Blujepa (gepotidacin) / GSK - LARVOL DELTA

Treatment of Urinary Tract Infections with Gepotidacin: The Promising Antibiotic. (PubMed, Curr Drug Targets) - "Considering the cases of antibiotic resistance and novel mechanisms of action, the broad-spectrum action of gepotidacin may be beneficial in treating UTIs."

Journal • Infectious Disease • Nephrology

Novel potential treatment options for infections caused by multi-drug and extensively drug-resistant neisseria gonorrhoeae strains. (PubMed, Expert Rev Anti Infect Ther) - "Zoliflodacin and gepotidacin have the potential to optimize gonorrhea management as oral alternatives to current injectable ceftriaxone...Looking ahead, gonorrhea management will hopefully shift from empirical, syndromic treatment toward etiology-guided and AMR-informed therapy, driven by advances in rapid point-of-care testing and whole-genome sequencing technologies. Continuous phenotypic and genomic surveillance remains essential to detect early AMR signals, transmission of AMR strains, and inform treatment guidelines."

Journal • Review • Infectious Disease

Comparative efficacy of oral antibiotics against intracellular populations of uropathogenic Escherichia coli and bladder cell inflammatory response. (PubMed, Eur J Clin Microbiol Infect Dis) - "Here we investigated the efficacy of oral agents (nitrofurantoin, doxycycline, and gepotidacin) in intracellular bacterial clearance and proinflammatory signaling in bladder epithelial cell infection in-vitro. Our findings suggested variable and strain-dependent host inflammatory responses to UPEC infection and that mechanistically distinct oral antibiotics differentially affected the expression of proinflammatory mediators (TNFα and PTGS2) and efficacy in clearing intracellular bacteria."

Journal • Infectious Disease • Inflammation • Nephrology • PACERR • PTGS2 • TNFA

Characterization of isolates from two phase 3 uncomplicated urinary tract infection trials (EAGLE-2 and EAGLE-3) that show an apparent ≥4-fold increase in gepotidacin MIC between baseline and post-baseline visits. (PubMed, JAC Antimicrob Resist) - P3 | "Collectively, results from the Phase 3 trials indicate a low incidence of resistance development to gepotidacin, with only one potential case among gepotidacin-treated patients (1/1045; 0.096%). Further research is warranted to elucidate the mechanisms underlying elevated post-baseline gepotidacin MICs."

Journal • P3 data • Infectious Disease • Nephrology

Characterization of gepotidacin activity, including in vitro kill kinetics, checkerboard, and PAE/SME testing against gram-positive and gram-negative bacteria. (PubMed, Microbiol Spectr) - "No antagonism was observed in broth microdilution checkerboard studies with marketed antibiotics, and the only consistent synergy observed was with gepotidacin and vancomycin against S. saprophyticus. Importantly, gepotidacin did not interfere with the activity of other commonly used antibiotics, suggesting it can potentially be used alongside existing therapies if needed. These findings provide additional evidence supporting the effectiveness of gepotidacin against a broad range of UTI pathogens and help improve our understanding of how this new antibiotic may perform in clinical treatment."

Journal • Preclinical • Infectious Disease • Nephrology • Pneumonia

Antimicrobial resistance in Neisseria gonorrhoeae isolates at the Bangrak STIs Center, Bangkok, Thailand and WGS of antimicrobial-resistant isolates, 2018-23. (PubMed, J Antimicrob Chemother) - "Resistance to ceftriaxone, cefixime, azithromycin, tetracycline and ciprofloxacin was 0.5%, 0.8%, 1.7%, 83.7% and 95.7%, respectively. Resistance to ceftriaxone, cefixime and azithromycin has emerged in gonococcal strains circulating in Bangkok, Thailand, and resistance appears to be increasing. Resistance to these last options for monotherapy or dual therapy emphasize the need for strengthened national culture-based and genomic surveillance to prevent the spread of MDR and XDR strains in Thailand and globally, and implementation of the novel oral treatments, i.e. zoliflodacin and gepotidacin."

Journal • Infectious Disease

Oral Gepotidacin for the Treatment of Uncomplicated Urogenital Gonorrhea: Nucleic Acid Amplification Testing Outcomes in a Randomized, Multicenter Phase 3 Trial (EAGLE-1). (PubMed, Open Forum Infect Dis) - P3 | "In the microbiologically evaluable NAAT test-of-cure population, NAAT-confirmed success rates at the test-of-cure were 88.3% (151/171) for gepotidacin and 86.3% (132/153) for ceftriaxone plus azithromycin (adjusted difference 3.8%, 95% CI, -3.6%, 11.2%). The NAAT-confirmed success rates were high and similar between treatments, supporting the primary analysis results based on culture."

