Flunisolide
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Also known as AerobidAerospanAerospan hfaFlunisolidaFlunisolide anhydrousFlunisolide hemihydrateNasalideNasarelNSC-757871RS-3999SyntarisSyntaris hayfeverSID56322914SID56463079SID170465331SID144204276C0164996
Summary
Flunisolide (CHEMBL1512) is an approved small-molecule immunosuppressive agent (ATC R01AD04) targeting NR3C1; indicated across 5 conditions including obstructive lung disease and rhinitis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R01AD04 (+1 more)
- Targets: 1 (NR3C1)
- Indications: 5 conditions
- Clinical trials: 1
- Chemistry: 434.5 Da · C24H31FO6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1512 |
| Name | Flunisolide |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 82153 |
| ChEBI | CHEBI:5106 |
| ATC | R01AD04, R03BA03 |
| Molecular formula | C24H31FO6 |
| Molecular weight | 434.5 |
| InChIKey | XSFJVAJPIHIPKU-XWCQMRHXSA-N |
SMILES: C[C@]12C[C@@H]([C@H]3[C@H]([C@@H]1C[C@@H]4[C@]2(OC(O4)(C)C)C(=O)CO)C[C@@H](C5=CC(=O)C=C[C@]35C)F)O
IUPAC name: (1S,2S,4R,8S,9S,11S,12S,13R,19S)-19-fluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one
Pharmacological roles (ChEBI): immunosuppressive agent, anti-inflammatory drug, anti-asthmatic drug.
Also known as: Aerobid, Aerospan, Aerospan hfa, Flunisolida, Flunisolide, Flunisolide anhydrous, Flunisolide hemihydrate, Nasalide, Nasarel, NSC-757871, RS-3999, Syntaris
Patent coverage: 9,921 distinct patent families (42,177 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 | 8.62 | 0.9% | P04150 |
Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Alpha-2A adrenergic receptor, Glucocorticoid receptor, Progesterone receptor, 5-hydroxytryptamine receptor 1A, Alpha-1A adrenergic receptor, Bile salt export pump.
Bioactivity
ChEMBL activities: 7 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| NR3C1 | 8.62 | Ki | 2.42 | nM | CHEMBL_ACT_7669861 |
| NR3C1 | 8.27 | IC50 | 5.33 | nM | CHEMBL_ACT_7669860 |
| NR3C1 | 7.68 | AC50 | 21 | nM | CHEMBL_ACT_25116106 |
| ADRA1A | 7.32 | AC50 | 48 | nM | CHEMBL_ACT_25217740 |
| HTR1A | 6.25 | AC50 | 560 | nM | CHEMBL_ACT_25215673 |
| PGR | 6.19 | AC50 | 640 | nM | CHEMBL_ACT_25222671 |
| ADRA2A | 5.7 | AC50 | 2000 | nM | CHEMBL_ACT_25219443 |
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
5 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 |
|---|---|---|---|
| obstructive lung disease | 4 | MONDO:0002267 | HP:0006536 |
| rhinitis | 4 | MONDO:0003014 | EFO:0008521 |
| asthma | 4 | MONDO:0004979 | MONDO:0004979 |
| perennial allergic rhinitis | 3 | MONDO:0024332 | EFO:1001417 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 1.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00346775 | PHASE3 | COMPLETED | Validation Of Preference Module Of Experience With Allergic Rhinitis Nasal Sprays Questionnaire (EARNS-Q) |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
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 |
| FLUOCINOLONE ACETONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUOCINONIDE | ChEMBL | Phase 4 (approved) | NR3C1 |
| FLUOROMETHOLONE | 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: obstructive lung disease, rhinitis, asthma, perennial allergic rhinitis
- 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, Fluocinolone Acetonide, Fluocinonide, Fluorometholone, Fluoxymesterone, Flurandrenolide, Fluticasone Furoate, Fluticasone Propionate, Glucagon, Halcinonide, Hydrocortisone