Gepotidacin
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Also known as GepotidacinaGepotidacineGSK-2140944GSK2140944
Summary
Gepotidacin (CHEMBL3317856) is a phase-3 clinical-stage small molecule (ATC J01XX13); indicated across 5 conditions including gonorrhea and urinary tract infection.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- ATC class: J01XX13
- Indications: 5 conditions
- Clinical trials: 21
- Chemistry: 448.5 Da · C24H28N6O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3317856 |
| Name | Gepotidacin |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 25101874 |
| ATC | J01XX13 |
| Molecular formula | C24H28N6O3 |
| Molecular weight | 448.5 |
| InChIKey | PZFAZQUREQIODZ-LJQANCHMSA-N |
SMILES: C1CC2=CC(=NC=C2OC1)CNC3CCN(CC3)C[C@@H]4CN5C(=O)C=CC6=C5N4C(=O)C=N6
IUPAC name: (3R)-3-[[4-(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethylamino)piperidin-1-yl]methyl]-1,4,7-triazatricyclo[6.3.1.04,12]dodeca-6,8(12),9-triene-5,11-dione
Also known as: Gepotidacin, Gepotidacina, Gepotidacine, GSK-2140944, GSK2140944, GEPOTIDACIN
Parent form; salt/anhydrous children: CHEMBL3545364
Patent coverage: 93 distinct patent families (215 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 182 (85%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: DNA topoisomerase 2-alpha, DNA gyrase, DNA gyrase, Topoisomerase IV, DNA gyrase subunit A/DNA gyrase subunit B.
Bioactivity
ChEMBL activities: 15 potent at pChembl ≥ 5 of 16 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P0A0K8 | 8.74 | IC50 | 1.8 | nM | CHEMBL_ACT_29229232 |
| P0A0K8 | 7.33 | IC50 | 47 | nM | CHEMBL_ACT_19131868 |
| P0A0K8 | 7.33 | IC50 | 47 | nM | CHEMBL_ACT_20657350 |
| P0AES4 | 7.22 | IC50 | 60 | nM | CHEMBL_ACT_24843786 |
| P0A0K8 | 6.77 | IC50 | 170 | nM | CHEMBL_ACT_23293593 |
| P0A0K8 | 6.61 | IC50 | 244 | nM | CHEMBL_ACT_23225803 |
| P0AES4 | 6.61 | IC50 | 244 | nM | CHEMBL_ACT_25708009 |
| P0A0K8 | 6.43 | IC50 | 374 | nM | CHEMBL_ACT_23225817 |
| P0A0K8 | 6.43 | IC50 | 374 | nM | CHEMBL_ACT_25707995 |
| P0C1S7 | 6.22 | IC50 | 600 | nM | CHEMBL_ACT_19131875 |
| P0C1S7 | 6.05 | IC50 | 900 | nM | CHEMBL_ACT_29229236 |
| P0C1S7 | 5.55 | IC50 | 2800 | nM | CHEMBL_ACT_23293634 |
| P9WG45 | 5.41 | IC50 | 3940 | nM | CHEMBL_ACT_29075593 |
| P0C1S7 | 5.08 | IC50 | 8299 | nM | CHEMBL_ACT_23225831 |
| P0C1S7 | 5.08 | IC50 | 8299 | nM | CHEMBL_ACT_25708023 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
5 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| gonorrhea | 3 | MONDO:0004277 | DOID:7551 |
| urinary tract infection | 3 | MONDO:0100338 | EFO:0003103 |
| bacterial infectious disease | 3 | MONDO:0005113 | EFO:0000771 |
| respiratory tract infectious disorder | 1 | MONDO:0024355 | MONDO:0024355 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 21.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 13 |
| PHASE3 | 5 |
| PHASE2 | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04010539 | PHASE3 | COMPLETED | A Study Evaluating Efficacy and Safety of Gepotidacin Compared With Ceftriaxone Plus Azithromycin in the Treatment of Uncomplicated Urogenital Gonorrhea |
| NCT04020341 | PHASE3 | COMPLETED | A Study to Evaluate Efficacy and Safety of Gepotidacin in the Treatment of Uncomplicated Urinary Tract Infection (UTI) |
