Drug intelligence / Profile preview

GSK 2115160A

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

GSK 2115160A is a novel bacterial topoisomerase inhibitor (NBTI) that was under development by GSK for the treatment of various bacterial infections, including acute bacterial skin and skin structure infections (ABSSSI) and community-acquired bacterial pneumonia (CABP). As an NBTI, it belongs to a class of antibiotics distinct from fluoroquinolones; while fluoroquinolones stabilize the covalent DNA-enzyme complex and induce double-strand breaks, NBTIs like GSK 2115160A bind to a different site on the bacterial DNA gyrase and topoisomerase IV enzymes, inhibiting DNA synthesis without necessarily inducing the same type of DNA damage. This unique mechanism allows it to maintain activity against strains resistant to existing antibiotic classes. However, clinical development of GSK 2115160A was discontinued in Phase 2, with GSK shifting focus to its successor compound, gepotidacin (GSK2140944).

02

Targets

Topo IV (Bacterial Topoisomerase IV)DNA gyrase

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