Journal • P3 data • Infectious Disease

Antibiotic Stewardship in Pediatric Urinary Tract Infections: Current Evidence and Practical Strategies. (PubMed, Antibiotics (Basel)) - "Antibiotic prophylaxis was not indicated in children with a normal urinary tract following a first febrile UTI and should be reserved for specific high-risk subgroups, with nitrofurantoin as the preferred agent...Gepotidacin, a first-in-class oral antibiotic approved in 2025 for uncomplicated UTI in female patients aged 12 years and older and weighing at least 40 kg, represented a limited option for eligible adolescents with resistant infections...Evidence-based interventions targeting urine collection, urinalysis-guided decision-making, early intravenous-to-oral transition, duration optimization, and selective prophylaxis use can collectively reduce unnecessary antibiotic exposure without compromising patient outcomes. A dedicated stewardship-oriented pediatric UTI guideline, standardized resistance surveillance, and multicenter stewardship program evaluations with patient-centered outcomes are critical research priorities."

Journal • Review • Infectious Disease • Nephrology • Pediatrics

Efficacy and Safety of Oral Type II Topoisomerase Inhibitors Versus Ceftriaxone-Based Regimens for the Treatment of Gonorrhoea: A Systematic Review and Meta-Analysis of Randomised Controlled Trials. (PubMed, J Infect Chemother) - "Preliminary evidence from a limited number of randomised controlled trials suggests that oral bacterial topoisomerase II inhibitors may represent promising treatment options for uncomplicated gonorrhoea. However, the current evidence remains limited, and further adequately powered clinical trials and post-approval surveillance are required to confirm their long-term efficacy, safety, and resistance implications."

Journal • Retrospective data • Review • Infectious Disease

In vitro evaluation of the activity of pairwise combinations of zoliflodacin, gepotidacin, and ciprofloxacin against Neisseria gonorrhoeae. (PubMed, bioRxiv) - "While combination therapy could, in principle, delay the emergence and spread of resistance, doing so depends on the absence of antagonism between the co-administered drugs. Using in vitro checkerboard testing, we observed no evidence of antagonism for all pairwise combinations of zoliflodacin, gepotidacin, and ciprofloxacin, including in strains with elevated ciprofloxacin MICs."

Journal • Preclinical • Infectious Disease

The balance between a new Antibiotic and Non-antibiotic Alternatives for the treatment and prevention of uncomplicated Urinary Tract Infections. (PubMed, Clin Infect Dis) - No abstract available

Journal • Infectious Disease • Nephrology

The changing picture of community acquired urinary tract infections in the US: a daunting prospect. (PubMed, Expert Rev Anti Infect Ther) - "Resistance to fluoroquinolones and trimethoprim-sulfamethoxazole exceeding 40% among uropathogenic Escherichia coli - driven largely by multidrug-resistant and extended‑spectrum β‑lactamase (ESBL) - producing Enterobacterales strains such as ST131-are fueling increased reliance on parenteral agents, emergency department visits, and hospitalizations...It highlights oral agents approved or under review in the US, including pivmecillinam, sulopenem, and gepotidacin, each approved for uncomplicated UTI, as well as tebipenem pivoxil hydrobromide, which if approved, would represent the first oral carbapenem option for selected complicated UTIs, and discusses antimicrobial stewardship principles for community UTI management...Pharmacoeconomic analyses incorporating avoided admissions and patient convenience will be essential. Judiciously deployed within stewardship frameworks, these agents have potential to reduce the clinical and economic burden of multidrug-resistant UTI,..."

Journal • Review • Infectious Disease • Nephrology

Gepotidacin in oral antibacterial pharmacotherapy: efficacy, safety, and clinical positioning. (PubMed, Expert Opin Pharmacother) - "Gepotidacin should be viewed as a selective addition to oral antibacterial pharmacotherapy rather than a replacement for established first-line regimens. Its long-term role will depend on stewardship-aligned use, resistance surveillance, comparative-effectiveness data, and careful safety management."

Journal • Review • Infectious Disease • Nephrology

Safety and efficacy of gepotidacin in urinary tract infection: a GRADE-assessed systematic review and meta-analysis-right-to-reply. (PubMed, J Antimicrob Chemother) - No abstract available

Journal • Retrospective data • Infectious Disease • Nephrology

Subgroup Analysis of Pooled Phase 3 Efficacy Data from Two Randomized Trials of Gepotidacin Versus Nitrofurantoin in Uncomplicated Urinary Tract Infections (EAGLE-2 and EAGLE-3) including Participants with Uropathogens Not-Susceptible to Nitrofurantoin. (PubMed, Clin Infect Dis) - P3 | "Gepotidacin demonstrated efficacy with generally higher therapeutic success rates versus nitrofurantoin in participants with NTF-S and NTF-NS uropathogens, and across a range of key subgroups."

Journal • P3 data • Diabetes • Infectious Disease • Metabolic Disorders • Nephrology • Renal Disease

In vitro antibacterial activity of gepotidacin in combination with other antimicrobial agents against Neisseria gonorrhoeae isolates. (PubMed, Antimicrob Agents Chemother) - "Synergy and antagonism were evaluated using fractional inhibitory concentration (FIC) and FIC index (FICI) results for gepotidacin and comparator agents (azithromycin, cefixime, ceftriaxone, gemifloxacin, sitafloxacin, gentamicin, spectinomycin, doxycycline, and lefamulin). The evaluation of FICI showed no antagonistic or synergistic interactions, while the evaluation of individual FIC values revealed strain- and agent-specific synergistic or additive effects."

