Gepotidacin (Blujepa): A Comprehensive Monograph on a First-in-Class Triazaacenaphthylene Antibiotic

1.0 Executive Summary & Introduction

1.1 The Evolving Landscape of Antimicrobial Resistance in Common Infections

The global public health infrastructure faces an escalating threat from antimicrobial resistance (AMR), a crisis that compromises the efficacy of modern medicine.[1] Common bacterial infections, once readily treatable, are increasingly caused by multidrug-resistant (MDR) organisms, leading to higher morbidity, mortality, and healthcare costs.[2] This challenge is particularly acute in the management of uncomplicated urinary tract infections (uUTIs) and sexually transmitted infections (STIs) like gonorrhea. Uropathogens, predominantly

Escherichia coli, have developed widespread resistance to standard oral therapies, including trimethoprim-sulfamethoxazole and fluoroquinolones.[3] Similarly,

Neisseria gonorrhoeae has been designated an "urgent threat" pathogen due to its remarkable ability to acquire resistance, rendering many antibiotic classes, including penicillins, tetracyclines, and fluoroquinolones, clinically ineffective.[1] The current reliance on injectable cephalosporins for gonorrhea is tenuous, with emerging resistance threatening the last line of effective monotherapy.[1] This backdrop of dwindling therapeutic options is compounded by a stagnant developmental pipeline for new oral antibiotics, creating a critical unmet medical need for novel agents with distinct mechanisms of action capable of overcoming existing resistance patterns.[2]

1.2 Introduction to Gepotidacin: A Novel Bacterial Topoisomerase Inhibitor