Drug intelligence / Profile preview

sulopenem etzadroxil

Development stage
Phase 3
Lead developer
Iterum Therapeutics
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Sulopenem etzadroxil is an orally available ester prodrug of sulopenem, a penem-class beta-lactam antibiotic. After oral administration, it is hydrolyzed to the active drug sulopenem, which exhibits broad-spectrum bactericidal activity against gram-positive and gram-negative aerobic and anaerobic bacteria by inhibiting bacterial cell wall synthesis through binding to penicillin-binding proteins (PBPs), with highest affinity for PBP2. Sulopenem etzadroxil is administered in combination with probenecid under the brand name Orlynvah to treat uncomplicated urinary tract infections (uUTI) in adult women who have limited or no alternative oral antibacterial treatment options. Probenecid acts as a renal tubular inhibitor to increase systemic exposure of sulopenem by reducing its renal excretion. The drug was developed by Iterum Therapeutics and received FDA approval in October 2024 for this indication[2][4][5][7].

Brand names
Orlynvah
Other names
sulopenem etzadroxilSulopenem Etzadroxil (USAN)1000296-70-7
02

Targets

PBP1b (Penicillin-binding protein 1B)PBP2 (Penicillin-binding protein 2)PBP1A (Penicillin-binding protein 1A)

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