| NCT04187144 | PHASE3 | COMPLETED | Comparative Study to Evaluate Efficacy and Safety of Gepotidacin to Nitrofurantoin in Treatment of Uncomplicated Urinary Tract Infection (UTI) |
| NCT05630833 | PHASE3 | COMPLETED | A Study to Investigate the Efficacy and Safety With Gepotidacin in Japanese Female Participants With Uncomplicated Urinary Tract Infection (Acute Cystitis) |
| NCT06597344 | PHASE3 | COMPLETED | A Study in Adolescent and Adult Female Participants to Evaluate Clinical Symptom Improvement and the Safety of Gepotidacin During Treatment of Uncomplicated Urinary Tract Infections (Acute Cystitis) |
| NCT02045797 | PHASE2 | COMPLETED | Dose-Ranging Study of GSK2140944 in the Treatment of Subjects With Suspected or Confirmed Gram-Positive Acute Bacterial Skin and Skin Structure Infections |
| NCT02294682 | PHASE2 | COMPLETED | A Dose-Ranging Study Evaluating the Efficacy, Safety, and Tolerability of GSK2140944 in the Treatment of Uncomplicated Urogenital Gonorrhea Caused by Neisseria Gonorrhoeae |
| NCT03568942 | PHASE2 | COMPLETED | Pharmacokinetic Study of Oral Gepotidacin (GSK2140944) in Subjects With Uncomplicated Urinary Tract Infection (Acute Cystitis) |
| NCT07371429 | PHASE1 | NOT_YET_RECRUITING | A Study in Pediatric Participants Aged ≥2 to <12 Years With a Suspected or Confirmed Bacterial Infection or Receiving Prophylaxis Antibiotics |
| NCT01706315 | PHASE1 | COMPLETED | This Study Will Investigate the Safety, Tolerability and Pharmacokinetic Profile of Repeat Oral Doses of GSK2140944 in Healthy Adult Subjects |
| NCT02000765 | PHASE1 | COMPLETED | A Study to Investigate the Recovery, Excretion and Pharmacokinetics of [14C]-GSK2140944 Administered as a Single Intravenous and Single Oral Dose to Healthy Adult Male Subjects |
| NCT02045849 | PHASE1 | COMPLETED | Relative Bioavailability, Safety, Tolerability, Pharmacokinetics (PK) and Food Effect Study of GSK2140944 in Healthy Subjects |
| NCT02202187 | PHASE1 | COMPLETED | A Single Oral Escalating Dose Study of GSK2140944 in Healthy Volunteers |
| NCT02257398 | PHASE1 | COMPLETED | Placebo and Moxifloxacin Controlled Cardiac Conduction Study of GSK2140944 in Healthy Volunteers |
| NCT02729038 | PHASE1 | COMPLETED | Pharmacokinetic Study of Gepotidacin in Subjects With Varying Degrees of Renal Impairment and in Subjects With Normal Renal Function |
| NCT02853435 | PHASE1 | COMPLETED | To Assess Bioavailability, Food Effect and Pharmacokinetics of Gepotidacin Tablets: A Phase I, Single-Dose, 2 Part Study in Healthy Subjects. |
| NCT03562117 | PHASE1 | COMPLETED | Pharmacokinetics (PK) Study of Gepotidacin (GSK2140944) in Adult Subjects With Varying Degrees of Hepatic Impairment and in Matched Control Subjects With Normal Hepatic Function |
| NCT04079790 | PHASE1 | COMPLETED | Pharmacokinetics of Gepotidacin Tablets in Adults and Adolescents Subjects |
| NCT04484740 | PHASE1 | COMPLETED | Penetration of the Innovative Antibiotic Gepotidacin Into Prostate and Tonsillar Tissue |
| NCT04493931 | PHASE1 | COMPLETED | Drug-drug Interaction Study of Gepotidacin |
| NCT05271799 | PHASE1 | COMPLETED | A Study to Evaluate Pharmacokinetic, Safety, Tolerability and Relative Bioavailability of Gepotidacin in Healthy Adult Male and Female Participants |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).