Drug intelligence / Profile preview

sultamicillin (Pfizer)

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Sultamicillin is an orally bioavailable mutual prodrug that chemically links the semi-synthetic beta-lactam antibiotic ampicillin and the beta-lactamase inhibitor sulbactam via a double ester bond. Following oral administration, sultamicillin is efficiently absorbed from the gastrointestinal tract and rapidly hydrolyzed by esterases in the intestinal wall and blood to release equimolar concentrations of ampicillin and sulbactam into the systemic circulation. Ampicillin exerts its bactericidal effect by binding to penicillin-binding proteins (PBPs), thereby inhibiting the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls. Sulbactam acts as an irreversible "suicide" inhibitor of various beta-lactamases (primarily Class A), protecting ampicillin from enzymatic degradation and extending its spectrum of activity to include many beta-lactamase-producing Gram-positive and Gram-negative organisms. Medimark Biotech (Medimarket) markets this formulation as Ampium 375 for the treatment of various bacterial infections, including respiratory tract, urinary tract, and skin and soft tissue infections.

Brand names
AmpiumAmpium 375Ampium375Ampium-375Unasyn
Other names
Sultamicillin tosilateSultamicillin tosylate
02

Targets

β-lactamasePBP (Penicillin-binding protein family)

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