Cefsulodin (sodium)

Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacterium tuberculosis, with an IC₅₀ value of 16 μM^[1][2][3][4]. IC50 & Target: 16 μM (mPTPB, phosphatase from Mycobacterium tuberculosis)^[1] In Vitro: Cefsulodin sodium (0.5-64 mg/mL; 18 h) is active in minimum inhibitory concentrations (MICs) of 0.5-64 mg/mL, is about 16- to 32-fold more active than Carbenicillin (HY-B0525) against Psuedomonas aeruginosa^[1].
Cefsulodin sodium (8-16 μg/mL; 4.5 h) is not hydrolyzed by the beta-lactamase induced in P. aeruginosa by growth in the presence of benzylpenicillin^[1].
In Vivo: Cefsulodin sodium (1 g/kg/tag; i.p.; 5 d, 9 single doses with intervals of 12 h) shows a increasing excretion of tubule cells in the rat, as a measure of nephrotoxicity, and displays tubule toxic threshold doses of 250 mg/kg (s.c.; 12 d) with nine single doses^[4].