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This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C32H44O7
Molecular Weight 540.6876
Optical Activity UNSPECIFIED
Defined Stereocenters 9 / 9
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CICLESONIDE

SMILES

CC(C)C(=O)OCC(=O)[C@@]12O[C@@H](O[C@@H]1C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]23C)C6CCCCC6

InChI

InChIKey=LUKZNWIVRBCLON-GXOBDPJESA-N
InChI=1S/C32H44O7/c1-18(2)28(36)37-17-25(35)32-26(38-29(39-32)19-8-6-5-7-9-19)15-23-22-11-10-20-14-21(33)12-13-30(20,3)27(22)24(34)16-31(23,32)4/h12-14,18-19,22-24,26-27,29,34H,5-11,15-17H2,1-4H3/t22-,23-,24-,26+,27+,29+,30-,31-,32+/m0/s1

HIDE SMILES / InChI
Molecular Formula C32H44O7
Molecular Weight 540.6876
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 9 / 9
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/12054077

Ciclesonide is a glucocorticoid receptor agonist indicated for the treatment of allergic rhinitis (Omnaris nasal spray) and asthma (Alvesco). It was also developed by Byk Gulden for chronic obstructive pulmonary disease (COPD), but no development had been reported for this indication since 1999. Ciclesonide is a pro-drug and rapidly metabolized to C21-desisobutyryl-ciclesonide which is more potent toward GR receptor than the parent drug.

Originator

Approval Year

2006
190
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2752
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8583
OMNARIS

Approved Use

OMNARIS Nasal Spray is indicated for the treatment of nasal symptoms associated with seasonal allergic rhinitis in adults and children 6 years of age and older and for the treatment of nasal symptoms associated with perennial allergic rhinitis in adults and adolescents 12 years of age and older.

Launch Date

2006
Palliative
Approved
8583
OMNARIS

Approved Use

OMNARIS Nasal Spray is indicated for the treatment of nasal symptoms associated with seasonal allergic rhinitis in adults and children 6 years of age and older and for the treatment of nasal symptoms associated with perennial allergic rhinitis in adults and adolescents 12 years of age and older.

Launch Date

2006
Preventing
Approved
8583
ALVESCO

Approved Use

Alvesco is an inhaled corticosteroid indicated for: Maintenance treatment of asthma as prophylactic therapy in adult and adolescent patients 12 years of age and older

