Gepotidacin

Gepotidacin

Gepotidacin is a novel antibacterial agent that belongs to the class of antibiotics known as triazaacenaphthylene bacterial topoisomerase inhibitors. It is currently under development by GlaxoSmithKline (GSK) for the treatment of bacterial infections caused by Gram-positive bacteria and Gram-negative bacteria.

Mechanism of Action

Gepotidacin works by inhibiting bacterial DNA gyrase and topoisomerase IV, enzymes that are essential for bacterial DNA replication, transcription, repair, and recombination. By inhibiting these enzymes, gepotidacin disrupts the process of bacterial DNA replication, leading to the death of the bacteria.

Clinical Trials

Gepotidacin has undergone Phase 2 and Phase 3 clinical trials for the treatment of uncomplicated urinary tract infection (UTI) and uncomplicated gonorrhea. In these trials, gepotidacin has shown promising results, with a high rate of clinical cure and a favorable safety profile.

Resistance

Resistance to gepotidacin has been observed in laboratory studies. The main mechanism of resistance is through mutations in the genes encoding for DNA gyrase and topoisomerase IV. However, the clinical significance of this resistance is currently unknown.

Future Development

Gepotidacin is currently in Phase 3 clinical trials for the treatment of uncomplicated UTI and uncomplicated gonorrhea. If these trials are successful, GSK plans to submit a New Drug Application (NDA) to the Food and Drug Administration (FDA) for the approval of gepotidacin.

See Also

• Antibiotics
• Antibacterial
• Clinical trials
• GlaxoSmithKline
• Gram-positive bacteria
• Gram-negative bacteria
• Topoisomerase inhibitors
• Urinary tract infection
• Gonorrhea