Fluorometholone
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Also known as FluatonFluor-opFluorometholone component of fml-sFluorometolonaFmlFml forteFml fteFml-neoNSC-33001OxyloneSID855588SID56422125SID91286SID144212910SID144203991SID170464629
Summary
Fluorometholone (CHEMBL1200600) is an approved small-molecule anti-inflammatory drug (ATC S01BA07) targeting NR3C1; indicated across 6 conditions including acne and eye disorder.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: S01BA07 (+5 more)
- Targets: 1 (NR3C1)
- Indications: 6 conditions
- Clinical trials: 14
- Chemistry: 376.5 Da · C22H29FO4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1200600 |
| Name | Fluorometholone |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 9878 |
| ChEBI | CHEBI:31625 |
| ATC | S01BA07, D07XB04, D07AB06, D10AA01, S01CB05, C05AA06 |
| Molecular formula | C22H29FO4 |
| Molecular weight | 376.5 |
| InChIKey | FAOZLTXFLGPHNG-KNAQIMQKSA-N |
SMILES: C[C@H]1C[C@H]2[C@@H]3CC[C@@]([C@]3(C[C@@H]([C@@]2([C@@]4(C1=CC(=O)C=C4)C)F)O)C)(C(=O)C)O
IUPAC name: (6S,8S,9R,10S,11S,13S,14S,17R)-17-acetyl-9-fluoro-11,17-dihydroxy-6,10,13-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one
ChEBI definition: A member of the class of glucocorticoids that is Δ1-progesterone substituted at positions 11β and 17 by hydroxy groups, at position 6α by a methyl group and at position 9 by a fluoro group. Used for the treatment of corticosteroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.
Pharmacological roles (ChEBI): anti-inflammatory drug.
Also known as: Fluaton, Fluor-op, Fluorometholone, Fluorometholone component of fml-s, Fluorometolona, Fml, Fml forte, Fml fte, Fml-neo, NSC-33001, Oxylone, SID855588
Patent coverage: 6,921 distinct patent families (24,094 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| NR3C1 | Glucocorticoid receptor | Agonist | 8.8 | 0.9% | P04150 |
Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Nuclear receptor ROR-gamma, Glucocorticoid receptor, Progesterone receptor, Nuclear receptor subfamily 1 group I member 2, Lysosomal alpha-glucosidase, Androgen receptor, Nuclear receptor subfamily 1 group I member 2, Hypoxia-inducible factor 1-alpha, Huntingtin.
Bioactivity
ChEMBL activities: 17 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| NR3C1 | 8.8 | Ki | 1.58 | nM | CHEMBL_ACT_7657186 |
| NR3C1 | 8.46 | IC50 | 3.47 | nM | CHEMBL_ACT_7657185 |
| NR3C1 | 8.4 | AC50 | 4 | nM | CHEMBL_ACT_25176086 |
| HIF1A | 8 | Potency | 10 | nM | CHEMBL_ACT_4128924 |
| HIF1A | 8 | Potency | 10 | nM | CHEMBL_ACT_4520746 |
| PGR | 7.28 | AC50 | 53 | nM | CHEMBL_ACT_25223239 |
| GAA | 6.75 | Potency | 177.8 | nM | CHEMBL_ACT_5009809 |
| GAA | 6.75 | Potency | 177.8 | nM | CHEMBL_ACT_5058338 |
| Q9R1A7 | 6.4 | EC50 | 400 | nM | CHEMBL_ACT_15463736 |
| P51450 | 6.35 | Potency | 446.7 | nM | CHEMBL_ACT_5008570 |
| P15207 | 6.08 | AC50 | 829 | nM | CHEMBL_ACT_25187595 |
| P15207 | 6.07 | Ki | 857 | nM | CHEMBL_ACT_7659320 |
| NR1I2 | 5.89 | EC50 | 1300 | nM | CHEMBL_ACT_15448163 |
| P15207 | 5.89 | IC50 | 1285 | nM | CHEMBL_ACT_7659319 |
| P51450 | 5.75 | Potency | 1771 | nM | CHEMBL_ACT_4535643 |
| NR1I2 | 5.5 | EC50 | 3200 | nM | CHEMBL_ACT_15463729 |
| HTT | 5.2 | Potency | 6310 | nM | CHEMBL_ACT_3753410 |
Target pathways
Aggregated over 1 target gene(s): NR3C1.