Launch Date

2008
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
59.2 nM
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/15139796
0.64 mg single, intravenous
dose: 0.64 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg single, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
4.3 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg 1 times / day multiple, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: MULTIPLE
co-administered:
CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
15.2 ng/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/20110036/
300 μg single, nasal
dose: 300 μg
route of administration: Nasal
experiment type: SINGLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
59.1 ng/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/20110036/
300 μg single, nasal
dose: 300 μg
route of administration: Nasal
experiment type: SINGLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
586.2 ng/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/20110036/
320 μg single, respiratory
dose: 320 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
35.3 ng/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21501692/
282 μg single, nasal
dose: 282 μg
route of administration: Nasal
experiment type: SINGLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
35.84 ng/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21501692/
282 μg 1 times / day multiple, nasal
dose: 282 μg
route of administration: Nasal
experiment type: MULTIPLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.31 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg single, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
DES-CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
0.41 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg 1 times / day multiple, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: MULTIPLE
co-administered:
DES-CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
51 ng × min/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg single, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
62.3 ng × min/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg 1 times / day multiple, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: MULTIPLE
co-administered:
CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
397.5 ng × h/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/20110036/
300 μg single, nasal
dose: 300 μg
route of administration: Nasal
experiment type: SINGLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2685 ng × h/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/20110036/
320 μg single, respiratory
dose: 320 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
260 ng × h/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21501692/
282 μg single, nasal
dose: 282 μg
route of administration: Nasal
experiment type: SINGLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
337.8 ng × h/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21501692/
282 μg 1 times / day multiple, nasal
dose: 282 μg
route of administration: Nasal
experiment type: MULTIPLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
65.4 ng × min/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg single, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
DES-CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
81.4 ng × min/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg 1 times / day multiple, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: MULTIPLE
co-administered:
DES-CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
0.38 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/15139796
0.64 mg single, intravenous
dose: 0.64 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
15 min
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg single, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
13 min
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg 1 times / day multiple, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: MULTIPLE
co-administered:
CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
3.46 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21501692/
282 μg single, nasal
dose: 282 μg
route of administration: Nasal
experiment type: SINGLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4.84 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21501692/
282 μg 1 times / day multiple, nasal
dose: 282 μg
route of administration: Nasal
experiment type: MULTIPLE
co-administered:
DES-CICLESONIDE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
156 min
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg single, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
DES-CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
224 min
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21296519/
400 μg 1 times / day multiple, respiratory
dose: 400 μg
route of administration: Respiratory
experiment type: MULTIPLE
co-administered:
DES-CICLESONIDE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021658s006lbl.pdf
800 μg single, intravenous
dose: 800 μg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
CICLESONIDE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
0.64 mg single, intravenous
Dose: 0.64 mg
Route: intravenous
Route: single
Dose: 0.64 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/15139796
healthy, 27.3 years (range: 19-40 years)
Health Status: healthy
Age Group: 27.3 years (range: 19-40 years)
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/15139796
Sources:
https://pubmed.ncbi.nlm.nih.gov/15139796
6.9 mg single, oral
Dose: 6.9 mg
Route: oral
Route: single
Dose: 6.9 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/15139796
healthy, 27.3 years (range: 19-40 years)
Health Status: healthy
Age Group: 27.3 years (range: 19-40 years)
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/15139796
Sources:
https://pubmed.ncbi.nlm.nih.gov/15139796
640 ug 2 times / day multiple, respiratory
Highest studied dose
Dose: 640 ug, 2 times / day
Route: respiratory
Route: multiple
Dose: 640 ug, 2 times / day
Sources:
accessdata.fda.gov/drugsatfda_docs/nda/2008/021658s000_MedR_P6.pdf
unhealthy, 48.3 years (range: 17-70 years)
Health Status: unhealthy
Age Group: 48.3 years (range: 17-70 years)
Sex: M+F
Sources:
accessdata.fda.gov/drugsatfda_docs/nda/2008/021658s000_MedR_P6.pdf
Sources:
accessdata.fda.gov/drugsatfda_docs/nda/2008/021658s000_MedR_P6.pdf
10 mg single, oral
Highest studied dose
Dose: 10 mg
Route: oral
Route: single
Dose: 10 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021658lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021658lbl.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021658lbl.pdf
282 ug 1 times / day multiple, intranasal
Highest studied dose
Dose: 282 ug, 1 times / day
Route: intranasal
Route: multiple
Dose: 282 ug, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202129Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202129Orig1s000MedR.pdf
Disc. AE: Burning sensation...
AEs leading to
discontinuation/dose reduction:
Burning sensation (severe, 1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202129Orig1s000MedR.pdf
2880 ug single, respiratory
Highest studied dose
Dose: 2880 ug
Route: respiratory
Route: single
Dose: 2880 ug
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021658lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021658lbl.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021658lbl.pdf
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Other AEs: Lobar pneumonia, Asthma...
Other AEs:
Lobar pneumonia (serious, 1 patient)
Asthma (serious, 1 patient)
Pyrexia (below serious, 6 patients)
Ear infection (below serious, 5 patients)
Pharyngitis (below serious, 5 patients)
Rhinitis (below serious, 4 patients)
Upper respiratory tract infection (below serious, 18 patients)
Cough (below serious, 6 patients)
Allergic rhinitis (below serious, 7 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Other AEs: Laryngitis, Epistaxis...
Other AEs:
Laryngitis (serious, 1 patient)
Epistaxis (serious, 1 patient)
Myringoplasty (serious, 1 patient)
Ear infection (below serious, 3 patients)
Influenza (below serious, 6 patients)
Lower respiratory tract infection (below serious, 4 patients)
Upper respiratory tract infection (below serious, 19 patients)
Cough (below serious, 4 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
Other AEs: Cough, Asthenia...
Other AEs:
Cough (below serious, 2 patients)
Asthenia (below serious, 1 patient)
Chest pain (below serious, 1 patient)
Decreased activity (below serious, 1 patient)
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
AEs

