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sulopenem
- Development stage
- Phase 3
- Lead developer
- Iterum Therapeutics
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Sulopenem is a broad-spectrum thiopenem β-lactam antibiotic developed for the treatment of infections caused by multidrug-resistant bacteria. It is active against both Gram-negative and Gram-positive organisms, including fluoroquinolone-resistant and extended-spectrum beta-lactamase (ESBL)-producing Enterobacterales. Sulopenem exerts its bactericidal effect by inhibiting bacterial cell wall synthesis through binding to penicillin-binding proteins (PBPs), with the highest affinity for PBP2. The drug is available in both intravenous form and as an oral prodrug (sulopenem etzadroxil), which is hydrolyzed in the body to release active sulopenem. When administered orally, it is co-formulated with probenecid to inhibit renal clearance and increase systemic exposure. Sulopenem has been approved for use in combination with probenecid under the brand name Orlynvah for treating uncomplicated urinary tract infections (uUTI) in adult women who have limited or no alternative oral antibacterial options[3][4][5][6][7].
- Brand names
- Orlynvah
- Other names
- sulopenem etzadroxil
02
Targets
PBP2 (Penicillin-binding protein 2)PBP1b (Penicillin-binding protein 1B)PBP4 (Penicillin-binding protein 4)PBP1A (Penicillin-binding protein 1A)PBP5 (D-alanyl-D-alanine carboxypeptidase DacA)
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