Sulopenem Etzadroxil

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

Sulopenem, similar to other beta-lactam antibacterials, exhibits time-dependent bacterial inhibition. The percentage of time that unbound plasma concentrations of sulopenem exceed the sulopenem minimum inhibitory concentration (MIC) against the infecting organism has been shown to best correlate with efficacy in _in vitro_ models of infection. In E. coli_, sulopenem demonstrated binding affinity for PBPs in the following order: PBP2 > PBP1A > PBP1B > PBP4 > PBP3 > PBP5/6.

Sulopenem has _in vitro_ activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of sulopenem results from the inhibition of cell wall synthesis and is mediated through sulopenem binding to penicillin binding proteins (PBPs). Sulopenem's β-lactam ring alkylates the serine residues of PBPs, ultimately inhibiting peptidoglycan cross-linking.

After oral administration, sulopenem etzadroxil is hydrolyzed via esterases to the active [sulopenem], which is further metabolized via hydrolysis and then dehydrogenation. Two inactive metabolites of sulopenem have been identified - M1a and M1b - which accounted for 21.8% and 43.6%, respectively, of circulating radioactivity following the administration of a radiolabeled dose.

Following rapid conversion into the active moiety, sulopenem bioavailability is approximately 40% in the fasted state, increasing to 64% when administered with a meal.

Following a single oral dose of radiolabeled sulopenem etzadroxil in healthy adult subjects, 44.3% of radioactive product was recovered in the feces (26.9% as unchanged sulopenem) and 40.8% was recovered in the urine (3.1% as unchanged sulopenem).