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Determination of gepotidacin levels in tonsils and prostatic tissue


Gepotidacin (GSK2140944) is a novel antibiotic that selectively inhibits bacterial DNA gyrase and topoisomerase IV by a unique mechanism, which is not utilised by any currently approved human therapeutic agent. Structural data with a type II topoisomerase, DNA gyrase, reveals the novel binding mode of the triazaacenaphthylene class and distinguishes it from the binding mode of the quinolone antibacterials. As a consequence of its novel mode of action, gepotidacin is active in vitro against most target pathogens carrying resistance determinants to established antibacterials, including fluoroquinolones. Gepotidacin has broad Gram positive activity and selective Gram negative activity. With increasing antimicrobial resistance, there are fewer options to treat gonorrhoea (Centers for Disease Control and Prevention (CDC) and World Health Organisation (WHO) urgent need), in particular at the pharyngeal site where tissue penetration is essential to activity and extended spectrum beta-lactamases (ESBL)/MDR (CDC and WHO serious need) urological infections due to Escherichia coli. In addition, few orally available agents have favourable penetration characteristics which are essential to activity.

The scope of this action is to assess the novel antibiotic gepotidacin (GSK2140944).

The Portfolio Building Network (PBN), Pillar C of the IMI2 JU AMR Accelerator programme, will address the limited pipeline of treatments and preventions for AMR infections by enabling vibrant and nimble collaborations between EFPIA companies and small and medium-sized enterprises (SMEs) and/or academics that will advance the R&D pipeline of new and innovative agents to address AMR.

The expected impact of actions selected under this Call will be to: (1) contribute to the development of a vibrant AMR research environment in the EU and strengthen the competitiveness and industrial leadership of Europe; (2) contribute to the EU’s ambition of being a ‘best practice region’ for addressing AMR; (3) enhance the overall pipeline of medicines for patients with AMR infections and advance new and innovative agents.