Griseofulvin
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Also known as FulcinFulcin 125Fulcin 500FulsovinFulvicin p/gFulvicin p/g 165Fulvicin p/g 330Fulvicin-u/fGrifulvin vGris-pegGrisactinGrisactin ultraGrisactin vGriseofulvin microsizeGriseofulvin permeability diametermicrocrystallinemicrosizeultramicrocrystallineultramicrosize
Summary
Griseofulvin (CHEMBL562) is an approved small-molecule antibacterial agent (ATC D01AA08); indicated across 4 conditions including tinea pedis and tinea infection.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: D01AA08 (+1 more)
- Indications: 4 conditions
- Clinical trials: 6
- Chemistry: 352.8 Da · C17H17ClO6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL562 |
| Name | Griseofulvin |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 441140 |
| ChEBI | CHEBI:27779 |
| ATC | D01AA08, D01BA01 |
| Molecular formula | C17H17ClO6 |
| Molecular weight | 352.8 |
| InChIKey | DDUHZTYCFQRHIY-RBHXEPJQSA-N |
SMILES: C[C@@H]1CC(=O)C=C([C@]12C(=O)C3=C(O2)C(=C(C=C3OC)OC)Cl)OC
IUPAC name: (2S,5’R)-7-chloro-3’,4,6-trimethoxy-5’-methylspiro[1-benzofuran-2,4’-cyclohex-2-ene]-1’,3-dione
ChEBI definition: An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment.
Pharmacological roles (ChEBI): antibacterial agent.
Other ChEBI roles (chemical / environmental): Penicillium metabolite.
Also known as: Fulcin, Fulcin 125, Fulcin 500, Fulsovin, Fulvicin p/g, Fulvicin p/g 165, Fulvicin p/g 330, Fulvicin-u/f, Grifulvin v, Gris-peg, Grisactin, Grisactin ultra
Parent form; salt/anhydrous children: CHEMBL3794184
Patent coverage: 10,204 distinct patent families (36,847 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 36,636 (99%) 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: 16 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Lysine-specific demethylase 4E, Survival motor neuron protein, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Thyrotropin receptor, DNA polymerase beta, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Cytochrome P450 3A4, Nuclear receptor subfamily 1 group I member 2, Cruzipain.
Bioactivity
ChEMBL activities: 7 potent at pChembl ≥ 5 of 30 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| TDP1 | 6.4 | Potency | 398.1 | nM | CHEMBL_ACT_3929954 |
| HIF1A | 5.4 | Potency | 3981 | nM | CHEMBL_ACT_4130806 |
| HIF1A | 5.4 | Potency | 3981 | nM | CHEMBL_ACT_4519083 |
| PDE3A | 5.35 | AC50 | 4500 | nM | CHEMBL_ACT_25191346 |
| SLC22A1 | 5.14 | IC50 | 7300 | nM | CHEMBL_ACT_18040331 |
| TSHR | 5.1 | Potency | 7943 | nM | CHEMBL_ACT_3921116 |
| TSHR | 5.1 | Potency | 7943 | nM | CHEMBL_ACT_4618576 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
4 indications (4 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 |
|---|---|---|---|
| tinea pedis | 4 | MONDO:0005984 | EFO:0007512 |
| tinea infection | 4 | MONDO:0005982 | EFO:0007510 |
| candidiasis | 4 | MONDO:0002026 | MONDO:0002026 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 6.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 4 |
| PHASE3 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00117767 | PHASE3 | COMPLETED | Terbinafine Compared to Griseofulvin in Children With Tinea Capitis |
| NCT00863863 | PHASE1 | COMPLETED | A Relative Bioavailability Study of Griseofulvin 125 mg/5 mL Suspension Under Non-fasting Conditions |
| NCT00864071 | PHASE1 | COMPLETED | A Relative Bioavailability Study of Griseofulvin 125 mg/5 mL Suspension Under Fasting Conditions |
| NCT01518166 | PHASE1 | COMPLETED | Effect of Liraglutide on Gastrointestinal Absorption of Several Drugs and Potential Influence of Liraglutide on Intragastric pH |
| NCT04318535 | PHASE1 | COMPLETED | Bioequivalence (BE) Study of Test Griseofulvin 500 Milligram (mg) Tablets Versus Reference and Dose Proportionality Study of Test Griseofulvin 250 mg and 500 mg Tablets Under Fed Conditions |
| NCT00127868 | Not specified | COMPLETED | Selenium Sulfide, Ketoconazole and Ciclopirox Shampoo as Additional Treatments for Tinea Capitis (Scalp Ringworm) |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Diseases: tinea pedis, tinea infection, candidiasis