS Number : 87120-72-7
End Use API : Relebactam
About The Company : Tagoor Laboratories, established in 2018, is a part of the Tagoor Group. It specializes in providing APIs, advanced intermediates and key starting materials for...
Benzyl (2S,5R)-5- [(Benzyloxy)Amino] Piperidine- 2...
CAS Number : CAS-1171080-45-7
End Use API : Relebactam
About The Company : Almelo are the industry leaders in manufacturing advanced intermediates, Active Pharmaceutical Ingredients (APIs) and specialty fine chemicals. With a diverse p...
CAS Number : 87120-72-7
End Use API : Relebactam
About The Company : Saptagir Laboratories Private incorporated in 2016, is a manufacturer and supplier of Active Pharmaceutical Ingredients (APIs) and Intermediates for a wide rang...
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Digital Content
NEWS #PharmaBuzz
Patents & EXCLUSIVITIES
ABOUT THIS PAGE
LOOKING FOR A SUPPLIER?