Journal • Preclinical • Infectious Disease

A high-throughput fluorescent DNA cleavage assay for discovering bacterial DNA gyrase poisons. (PubMed, Nucleic Acids Res) - "We also discovered a new gyrase poison, Pyr-AMC. Biochemical assays and molecular dynamic simulation demonstrate that a single Pyr-AMC molecule binds the hydrophobic gepotidacin-binding pocket of gyrase, stabilizing cleavage complexes, and trapping gyrase-mediated DNA cleavages."

Journal

A Study to Evaluate Gepotidacin Exposure in Breast Milk of Healthy Lactating Women (clinicaltrials.gov) - P1 | N=8 | Not yet recruiting | Sponsor: GlaxoSmithKline

New P1 trial • Infectious Disease • Nephrology

Novel Bacterial Topoisomerase Inhibitors: A New Front in an Old War. (PubMed, J Mol Biol) - "The clinical translation of this class is exemplified by gepotidacin, the first-in-class triazaacenaphthylene approved in March 2025, which demonstrates balanced dual-targeting of gyrase and topoisomerase IV and maintains activity against fluoroquinolone-resistant pathogens. Ongoing clinical development of next-generation NBTIs, including BWC0977, underscores the continued promise of this class. Collectively, these efforts highlight NBTIs as a critical and expanding weapon in the fight against antimicrobial resistance."

Journal • Review • Cardiovascular

Prostatic tissue distribution of gepotidacin in patients undergoing prostatectomy: an ex-vivo microdialysis and pharmacokinetic modelling study. (PubMed, Clin Microbiol Infect) - "Ex-vivo MD proved feasible for quantifying gepotidacin in human prostate tissue, interstitial fluid showing exposures comparable to plasma. However, defining PK/PD targets against relevant pathogens for bacterial prostatitis remains essential for predicting drug efficacy for treatment of this disease."

Journal • PK/PD data • Preclinical • Infectious Disease

Extensively drug-resistant (XDR) Neisseria gonorrhoeae cured with ceftriaxone 2 g intravenous monotherapy in Croatia, March 2026. (PubMed, Euro Surveill) - "The Neisseria gonorrhoeae HR027 isolate (genomic lineage B, MLST sequence type (ST)9903) exhibited high-level azithromycin, ceftriaxone, cefixime, benzylpenicillin, ciprofloxacin and tetracycline resistance. A single dose of ceftriaxone 2 g administered intravenously cured the infection. HR027 showed zoliflodacin and gepotidacin wild-type minimum inhibitory concentrations."

Journal • Monotherapy • Infectious Disease

Antibacterial and antibiofilm activities of novel bacterial topoisomerase inhibitors against Staphylococcus aureus and other clinically relevant pathogens. (PubMed, Eur J Med Chem) - "Additionally, both compounds inhibited biofilm formation at 1/2 MIC and reduced metabolic activity within mature biofilms at 2 × MIC, outperforming gepotidacin, an FDA-approved NBTI, in several assays. Together, these findings identify new NBTI chemotypes with enhanced potency and promising antibiofilm activity, providing a strong foundation for future antibacterial development."

Journal • Infectious Disease

Synthesis and Clinical Application of Small-Molecule Drugs Approved by FDA in 2025. (PubMed, Med Res Rev) - "According to the FDA's 2025 Novel Drug Approvals list, 46 new drugs received approval, including both new chemical entities such as Ziftomenib, Sevabertinib, Zoliflodacin, and Gepotidacin, as well as new biologics. A significant proportion of the approved products navigated accelerated or priority review pathways, reflecting their potential impact on unmet medical needs. This review provides a comprehensive overview of the synthetic routes and clinical applications of FDA-approved small-molecule drugs in 2025, aiming to inspire future development in drug discovery."

FDA event • Journal • Review • Cardiovascular • Genetic Disorders • Immunology • Infectious Disease • Oncology

Sulopenem Etzadroxil/Probenecid: A Comprehensive Review of an Oral Thiopenem. (PubMed, Ann Pharmacother) - "Sulopenem etzadroxil/probenecid provides an additional oral treatment option for uUTI in adult women with limited or no alternative options."

Journal • Review • Infectious Disease • Nephrology

Determination of frequency of spontaneous resistance for gepotidacin and levofloxacin against a collection of gram-positive and gram-negative organisms. (PubMed, Antimicrob Agents Chemother) - "As gepotidacin target site mutations in gyrA/B were only found in Enterococcus faecalis, repressor inactivation or activator dysregulation mutations in efflux pumps were identified as possible mechanisms of reduced susceptibility in the Gram-negative isolates. Further investigation is needed into the relevance of these resistance mechanisms, the clinical significance of these findings, and whether there are any potential fitness costs of decreased gepotidacin susceptibility."

Journal • Infectious Disease • Nephrology • Pneumonia