Ciclesonide

Summary

Ciclesonide (CHEMBL2040682) is an approved small molecule (ATC R03BA08) targeting NR3C1; indicated across 11 conditions including allergic rhinitis and seasonal allergic rhinitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R03BA08 (+1 more)
• Targets: 1 (NR3C1)
• Indications: 11 conditions
• Clinical trials: 56
• Chemistry: 540.7 Da · C32H44O7

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2040682
Name	Ciclesonide
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	6918155
ATC	R03BA08, R01AD13
Molecular formula	C32H44O7
Molecular weight	540.7
InChIKey	LUKZNWIVRBCLON-GXOBDPJESA-N

SMILES: CC(C)C(=O)OCC(=O)[C@@]12[C@@H](C[C@@H]3[C@@]1(C[C@@H]([C@H]4[C@H]3CCC5=CC(=O)C=C[C@]45C)O)C)O[C@H](O2)C6CCCCC6

IUPAC name: [2-[(1S,2S,4R,6R,8S,9S,11S,12S,13R)-6-cyclohexyl-11-hydroxy-9,13-dimethyl-16-oxo-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-8-yl]-2-oxoethyl] 2-methylpropanoate

Also known as: Alvesco, Alvesco 160, Alvesco 80, Aservo equihaler, BI54903, Ciclesonida, Ciclesonide, Omnaris, RPR-251526, RPR251526, Zetonna, CICLESONIDE

Patent coverage: 5,159 distinct patent families (21,189 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	7.43	0.9%	P04150

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Glucocorticoid receptor, Progesterone receptor, Cannabinoid receptor 1, Kappa-type opioid receptor, Adenosine receptor A3, Androgen receptor, Nuclear receptor subfamily 1 group I member 2.

Bioactivity

ChEMBL activities: 8 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
NR3C1	8.7	IC50	2	nM	CHEMBL_ACT_25523050
NR3C1	7.66	EC50	22	nM	CHEMBL_ACT_25523058
NR3C1	7.54	AC50	29	nM	CHEMBL_ACT_25175708
P15207	5.58	AC50	2600	nM	CHEMBL_ACT_25187362
ADORA3	5.38	AC50	4200	nM	CHEMBL_ACT_25134053
PGR	5.15	AC50	7100	nM	CHEMBL_ACT_25222922
NR1I2	5.04	AC50	9100	nM	CHEMBL_ACT_25188075
OPRK1	5.01	AC50	9718	nM	CHEMBL_ACT_25129286

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

11 indications (6 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
allergic rhinitis	4	MONDO:0011786	EFO:0005854
seasonal allergic rhinitis	4	MONDO:0005324	EFO:0003956
obstructive lung disease	4	MONDO:0002267	HP:0006536
perennial allergic rhinitis	4	MONDO:0024332	EFO:1001417
asthma	4	MONDO:0004979	MONDO:0004979
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
chronic rhinosinusitis	3	MONDO:0006031	EFO:1000024
allergic disease	3	MONDO:0005271	MONDO:0005271
respiratory system disorder	3	MONDO:0005087	EFO:0000684
chronic obstructive pulmonary disease	2	MONDO:0005002	EFO:0000341

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 56.

