Avibactam
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| Systematic (IUPAC) name | |
|---|---|
|
[(2S,5R)-2-Carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] hydrogen sulfate | |
| Clinical data | |
| Trade names | Avycaz (formulated with ceftazidime) |
| Pregnancy category |
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| Routes of administration | IV |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 100% (intravenous) |
| Protein binding | 5.7–8.2%[1] |
| Metabolism | Nil |
| Onset of action | Increases in proportion to dose |
| Excretion | Renal (97%) |
| Identifiers | |
| CAS Number | 1192500-31-4 |
| ATC code | None |
| PubChem | CID 9835049 |
| ChemSpider | 8010770 |
| KEGG | D10340 |
| ChEBI |
CHEBI:85984  |
| ChEMBL | CHEMBL1689063 |
| Chemical data | |
| Formula | C7H11N3O6S |
| Molar mass | 265.24 g/mol |
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Avibactam is a non-β-lactam β-lactamase inhibitor antibiotic developed by Actavis (now Allergan) jointly with AstraZeneca. A new drug application for avibactam in combination with ceftazidime was approved by the FDA on February 25, 2015, for treating complicated urinary tract (cUTI) and complicated intra-abdominal infections (cIAI) caused by antibiotic resistant-pathogens, including those caused by multi-drug resistant Gram-negative bacterial pathogens.[2][3][4]
Increasing resistance to cephalosporins among Gram-(−) bacterial pathogens, especially among hospital-acquired infections, results in part from the production of β-lactamase enzymes that deactivate these antibiotics. While the co-administration of a β-lactamase inhibitor can restore antibacterial activity to the cephalosporin, previously approved β-lactamase inhibitors such as tazobactam and clavulanic acid do not inhibit important classes of β-lactamases, including Klebsiella pneumoniae carbapenemases (KPCs), New Delhi metallo-β-lactamase 1 (NDM-1), and AmpC-type β-lactamases. Avibactam inhibits KPCs, AmpC, and some Class D β-lactamases, but is not active against NDM-1.[5]
References
- ↑ "Full Prescribing Information: AVYCAZ™ (ceftazidime-avibactam) for Injection, for intravenous use". ©2015 Actavis. All rights reserved. Retrieved 1 June 2015.
- ↑ Zhanel, GG (2013). "Ceftazidime-avibactam: a novel cephalosporin/β-lactamase inhibitor combination". Drugs 73 (2): 159-77. doi:10.1007/s40265-013-0013-7. PMID 23371303.
- ↑ "Actavis Announces FDA Acceptance of the NDA Filing for Ceftazidime-Avibactam, a Qualified Infectious Disease Product". Actavis—a global, integrated specialty pharmaceutical company—Actavis. Actavis plc. Retrieved 1 June 2015.
- ↑ Ehmann, DE; Jahic, H; Ross, PL; Gu, RF; Hu, J; Durand-Réville, TF; Lahiri, S; Thresher, J; Livchak, S; Gao, N; Palmer, T; Walkup, GK; Fisher, SL (2013). "Kinetics of Avibactam Inhibition against Class A, C, and D β-Lactamases". The Journal of Biological Chemistry 288 (39): 27960–71. doi:10.1074/jbc.M113.485979. PMC: 3784710. PMID 23913691.
- ↑ "www.accessdata.fda.gov" (PDF).
External links
- T. Edeki, J. Armstrong, J. Li. "Pharmacokinetics of Avibactam (AVI) and Ceftazidime (CAZ) Following Separate or Combined Administration in Healthy Volunteers".
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