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Brand Name :
N/A
Synonyms :
gepotidacin
Class :
Antibiotics, Antibacterial agent, Type II topoisomerase inhibitor
Brand Name :
N/A
Synonyms :
gepotidacin
Class :
Antibiotics, Antibacterial agent, Type II topoisomerase inhibitor
Dosage Forms & Strengths
It is used for investigational and research purpose
Tablet
1500 mg
3000 mg
Take dose of 1500 mg orally two times daily for 5 days
Dose Modifications
Renal impairment
Mild-to-moderate: No dose adjustment required
Severe: Avoid due to risk of QT prolongation from gepotidacin.
Hepatic impairment
Mild-to-moderate: No dose adjustment required
Severe: Avoid due to risk of QT prolongation from gepotidacin
Dosing Considerations
Use only for infections confirmed or likely caused by sensitive bacteria to prevent drug resistance
Safety and efficacy are not seen in pediatrics
Urinary Tract Infections
Take dose of 1500 mg orally two times daily with food for 5 days
Dosage Modifications
Renal impairment
Mild-to-moderate: No dose adjustment required
Severe: Avoid due to risk of QT prolongation from gepotidacin
Hepatic impairment
Mild-to-moderate: No dose adjustment required
Severe: Avoid due to risk of QT prolongation from gepotidacin.
Refer to the adult dosing
Actions and Spectrum:
Actions:
The growing danger of antibiotic resistance makes curing easy urinary tract infections (UTIs) and urogenital gonorrhea really hard. This shows we urgently need new oral medications. Gepotidacin, an innovative bacteria-killing antibiotic, could help solve this issue. It’s the first triazaacenaphthylene antibiotic ever created. It disrupts how bacteria copy their DNA by targeting two key enzymes. To become resistant, bacteria would need multiple mutations, which is unlikely. Early Phase II trial results for UTIs and gonorrhea look encouraging. Phase III trials are also happening now. If approved, gepotidacin would be the first new oral UTI antibiotic in over twenty years – a major breakthrough.
Spectrum:
Gepotidacin, born from GSK scientists’ innovative minds, emerges as a distinct investigational antibiotic. Its bactericidal nature stems from a unique triazaacenaphthylene structure. Gepotidacin inhibits bacterial DNA replication via a distinctive mechanism and binding site. Remarkably, it balances inhibition of two separate Type II topoisomerase enzymes. This capability empowers gepotidacin against diverse uropathogens, like E. coli, S. saprophyticus, and N. gonorrhoeae. Even strains resistant to existing antibiotics fall prey to gepotidacin’s prowess. Notably, susceptibility to gepotidacin requires specific mutations in both enzymes, underscoring its promise against challenging bacterial infections.
Microbiological Spectrum and Antimicrobial Susceptibility:
Gepotidacin exhibits robust in vitro activity against prevalent bacterial pathogens. Testing on globally collected isolates from 2010-2012 by Biedenbach et al. showcased its efficacy. Strains like Streptococcus pneumoniae, Haemophilus influenzae, E. coli, and Staphylococcus aureus were scrutinized. E. coli exhibited an MIC90 of 2 mg/L, slightly higher in levofloxacin-non-susceptible strains. Nitrofurantoin-non-susceptible and fosfomycin-non-susceptible isolates followed suit, highlighting gepotidacin’s versatility. N. gonorrhoeae susceptibility was assessed, revealing test conditions impacted MIC determinations. Gepotidacin also inhibited Gram-negative and Gram-positive anaerobes. Notably, a 5-day gepotidacin course showed no lasting human microbiome impact, swiftly reverting within one month post-treatment. These findings underscore gepotidacin’s broad-spectrum activity and antimicrobial potential.
Frequency defined
Diarrhea (14-18%)
Frequency not defined
Emesis
Abdominal pain
Nausea
faltulence
Limited data is available
Contraindication/Caution:
Contraindications
Cautions
Pregnancy consideration:
No data is available regarding the administration of the drug during pregnancy.
Breastfeeding warnings:
No data is available regarding the excretion of drug in breast milk.
Pregnancy categories:
Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: No data is available for the drug under this category.
