Avibactam sodium salt- 13 C 5 (NXL-104- 13 C 5 ) is 13 C labeled Avibactam (sodium). Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50 s of 8 nM and 5 nM, respectively [1] [2].
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Berkhout J, et al. Pharmacokinetics and penetration of GR20263 and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrob Agents Chemother. 2015 Apr;59(4):2299-304.
[3]. Ehmann DE, et al.
Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor.
Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8.
[4]. Livermore DM, et al.
Characterization of β-lactamase and porin mutants of Enterobacteriaceae selected with ceftaroline + avibactam (NXL104).
J Antimicrob Chemother. 2012 Jun;67(6):1354-8.
[5]. Zhang W, et al. In vitro and in vivo bactericidal activity of ceftazidime-avibactam against Carbapenemase-producing Klebsiella pneumoniae. Antimicrob Resist Infect Control. 2018 Nov 21;7:142.
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Berkhout J, et al. Pharmacokinetics and penetration of GR20263 and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrob Agents Chemother. 2015 Apr;59(4):2299-304.
[3]. Ehmann DE, et al.
Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor.
Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8.
[4]. Livermore DM, et al.
Characterization of β-lactamase and porin mutants of Enterobacteriaceae selected with ceftaroline + avibactam (NXL104).
J Antimicrob Chemother. 2012 Jun;67(6):1354-8.
[5]. Zhang W, et al. In vitro and in vivo bactericidal activity of ceftazidime-avibactam against Carbapenemase-producing Klebsiella pneumoniae. Antimicrob Resist Infect Control. 2018 Nov 21;7:142.