AEs

AESignificanceDosePopulation
Burning sensation severe, 1 patient
Disc. AE
282 ug 1 times / day multiple, intranasal
Highest studied dose
Dose: 282 ug, 1 times / day
Route: intranasal
Route: multiple
Dose: 282 ug, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202129Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202129Orig1s000MedR.pdf
Upper respiratory tract infection below serious, 18 patients
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Rhinitis below serious, 4 patients
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Ear infection below serious, 5 patients
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Pharyngitis below serious, 5 patients
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Cough below serious, 6 patients
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Pyrexia below serious, 6 patients
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Allergic rhinitis below serious, 7 patients
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Asthma serious, 1 patient
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Lobar pneumonia serious, 1 patient
100 ug 1 times / day steady, respiratory
Dose: 100 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 100 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Upper respiratory tract infection below serious, 19 patients
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Ear infection below serious, 3 patients
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Cough below serious, 4 patients
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Lower respiratory tract infection below serious, 4 patients
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Influenza below serious, 6 patients
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Epistaxis serious, 1 patient
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Laryngitis serious, 1 patient
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Myringoplasty serious, 1 patient
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
unhealthy, children
Health Status: unhealthy
Age Group: children
Sources:
https://clinicaltrials.gov/ct2/show/NCT00163293
Asthenia below serious, 1 patient
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
Chest pain below serious, 1 patient
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
Decreased activity below serious, 1 patient
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
Cough below serious, 2 patients
200 ug 1 times / day steady, respiratory
Dose: 200 ug, 1 times / day
Route: respiratory
Route: steady
Dose: 200 ug, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT02155881
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252

inducer
1087
inhibitor
2438

inducer
440
substrate
1388

inhibitor
2507

inducer
109

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2A6
879

CYP2C19
2057

CYP2E1
1060

P-gp
1741

BCRP
910

CYP2B6
926

CYP2C8
1057
CYP2C8
810

CYP4A11
137

P-gp
2052
CYP1A2
832

CYP2A6
86

CYP2C19
329

CYP2E1
131

P-gp
301
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
2333
 no
CYP1A2
2333
 no
CYP2A6
911
 no
CYP2A6
911
 no
CYP2B6
1160
 no
CYP2C19
2141
 no
CYP2C8
1117
 no
CYP2C9
2497
 no
CYP2D6
2546
 no
CYP2E1
1146
 no
CYP2E1
1146
 no
CYP3A4
2633
 no
CYP3A4
2633
 yes [IC50 0.734 uM]
CYP2D6
2546
 yes [IC50 2.4 uM]
CYP2C19
2141
 yes [Inhibition 3 uM]
CYP2C9
2497
 yes [Inhibition 3 uM]
BCRP
985
 yes
P-gp
1932
 yes
P-gp
1932
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
P-gp
2052
 inconclusive
CYP2C8
810
 minor
CYP2C8
810
 yes
RM1
1
CYP2D6
1388
 yes
CYP2D6
1388
 yes
RM1
1
CYP3A4
1946
 yes
RM1
1
CYP4A11
137
 yes
CYP4A11
137
 yes
RM1
1
CYP3A4
1946
 yes
yes (co-administration study)
Comment: ketoconazole increased ciclesonide AUC by 3.6-fold
Page: 8.0
Sourcing

