Avibactam (sodium dihydrate)

Avibactam sodium (NXL-104) dihydrate is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively^[1]. IC50 & Target: IC₅₀: 5 nM (CTX-M-15), 8 nM (TEM-1)^[1] In Vitro: Avibactam is a molecule with little antibacterial activity, that inhibits class A and C β-lactamases, but not metallo types and Acinetobacter OXA carbapenemases^[2].
Ceftazidime (HY-B0593)-Avibactam (0-256 mg/L) inhibits 16 bla_KPC-2 positive and 1 of bla_OXA-232 positive Klebsiella pneumonia growth with MIC₅₀ and MIC₉₀ for both 8?mg/L^[4]. In Vivo: Ceftazidime-Avibactam (0.375?mg/g; s.c.; q8h for 10 days) has a significant effect on the bacteria and led to a certain therapeutic efficacy in K. pneumoniae strain Y8 infected mouse model^[3].
Avibactam (64 mg/kg; s.c.; once) shows mean estimated half-life in plasma in the terminal phase of 0.24 h in Pseudomonas aeruginosa infected neutropenic mice with lung infection^[3].