Avibactam

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Avibactam
Clinical data
Trade namesAvycaz (formulated with ceftazidime)
Routes of
administration		Intravenous therapy
ATC code
  • None
Legal status
Legal status
Pharmacokinetic data
Bioavailability100% (intravenous)
Protein binding5.7–8.2%[1]
MetabolismNil
Onset of actionIncreases in proportion to dose
ExcretionKidney (97%)
Identifiers
  • [(2S,5R)-2-Carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] hydrogen sulfate
JSmol)
  • [C@]12C[N@]([C@@H](CC1)C(N)=O)C(=O)N2OS(O)(=O)=O
  • InChI=1S/C7H11N3O6S/c8-6(11)5-2-1-4-3-9(5)7(12)10(4)16-17(13,14)15/h4-5H,1-3H2,(H2,8,11)(H,13,14,15)/t4-,5+/m1/s1
  • Key:NDCUAPJVLWFHHB-UHNVWZDZSA-N

Avibactam is a non-

antibiotic resistant-pathogens, including those caused by multi-drug resistant Gram-negative bacterial pathogens.[3][4][5]

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 (KPCs, CTX-M, TEM, SHV), class C (AmpC), and, some, class D serine β-lactamases (such as OXA-23, OXA-48), 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.[6]

For infections sustained by metallo-β-lactamases producing bacteria, a therapeutic strategy consists in administering avibactam as companion drug administered alongside aztreonam. In fact, although in theory aztreonam is not hydrolyzed by metallo-β-lactamases, many metallo-β-Lactamases-producing strains co-produce enzymes that could hydrolyze aztreonam (e.g. AmpC, ESBL), therefore avibactam is given to protect aztreonam exploiting its robust β-lactamases inhibition.[7] Avibactam is available in a combination with aztreonam (aztreonam/avibactam).

References

  1. ^ "Full Prescribing Information: Avycaz (ceftazidime-avibactam) for Injection, for intravenous use". ©2015 Actavis. All rights reserved. Archived from the original on 2 June 2015. Retrieved 1 June 2015.
  2. PMID 27327972
    .
  3. S2CID 32700350
    .
  4. ^ "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. Archived from the original on 27 May 2015. Retrieved 1 June 2015.
  5. PMID 23913691
    .
  6. PMID 27401561
    .
  7. PMID 34439062
    .

Further reading

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