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gepotidacin + rifampicin
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This is a **combination of gepotidacin, a novel triazaacenaphthylene small molecule antibiotic, and rifampicin, a classic rifamycin antibacterial agent**. Gepotidacin inhibits bacterial DNA replication by selectively inhibiting type IIA bacterial topoisomerases—DNA gyrase (GyrA subunit) and topoisomerase IV (ParC subunit)—at a unique binding site, which is distinct from fluoroquinolones. Rifampicin is a potent inducer of cytochrome P450 3A4 and P-glycoprotein, and works by inhibiting bacterial DNA-dependent RNA polymerase, thereby suppressing RNA synthesis.
- Other names
- gepotidacinrifampin
02
Targets
Topo IV (Bacterial Topoisomerase IV)GyrA (DNA gyrase subunit A)
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