Pharmacology:
Antimicrobial resistance presents a serious problem for gonorrhea patients. Neisseria gonorrhoeae has developed resistance to almost all recommended antibiotics. The upcoming trial phase aims to evaluate the effectiveness of gepotidacin, a novel antibiotic, in treating uncomplicated urogenital gonorrhea. Gepotidacin’s unique mechanism could address the urgent need for new oral treatments against antibiotic-resistant gonorrhea strains. This study is crucial for assessing gepotidacin’s potential role in combating resistant Neisseria gonorrhoeae.
Gepotidacin is a novel bacterial topoisomerase inhibitor. It selectively targets topoisomerase IV and DNA gyrase’s B subunit. This distinctive mechanism induces single-stranded breaks via gyrase, exhibiting bactericidal activity and low spontaneous single-step resistance rates. Structural data shows gepotidacin’s binding mode differs from fluoroquinolones. In vitro, it demonstrates efficacy against bacteria with fluoroquinolone resistance determinants.
Pharmacodynamics:
Gepotidacin’s PD index for efficacy mirrors that of fluoroquinolones. MIC values for E. coli isolates were between 1 and 4 mg/L. The median free-drug AUC/MIC ratios associated with bacterial stasis and reductions were 33.9, 43.7, and 60.7, respectively. AUC/MIC ratios ≥ 275 suppressed microbial resistance development. For UTI treatment, Phase III trials adopted a 1500 mg twice-daily regimen for 5 days. For urogenital gonorrhea, two doses of 3000 mg were spaced 10–12 h apart.
Gepotidacin (GSK2140944) is a valuable candidate for exploring resistance development against multitarget antibiotics. This compound inhibits bacterial DNA gyrase and topoisomerase IV selectively. It interacts with specific residues in their subunits. Studies reveal a single mutation does not confer significant gepotidacin resistance. The antibiotic shows excellent efficacy against gram-negative bacteria like K. pneumoniae. However, specific mutations in the target gene significantly reduce susceptibility in various Enterobacteriaceae. The GyrA D82N and ParC D79N mutations show substantial resistance. But, overall, a single mutation has minimal impact on gepotidacin sensitivity. FDA approval of multitarget compounds like gepotidacin holds promise. It could enhance our ability to combat bacterial infections and curb multidrug-resistant strains’ rise in the future.
Pharmacokinetics:
Absorption
Gepotidacin shows clear drug absorption patterns in healthy adults. A single dose leads to highest blood levels at 3 hours. However, two doses reach peaks at 1.5 and 2.25 hours after taking the medicine. When fasting, a 1500 mg capsule gives an AUC0-∞ of 15.8 and maximum concentration of 4.37 μg h/mL. These numbers indicate how much and how fast the drug is absorbed. They reveal details about gepotidacin’s bioavailability in the body.
Distribution
The dispersal of gepotidacin is seen through differences in tablet forms. Yet, they reveal comparable values for AUC0–∞, Cmax, and terminal half-life (t½). This shows how the medicine spreads evenly throughout the body. It demonstrates uniform pharmacokinetic behavior across formulations. A Phase IIa study used a 750 mg tablet. It confirmed gepotidacin reaches sufficient plasma levels. This supports its distribution profile.
Metabolism
Metabolic details for gepotidacin remain unclear in this context. Knowing how it’s broken down inside the body could help grasp its full journey though. Tracing the drug’s paths and transformations would expand our knowledge significantly.
Elimination and Excretion
Gepotidacin follows a specific pattern when it comes to excretion. About half of the drug gets absorbed after taking it orally. This shows its bioavailability is important. Additionally, urine levels stay above 4 mg/L for 24 hours. Understanding how gepotidacin leaves the body through urine gives key details. This information helps build its pharmacokinetic profile.
Administration:
Gepotidacin gets given through an IV or by mouth. Doctors decide how to give it, depending on the infection and drug form. They consider how serious the infection is, the patient’s health, and the bacteria causing it. The right way to give the drug ensures effective, personalized treatment.
Patient information leaflet
Generic Name: gepotidacin
Pronounced: jeh-poh-TYE-dah-sin
Why do we use gepotidacin?
Gepotidacin is an investigational antibiotic that can fight different types of bacteria. It works well against gram-positive and gram-negative bacteria, even those who are resistant to other treatments. As a type II topoisomerase inhibitor, gepotidacin targets enzymes bacteria need for DNA replication. Doctors decide to use gepotidacin based on the infection type, how bad it is, and the bacteria involved. Clinical trials are essential to show if gepotidacin is safe and effective for different infections. Gepotidacin could help treat infections that don’t respond to standard antibiotics.
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