Sourcing

Vendor/AggregatorIDURL
Achemtek
0104-021585
http://www.achemtek.com/126544-47-6
AHH Chemical co.,ltd
MT-49256
http://www.ahhchemical.com/product/MT-49256.html
AK Scientific, Inc. (AKSCI)
O945
http://www.aksci.com/item_detail.php?cat=O945
Alfa Chemistry
AP126544476
https://reagents.alfa-chemistry.com/product/ciclesonide-cas-126544-47-6-3410.html
Aurora Fine Chemicals LLC
A24.076.552
http://online.aurorafinechemicals.com/info?ID=A24.076.552
AvaChem Scientific
2479
http://www.avachem.com/productSearch.asp?2479
BioCrick
BCC5234
http://www.biocrick.com/Ciclesonide-BCC5234.html
Boerchem
BC220461
http://www.boerchem.com/?product_37265.html
Chem Scene
CS-2867
http://www.chemscene.com/126544-47-6.html
ChemFish Tokyo co.,ltd
6918155
http://www.chemfish.co.jp/index.php?id=3940&project=product
ChemMol
2100025
http://www.chemmol.com/chemmol/2100025.html
ChemMol
30108640
http://www.chemmol.com/chemmol/30108640.html
ChemMol
44006350
http://www.chemmol.com/chemmol/44006350.html
Chemspace
CSSB00000053551
https://chem-space.com/CSSB00000053551
eNovation Chemicals
D673908
https://www.enovationchem.com/ProductDetails.asp?ProductID=D673908
eNovation Chemicals
D762250
https://www.enovationchem.com/ProductDetails.asp?ProductID=D762250
eNovation Chemicals
Y0974262
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0974262
Excenen
EX-A4195
https://www.excenen.com/searchresultlist.php?id=EX-A4195
Hairui
HR125043
http://www.hairuichem.com/en/product/141845-82-1.html
Lab Network
LN01266864
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01266864
LGC Standards
DRE-A11666300AL-100
https://www.lgcstandards.com/US/en/p/DRE-A11666300AL-100
LGC Standards
DRE-C11666300
https://www.lgcstandards.com/US/en/p/DRE-C11666300
LGC Standards
MM3608.00
https://www.lgcstandards.com/US/en/p/MM3608.00
MedChem Express
HY-B0625
https://www.medchemexpress.com/Ciclesonide.html
OChem
1944
http://www.ocheminc.com/index.php?act=psearch&pid=544C476
Selleck Chemicals
S4646
http://www.selleckchem.com/products/ciclesonide.html
Sigma-Aldrich
SML1955_SIGMA
https://www.sigmaaldrich.com/catalog/product/sigma/sml1955?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
Y0001553_SIAL
https://www.sigmaaldrich.com/catalog/product/sial/y0001553?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Tocris
6357
https://www.tocris.com/products/ciclesonide_6357
Yuhao Chemical
LQ5489
http://www.chemyuhao.com/126544-47-6.html
PubMed