Phase distribution

Phase	Trials
PHASE3	39
PHASE4	8
PHASE2/PHASE3	3
PHASE2	3
Not specified	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00404547	PHASE4	COMPLETED	Asthma Care With Alvesco® (Ciclesonide) in Primary Care in Adults - The ACCEPT-study (BY9010/CA-102)
NCT00458835	PHASE4	COMPLETED	Comparison Between Systemic Exposure to Ciclesonide Nasal Spray, Ciclesonide HFA Nasal Aerosol and Orally Inhaled Ciclesonide (BY9010/M1-422)
NCT00826969	PHASE4	COMPLETED	Ciclesonide for the Treatment of Airway Hyperresponsiveness
NCT01171365	PHASE4	COMPLETED	Small Particle Steroids in Refractory Asthma
NCT01333800	PHASE4	COMPLETED	Cost-effectiveness Study of Beclomethasone Versus Ciclesonide as Controller Medications in Pediatric Asthma
NCT01430260	PHASE4	COMPLETED	Omnaris Versus Levocetirizine Phase 4 Study
NCT01550471	PHASE4	COMPLETED	Sunovion Growth Study Pediatric Subjects With Mild Asthma & Allergic Rhinitis
NCT03839433	PHASE4	COMPLETED	The Mannitol-Asthma-Ciclesonide-Study
NCT00163293	PHASE3	COMPLETED	Efficacy of Ciclesonide Inhaled Once Daily Versus Other Corticosteroids Used for Treatment of Mild Asthma in Children (4 to 11 Years) (BY9010/CA-101)
NCT00163319	PHASE3	COMPLETED	Efficacy of Ciclesonide and Fluticasone Propionate in Adult Patients With Moderate and Severe Persistent Asthma (18 to 75 y) (BY9010/IT-101)
NCT00163332	PHASE3	COMPLETED	Effect of Inhaled Ciclesonide Versus Fluticasone Propionate in Patients With Mild to Moderate Asthma (18 to 65 y) (BY9010/M1-129)
NCT00163345	PHASE3	COMPLETED	Efficacy of Ciclesonide on Small Airways in Patients With Stable Asthma (18 to 60 y) (BY9010/M1-131)
NCT00163358	PHASE3	COMPLETED	Efficacy of Ciclesonide vs Fixed Combination of Fluticasone Propionate/Salmeterol vs Placebo in Patients With Mild Persistent Asthma (12 to 75 y) (BY9010/M1-132)
NCT00163371	PHASE3	COMPLETED	Effects of Inhaled Ciclesonide Versus Fluticasone Propionate Versus Placebo on Lower Leg Growth in Prepubertal Children With Mild Persistent Asthma (6 to 12 y) (BY9010/M1-208)
NCT00163384	PHASE3	COMPLETED	Effectiveness of Ciclesonide Versus Budesonide in Patients With Asthma (18 to 75 y) (BY9010/M1-136)
NCT00163397	PHASE3	COMPLETED	Efficacy of Ciclesonide Versus Budesonide in Patients With Asthma (18 to 75 y) (BY9010/M1-137)
NCT00163410	PHASE3	COMPLETED	Efficacy of Ciclesonide Inhaled Once Daily Versus Fluticasone Propionate Inhaled Twice Daily in Children With Asthma (4 to 15 y) (BY9010/M1-205)
NCT00163423	PHASE3	COMPLETED	Efficacy of Ciclesonide Versus Fluticasone Propionate in Patients With Mild to Moderate Asthma (12 to 75 y) (BY9010/M1-142)
NCT00163436	PHASE3	COMPLETED	Efficacy and Safety of Ciclesonide Administered With or Without Different Spacers in Patients With Asthma (12 to 75 y) (BY9010/M1-145)
NCT00163449	PHASE3	COMPLETED	Efficacy and Safety of Ciclesonide in Preschool Children With Asthma (2 to 6 Years) (BY9010/M1-207)
NCT00163462	PHASE3	COMPLETED	Efficacy of Ciclesonide Inhaled Once Daily Versus Fluticasone Propionate Inhaled Twice Daily in Children With Asthma (6 to 11 y) (BY9010/M1-206)
NCT00163488	PHASE3	COMPLETED	Safety of Ciclesonide Nasal Spray Administered With Inhaled Fluticasone Dipropionate/Salmeterol in Adults With Perennial Allergic Rhinitis (BY9010/M1-409)
NCT00163501	PHASE3	COMPLETED	Safety and Effectiveness of Ciclesonide Nasal Spray in Patients With Perennial Allergic Rhinitis During One Year Treatment (BY9010/M1-404)
NCT00163514	PHASE3	COMPLETED	Safety and Effectiveness of Ciclesonide Nasal Spray in Children (6 to 11 Years) With Perennial Allergic Rhinitis (BY9010/M1-403)
NCT00174720	PHASE3	COMPLETED	Efficacy of Ciclesonide vs Placebo Administered as Once Daily or Twice Daily in Patients Not Treated With Inhaled Corticosteroid.
NCT00174733	PHASE3	COMPLETED	Efficacy of Ciclesonide Versus Placebo Administered Either as Once Daily or Twice Daily in Patients Treated Previously With an Inhaled Corticosteroid
NCT00254956	PHASE3	COMPLETED	Effects Of Ciclesonide And Beclomethasone On Lens Opacification In Adult Subjects With Moderate To Severe Persistent Asthma
NCT00261287	PHASE3	COMPLETED	Safety and Tolerability of Ciclesonide Nasal Spray in Patients With Perennial Allergic Rhinitis (2-5 Years Old) (BY9010/M1-416)
NCT00270348	PHASE3	COMPLETED	Effects of Ciclesonide MDI 50mg/Day and 200mg/Day (Ex-Valve) Once-Daily on Growth in Children With Mild Persistent Asthma
NCT00305461	PHASE3	COMPLETED	Effect of Ciclesonide on Quality of Life in Patients With Moderate Persistent Asthma (21 to 65 y) (BY9010/AR-101)
NCT00306163	PHASE3	COMPLETED	Responsiveness of Lower Airways in Adult Patients (18-60 Years) With Stable Asthma After Treatment With Ciclesonide and Fluticasone Propionate (BY9010/NL-101)
NCT00384189	PHASE3	COMPLETED	A Comparative Study of Inhaled Ciclesonide Versus Placebo in Children (6-11 Years) With Asthma
NCT00392288	PHASE3	COMPLETED	Efficacy and Safety of Ciclesonide (CIC) Administered Twice Daily in Pediatric Patients With Asthma.
NCT00525772	PHASE3	COMPLETED	Effect of Ciclesonide on Exercise Induced Bronchoconstriction
NCT00546520	PHASE3	COMPLETED	Effect of Inhaled Ciclesonide in Adult Patients With Asthma (BY9010/M1-125)
NCT00658918	PHASE3	COMPLETED	To Assess the Safety of Ciclesonide, Applied as a Nasal Spray at Three Dose Levels, in the Treatment of Perennial Allergic Rhinitis in Pediatrics (BY9010/M1-405)
NCT00659048	PHASE3	COMPLETED	Investigation of Potential Additive Inhibitory Effects on HPA-Axis of Ciclesonide Nasal Spray When Administered Concomitantly With Orally Inhaled Beclomethasone Dipropionate (HFA-BDP) in Patients With Perennial Allergic Rhinitis (PAR) (BY9010/M1-408)
NCT00659503	PHASE3	COMPLETED	Study Using the Environmental Exposure Unit (EEU) to Assess the Onset of Action of Ciclesonide, Applied as a Nasal Spray in the Treatment of Seasonal Allergic Rhinitis (BY9010/M1-407)
NCT00659594	PHASE3	COMPLETED	Study Using the Environmental Exposure Chamber (EEC) to Assess the Onset of Action of Ciclesonide, Applied as a Nasal Spray in Treatment of Seasonal Allergic Rhinitis (BY9010/M1-406)
NCT00659750	PHASE3	COMPLETED	To Assess the Safety and Efficacy of Ciclesonide Applied as a Nasal Spray in the Treatment of Perennial Allergic Rhinitis (BY9010/M1-402)

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

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
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
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