Avibactamavibactam ceftazidime, avibactam
Avibactam is a non-β-lactam β-lactamase inhibitor developed by Actavis now jointly with AstraZeneca A new drug application for avibactam in combination with ceftazidime branded as Avycaz 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
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 Whilst avibactam inhibits class A, class C, and, some, class D serine β-lactamases such as KPCs, AmpC, it has been reported to be a poor substrate/weak inhibitor of class B metallo-β-lactamases, such as VIM-2, VIM-4, SPM-1, BcII, NDM-1, Fez-1
- ^ "Full Prescribing Information: AVYCAZ™ ceftazidime-avibactam for Injection, for intravenous use" ©2015 Actavis All rights reserved Retrieved 1 June 2015
- ^ Wang, David Yuxin; Abboud, Martine I; Markoulides, Marios S; Brem, Jürgen; Schofield, Christopher J 2016-06-01 "The road to avibactam: the first clinically useful non-β-lactam working somewhat like a β-lactam" Future Medicinal Chemistry 8 10: 1063–1084 doi:104155/fmc-2016-0078 ISSN 1756-8919
- ^ Zhanel, GG 2013 "Ceftazidime-avibactam: a novel cephalosporin/β-lactamase inhibitor combination" Drugs 73 2: 159–77 doi:101007/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:101074/jbcM113485979 PMC 3784710 PMID 23913691
- ^ Abboud, Martine I; Damblon, Christian; Brem, Jürgen; Smargiasso, Nicolas; Mercuri, Paola; Gilbert, Bernard; Rydzik, Anna M; Claridge, Timothy D W; Schofield, Christopher J; Frère, Jean-Marie 2016-07-11 "Interaction of Avibactam with Class B Metallo-β-lactamases" Antimicrobial Agents and Chemotherapy 60: AAC00897–16 doi:101128/AAC00897-16 ISSN 0066-4804 PMC 5038302 PMID 27401561
- T Edeki; J Armstrong; J Li "Pharmacokinetics of Avibactam AVI and Ceftazidime CAZ Following Separate or Combined Administration in Healthy Volunteers" Archived from the original on 2016-03-03
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