PubMed

TitleDatePubMed
Formation of fatty acid conjugates of ciclesonide active metabolite in the rat lung after 4-week inhalation of ciclesonide.
2005
[Ciclesonide in the treatment of patients with bronchial asthma].
2005 Dec
Once-daily ciclesonide improves lung function and is well tolerated by patients with mild-to-moderate persistent asthma.
2005 Dec
Comparison of the efficacy of ciclesonide 160 microg QD and budesonide 200 microg BID in adults with persistent asthma: a phase III, randomized, double-dummy, open-label study.
2005 Nov
Gateways to clinical trials.
2005 Oct
[Ciclesonide -- a new inhaled corticosteroid].
2005 Oct
Identification of enzymes involved in phase I metabolism of ciclesonide by human liver microsomes.
2005 Oct-Dec
Gateways to clinical trials.
2005 Sep
Ciclesonide, a novel inhaled steroid, does not affect hypothalamic-pituitary-adrenal axis function in patients with moderate-to-severe persistent asthma.
2005 Sep
Equivalent pharmacokinetics of the active metabolite of ciclesonide with and without use of the AeroChamber Plus spacer for inhalation.
2006
Comparable efficacy of ciclesonide once daily versus fluticasone propionate twice daily in asthma.
2006
Gateways to clinical trials.
2006 Apr
Safety, tolerability, and exposure of ciclesonide nasal spray in healthy and asymptomatic subjects with seasonal allergic rhinitis.
2006 Apr
[AIDA--results of a large post-marketing product surveillance study of maintenance asthma therapy with once-daily ciclesonide].
2006 Apr 6
The systemic safety of inhaled corticosteroid therapy: a focus on ciclesonide.
2006 Aug
Modulation of p-glycoprotein and breast cancer resistance protein by some prescribed corticosteroids.
2006 Feb 15
[In persistent asthma always think of antiinflammatory agents. Inhaled corticoids as basic medication in guideline specified asthma therapy].
2006 Jan 19
Gateways to clinical trials.
2006 Jan-Feb
Developing the ideal inhaled corticosteroid.
2006 Jul
Gateways to clinical trials.
2006 Jul-Aug
A multinational, 12-week, randomized study comparing the efficacy and tolerability of ciclesonide and budesonide in patients with asthma.
2006 Jun
Gateways to clinical trials.
2006 Jun
Inhaled ciclesonide versus inhaled budesonide or inhaled beclomethasone or inhaled fluticasone for chronic asthma in adults: a systematic review.
2006 Jun 5
Pharmacologic characteristics and adrenal suppression with newer inhaled corticosteroids: A comparison of ciclesonide and fluticasone propionate.
2006 Mar
Gateways to clinical trials.
2006 Mar
Once-daily ciclesonide in children: efficacy and safety in asthma.
2006 Mar
High lung deposition of 99mTc-labeled ciclesonide administered via HFA-MDI to patients with asthma.
2006 Mar
[The optimal dosing times of corticoids].
2006 Mar-Apr
Ciclesonide reduces the need for oral steroid use in adult patients with severe, persistent asthma.
2006 May
Ciclesonide inhalation aerosol for persistent asthma.
2006 May
Effect of ciclesonide dose and duration of therapy on exercise-induced bronchoconstriction in patients with asthma.
2006 May
Anti-inflammatory effects of once daily low dose inhaled ciclesonide in mild to moderate asthmatic patients.
2006 May
In Vitro metabolism of ciclesonide in human lung and liver precision-cut tissue slices.
2006 May
Comparative efficacy of once-daily ciclesonide and budesonide in the treatment of persistent asthma.
2006 May
Inhaled corticosteroids in the treatment of respiratory allergy: safety vs. efficacy.
2006 Nov
Efficacy and safety of ciclesonide nasal spray for the treatment of seasonal allergic rhinitis.
2006 Nov
Effects of inhaled ciclesonide on circulating T-helper type 1/T-helper type 2 cells in atopic asthmatics after allergen challenge.
2006 Nov
Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma.
2006 Nov
Ciclesonide disposition and metabolism: pharmacokinetics, metabolism, and excretion in the mouse, rat, rabbit, and dog.
2006 Nov-Dec
Gateways to clinical trials.
2006 Oct
The newly developed inhaled corticosteroid ciclesonide for the treatment of asthma.
2006 Oct
A comparative study of inhaled ciclesonide 160 microg/day and fluticasone propionate 176 microg/day in children with asthma.
2006 Oct
Gateways to clinical trials.
2006 Sep
Effect of ciclesonide and fluticasone on exhaled nitric oxide in patients with mild allergic asthma.
2006 Sep
Two-dimensional and three-dimensional imaging show ciclesonide has high lung deposition and peripheral distribution: a nonrandomized study in healthy volunteers.
2006 Summer
Ciclesonide is more effective than budesonide in the treatment of persistent asthma.
2007
Safety of inhaled corticosteroids: room for improvement.
2007
The treatment of asthma in children: inhaled corticosteroids.
2007
In vitro metabolism of ciclesonide in human nasal epithelial cells.
2007 Jan
In vitro activation of the corticosteroid ciclesonide in animal nasal mucosal homogenates.
2007 Mar
Patents

Patents

08158780
1
JP2005539044A
11
JP2006501253A
6
JP2006526624A
22
JP2007262064A
2
JP2007500147A
8
JP2007500150A
28
JP2007501194A
4
JP2007507270A
5
JP2007513165A
55
JP2007517067A
31
JP2007518817A
5
JP2007520508A
6
JP2009534333A
15
JP2010506837A
76
JP2011021043A
1
JP2011528355A
29
JP2013542940A
4
JP4589928B2
9
JP4746318B2
18
JP4746535B2
1
JP4792032B2
112
JP5371189B2
1