Top Reactome pathways
8 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand | 1 | NR3C1 |
| Nuclear Receptor transcription pathway | 1 | NR3C1 |
| SUMOylation of intracellular receptors | 1 | NR3C1 |
| PTK6 Expression | 1 | NR3C1 |
| Regulation of RUNX2 expression and activity | 1 | NR3C1 |
| FOXO-mediated transcription of oxidative stress, metabolic and neuronal genes | 1 | NR3C1 |
| Potential therapeutics for SARS | 1 | NR3C1 |
| Regulation of NPAS4 gene transcription | 1 | NR3C1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| negative regulation of transcription by RNA polymerase II | 1 |
| regulation of gluconeogenesis | 1 |
| chromatin organization | 1 |
| regulation of DNA-templated transcription | 1 |
| regulation of transcription by RNA polymerase II | 1 |
| apoptotic process | 1 |
| chromosome segregation | 1 |
| signal transduction | 1 |
| glucocorticoid metabolic process | 1 |
| response to wounding | 1 |
| gene expression | 1 |
| microglia differentiation | 1 |
| adrenal gland development | 1 |
| nuclear receptor-mediated steroid hormone signaling pathway | 1 |
| regulation of glucocorticoid biosynthetic process | 1 |
Indications & clinical
Indications
6 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 |
|---|---|---|---|
| acne | 4 | MONDO:0011438 | EFO:0003894 |
| eye disorder | 4 | MONDO:0005328 | EFO:0005752 |
| hemorrhoid | 4 | MONDO:0004872 | EFO:0009552 |
| dry eye syndrome | 3 | MONDO:0006733 | EFO:1000906 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 14.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 6 |
| PHASE3 | 3 |
| Not specified | 3 |
| PHASE2/PHASE3 | 1 |
| PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05716945 | PHASE4 | RECRUITING | The OPTIMISE Study |
| NCT02816905 | PHASE4 | COMPLETED | Ocular-hypertensive Response to Topical Steroids in Children After Bilateral Strabismus Surgery |
| NCT03747614 | PHASE4 | UNKNOWN | Ocular Micro-vascular Research Base on Functional Slip Lamp Biomicroscopy |
| NCT05587231 | PHASE4 | UNKNOWN | Comparison of the Postoperative Use of Dextenza vs a Standard Regimen After PRK |
| NCT06876116 | PHASE4 | COMPLETED | Once-daily Fluorometholone vs Twice-daily Cyclosporine in Dry Eye Disease |
| NCT07588074 | PHASE4 | COMPLETED | Tolerability Comparison of Flarex to Lotemax SM |
| NCT00707421 | PHASE3 | COMPLETED | Usefulness of Topical Non-Steroidal Anti-Inflammatory Drugs or Steroids Before Trabeculectomy and Clinical Outcomes |
| NCT02030990 | PHASE2/PHASE3 | UNKNOWN | The Use of MMC During PRK and Its Effect on Postoperative Topical Steroid Requirements |
| NCT02051023 | PHASE3 | COMPLETED | Efficacy and Safety of Fluorometholone (FML) in Dry Eye Disease (Keratoconjunctivitis Sicca) |
| NCT04149210 | PHASE3 | COMPLETED | FLuorometholone as Adjunctive MEdical Therapy for TT Surgery (FLAME) Trial |
| NCT01448213 | PHASE2 | COMPLETED | Comparison of Two Steroid Regimens to Prevent Transplant Rejection After Corneal Transplant (DMEK) |
| NCT01288404 | Not specified | COMPLETED | Randomized Controlled Trial of Subconjunctival Bevacizumab Injection in Impending Recurrent Pterygium |
| NCT01949454 | Not specified | COMPLETED | Fluorometholone as Ancillary Therapy for TT Surgery |
| NCT05313828 | Not specified | UNKNOWN | Effect of Various Treatment Modalities on Dendritic Vial Ulcer |
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
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
173 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| FULVESTRANT | ChEMBL + PubChem | Phase 4 (approved) | NR3C1 |
| PODOFILOX | ChEMBL + PubChem | Phase 4 (approved) | NR3C1 |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | NR3C1 |
| ACENOCOUMAROL | ChEMBL | Phase 4 (approved) | NR3C1 |
| ALCLOMETASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| AMCINONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| APREPITANT | ChEMBL | Phase 4 (approved) | NR3C1 |
| AURANOFIN | ChEMBL | Phase 4 (approved) | NR3C1 |
| BAZEDOXIFENE | ChEMBL | Phase 4 (approved) | NR3C1 |
| BECLOMETHASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| BETAMETHASONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| BETAMETHASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| BETAMETHASONE PHOSPHORIC ACID | ChEMBL | Phase 4 (approved) | NR3C1 |
| BETAMETHASONE VALERATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| BUDESONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| BUTOCONAZOLE | ChEMBL | Phase 4 (approved) | NR3C1 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | NR3C1 |
| CANRENONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| CHLORMADINONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| CICLESONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| CLOBETASOL PROPIONATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| CLOFAZIMINE | ChEMBL | Phase 4 (approved) | NR3C1 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | NR3C1 |
| CORTISONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| DANAZOL | ChEMBL | Phase 4 (approved) | NR3C1 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | NR3C1 |
| DEFLAZACORT | ChEMBL | Phase 4 (approved) | NR3C1 |
| DESOGESTREL | ChEMBL | Phase 4 (approved) | NR3C1 |
| DESONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| DESOXIMETASONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| DESOXYCORTICOSTERONE PIVALATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| DEXAMETHASONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| DEXTROTHYROXINE | ChEMBL | Phase 4 (approved) | NR3C1 |
| DIENESTROL | ChEMBL | Phase 4 (approved) | NR3C1 |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | NR3C1 |
| DIFLORASONE DIACETATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| DOXORUBICIN | ChEMBL | Phase 4 (approved) | NR3C1 |
| DROSPIRENONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | NR3C1 |
| EFAVIRENZ | ChEMBL | Phase 4 (approved) | NR3C1 |
| ENZALUTAMIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| EPLERENONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| ESTRADIOL | ChEMBL | Phase 4 (approved) | NR3C1 |
| ESTRIOL | ChEMBL | Phase 4 (approved) | NR3C1 |
| ETHINYL ESTRADIOL | ChEMBL | Phase 4 (approved) | NR3C1 |
| EXEMESTANE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FELODIPINE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUDROCORTISONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUNISOLIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUOCINOLONE ACETONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUOCINONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUOXYMESTERONE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLURANDRENOLIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUTICASONE FUROATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUTICASONE PROPIONATE | ChEMBL | Phase 4 (approved) | NR3C1 |
| GLUCAGON | ChEMBL | Phase 4 (approved) | NR3C1 |
| HALCINONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| HYDROCORTISONE | ChEMBL | Phase 4 (approved) | NR3C1 |
Related Atlas pages
- Genes: NR3C1
- Diseases: acne, eye disorder, hemorrhoid, dry eye syndrome
- Drugs: Fulvestrant, Podofilox, Regorafenib, Acenocoumarol, Alclometasone Dipropionate, Amcinonide, Amiodarone, Aprepitant, Auranofin, Bazedoxifene, Beclomethasone Dipropionate, Benzbromarone, Betamethasone, Betamethasone Dipropionate, Betamethasone Phosphoric Acid, Betamethasone Valerate, Budesonide, Butoconazole, Candesartan Cilexetil, Canrenone, Chlormadinone, Ciclesonide, Clobetasol Propionate, Clofazimine, Clotrimazole, Cortisone, Danazol, Daunorubicin, Deflazacort, Desogestrel, Desonide, Desoximetasone, Desoxycorticosterone Pivalate, Dexamethasone, Dextrothyroxine, Dienestrol, Diethylstilbestrol, Diflorasone Diacetate, Doxorubicin, Drospirenone, Econazole, Efavirenz, Enzalutamide, Eplerenone, Estradiol, Estriol, Ethinyl Estradiol, Exemestane, Felodipine, Fludrocortisone, Flunisolide, Fluocinolone Acetonide, Fluocinonide, Fluoxymesterone, Flurandrenolide, Fluticasone Furoate, Fluticasone Propionate, Glucagon, Halcinonide, Hydrocortisone