Sulopenem etzadroxil CAS# 1000296-70-7 硫培南酯

Sulopenem etzadroxil is a penem antibiotic agent. In vitro, the active moiety Sulopenem demonstrates strong bactericidal activity: MIC₅₀/₉₀ values against Enterobacterales of ~0.03/0.25 mg/L (or ≤0.5 mg/L for ~98% of isolates) including ESBL-phenotype E. coli (0.03/0.06 mg/L) and K. pneumoniae (0.06/0.12 mg/L). Time-kill studies show ≥3 log₁₀ reduction at ~8× MIC within 24 h. In animal models, sulopenem (or the oral pro-drug etzadroxil) showed in vivo efficacy: in murine systemic and thigh infection models (e.g., ESBL-positive K. pneumoniae) and murine urinary tract infection models (including MDR ST131 E. coli in C3H/HeN mice) it led to large reductions in bacterial burden or complete resolution of bacteriuria and tissue infection. PK/PD modelling indicated that ~20–24% fT>MIC (free drug time above MIC) correlates with effect in thigh infection models.