Sample Use Guides

In Vivo Use Guide
Allergic rhinitis: The recommended dose of ciclesonide (in form of Omnaris Nasal Spray) is 200 ug per day administered as 2 sprays (50 mcg/spray) in each nostril once daily. Asthma: 80-320 ug twice daily.
Route of Administration: Other
In Vitro Use Guide
Ciclesonide at 10(-12)–10(-5) M significantly inhibited TNF-alpha stimulated MCP-1 production in human airway smooth muscle cells. IL1-stimulated MCP-1 release was also significantly inhibited in a concentration-dependent (10(-12)–10(-5) M) manner.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:28:48 GMT 2025
Edited
by admin
on Mon Mar 31 18:28:48 GMT 2025
Record UNII
S59502J185
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CICLESONIDE
INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
ALVESCO
Preferred Name English
CICLESONIDE [EP MONOGRAPH]
Common Name English
ciclesonide [INN]
Common Name English
CICLESONIDE [MI]
Common Name English
CICLESONIDE [MART.]
Common Name English
(11?,16?)-16,17-[[(R)-Cyclohexylmethylene]bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)pregna-1,4-diene-3,20-dione
Systematic Name English
OMNARIS
Brand Name English
PREGNA-1,4-DIENE-3,20-DIONE, 16,17-(((R)-CYCLOHEXYLMETHYLENE)BIS(OXY))-11-HYDROXY-21-(2-METHYL-1-OXOPROPOXY)-, (11.BETA.,16.ALPHA.)
Common Name English
CICLESONIDE [ORANGE BOOK]
Common Name English
BI54903
Code English
CICLESONIDE [VANDF]
Common Name English
ZETONNA
Brand Name English
RPR-251526
Code English
CICLESONIDE [JAN]
Common Name English
Ciclesonide [WHO-DD]
Common Name English
RPR251526
Code English
CICLESONIDE [USAN]
Common Name English
Classification Tree Code System Code
WHO-ATC R03BA08
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
WHO-ATC R01AD13
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
NCI_THESAURUS C521
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
WHO-VATC QR03BA08
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
WHO-VATC QR01AD13
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
Code System Code Type Description
USAN
PP-61
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
DAILYMED
S59502J185
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
MERCK INDEX
m3536
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY Merck Index
ChEMBL
CHEMBL2040682
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
DRUG CENTRAL
633
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
WIKIPEDIA
CICLESONIDE
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
INN
6546
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
NCI_THESAURUS
C65326
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
CAS
126544-47-6
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
PUBCHEM
6918155
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
FDA UNII
S59502J185
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
EVMPD
SUB06236MIG
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
MESH
C120481
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
LACTMED
Ciclesonide
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
EPA CompTox
DTXSID9046659
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
SMS_ID
100000081904
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
DRUG BANK
DB01410
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
CAS
141845-82-1
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
ALTERNATIVE
IUPHAR
7469
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY
RXCUI
274964
Created by admin on Mon Mar 31 18:28:48 GMT 2025 , Edited by admin on Mon Mar 31 18:28:48 GMT 2025
PRIMARY RxNorm
Related Record Type Details
GLUCOCORTICOID RECEPTOR
TARGET -> AGONIST
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
CYTOCHROME P450 2D6
METABOLIC ENZYME -> SUBSTRATE
MINOR
Related Record Type Details
Structure of DES-CICLESONIDE
METABOLITE ACTIVE -> PRODRUG
Des-ciclesonide has anti-inflammatory activity with affinity for the glucocorticoid receptor that is 120 times higher than the parent compound.
Related Record Type Details
Structure of DES-CICLESONIDE
IMPURITY -> PARENT
Structure of Ciclesonide, (S)-
IMPURITY -> PARENT
Structure of (2?R)-2?-[(1RS)-cyclohex-3-enyl]-11?-hydroxy-3,20-dioxo-16?H-[1,3]dioxolo[4?,5?:16,17]pregna-1,4-dien-21-yl 2-methylpropanoate
IMPURITY -> PARENT
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

ORAL BIOAVAILABILITY PHARMACOKINETIC
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