Description
Sulopenem is a parenteral penem that demonstrates high activity against Gram-positive, Gram-negative, and anaerobic bacteria. Since it is stable in relation to renal dehydropeptidase I, it does not require concomitant administration of an inhibitor of this enzyme.
Uses
Sulopenem is a β-Lactamase inhibitor which is used in treatment of microbial infections. It is an important reagent for many drugs synthesized against bacterial infections.
Mechanism of action
Sulopenem is one of the penems and, as such, interacts with penicillin-binding proteins (PBPs). From in vitro studies, sulopenem has shown a high affinity for PBP1a, 1b, 2, and 3 in E. coli.
Pharmacokinetics
When 1 g of CP-65,207 [containing 46.3% of S-isomer (sulopenem)
and 53.7% of R-isomer] was administered by 10-minute intravenous
infusions, the peak concentration of sulopenem in serum was 36.0 mg/
ml, its half-life was 52.8 minutes, and the area under the serum
concentration-versus-time curve (AUC) from 0 to 8 hours was
21.0 mg/ml per hour.
in vivo
The protective effects of Sulopenem in murine experimental systemic infections are superior to those of Imipenem/Cilastatin. In murine experimental mixed infection with Escherichia coli and Bacteroides fragilis, Sulopenem has lower ED50. In guinea pigs experimental lung infection with Klebsiella pneumoniae, Sulopenem is more effective than CZON or Cefotiam[3].
