Drug intelligence / Profile preview

gepotidacin + digoxin + midazolam

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Intranasal, Buccal, Rectal
01

Overview

**gepotidacin + digoxin + midazolam** is a hypothetical combination of three distinct pharmaceutical agents: gepotidacin (a novel antibacterial), digoxin (a cardiac glycoside), and midazolam (a benzodiazepine used for sedation). - **Gepotidacin** is a first-in-class triazaacenaphthylene antibiotic approved for the treatment of uncomplicated urinary tract infections (uUTI) caused by susceptible organisms in females aged 12 years and older. Gepotidacin selectively inhibits bacterial DNA gyrase (type II topoisomerase) and topoisomerase IV, interfering with bacterial DNA replication and transcription, and is distinct from fluoroquinolones in its binding and resistance profile[1][3][5]. - **Digoxin** is a cardiac glycoside used primarily in the management of various heart conditions, including atrial fibrillation and heart failure, acting by inhibiting the sodium-potassium ATPase in cardiac tissue. - **Midazolam** is a short-acting benzodiazepine that potentiates the effects of the neurotransmitter GABA at the GABA-A receptor, providing rapid onset sedation, anxiolysis, and amnesia, and is used routinely in procedural sedation and anesthesia[2][4]. There is no evidence in current literature or regulatory documents for a clinical product combining these three agents for a single indication. In pharmacological evaluation, gepotidacin can increase plasma concentrations of both digoxin and midazolam via inhibition of drug transporters and potential CYP3A4 interaction, requiring dose adjustment and monitoring[3].

02

Targets

Topo IV (Bacterial Topoisomerase IV)DNA gyrase

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