ciclesonide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
steroids for topical use, acetal derivatives 633 126544-47-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ciclesonide
  • omnaris
  • alvesco
nasal spray approved for seasonal and perennial allergic rhinitis
  • Molecular weight: 540.70
  • Formula: C32H44O7
  • CLOGP: 5.25
  • LIPINSKI: 2
  • HAC: 7
  • HDO: 1
  • TPSA: 99.13
  • ALOGS: -5.54
  • ROTB: 6

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 mg N
0.16 mg Inhal.aerosol

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.00 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 1 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 2.90 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 33.30 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.04 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Oct. 20, 2006 FDA TAKEDA GMBH

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Asthma 796.57 69.32 136 152 11178 2346619
Obstructive airways disorder 338.59 69.32 50 238 1323 2356474
Dyspnoea 306.32 69.32 90 198 78643 2279154
Wheezing 261.82 69.32 50 238 6334 2351463
Blood count abnormal 240.86 69.32 40 248 2242 2355555
Cough 213.24 69.32 57 231 33060 2324737
Therapeutic product effect incomplete 136.26 69.32 32 256 10499 2347298
Blood test abnormal 103.16 69.32 18 270 1300 2356497
Sleep apnoea syndrome 100.88 69.32 19 269 2107 2355690
Productive cough 100.02 69.32 22 266 5299 2352498
Drug ineffective 97.11 69.32 42 246 101582 2256215
Limb injury 79.47 69.32 16 272 2494 2355303
Sputum discoloured 78.34 69.32 14 274 1152 2356645
Wound 78.14 69.32 16 272 2712 2355085
Chest discomfort 77.97 69.32 22 266 14573 2343224

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Asthma 471.05 73.03 76 84 4828 1741793
Obstructive airways disorder 293.16 73.03 42 118 1032 1745589
Cough 177.54 73.03 43 117 19154 1727467
Blood count abnormal 174.12 73.03 28 132 1429 1745192
Wheezing 151.12 73.03 29 131 4124 1742497
Therapeutic product effect incomplete 131.27 73.03 27 133 5421 1741200
Dyspnoea 105.82 73.03 36 124 52023 1694598
Drug ineffective 87.27 73.03 33 127 63768 1682853
Pulmonary function test decreased 85.59 73.03 13 147 433 1746188
Hypoxia 83.49 73.03 19 141 5944 1740677
Asthma-chronic obstructive pulmonary disease overlap syndrome 82.50 73.03 9 151 14 1746607
Sputum discoloured 80.16 73.03 13 147 664 1745957

Pharmacologic Action:

SourceCodeDescription
ATC R01AD13 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Corticosteroids
ATC R03BA08 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Glucocorticoids
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D005938 Glucocorticoids
MeSH PA D006728 Hormones

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Allergic rhinitis indication 61582004
Asthma indication 195967001 DOID:2841
Seasonal allergic rhinitis indication 367498001
Asthma management indication 406162001
Severe chronic obstructive pulmonary disease off-label use 313299006
Mycosis contraindication 3218000 DOID:1564
Ocular hypertension contraindication 4210003 DOID:9282
Inactive tuberculosis contraindication 11999007
Epistaxis contraindication 12441001
Disease caused by parasite contraindication 17322007
Glaucoma contraindication 23986001 DOID:1686
Acute tuberculosis contraindication 25629007
Osteoporosis contraindication 64859006 DOID:11476
Operation on nose contraindication 88733004
Bilateral cataracts contraindication 95722004
Ophthalmic herpes simplex contraindication 186542001
Osteopenia contraindication 312894000
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Nasal Candidiasis contraindication
Oropharyngeal Candidiasis contraindication
Nasal Trauma contraindication
Uncontrolled Bacterial Infections contraindication
Nasal Septal Ulcers contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.78 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.08MG/INH ALVESCO COVIS PHARMA BV N021658 Jan. 10, 2008 RX AEROSOL, METERED INHALATION 8371292 Feb. 1, 2028 MAINTENANCE TREATMENT OF ASTHMA AS PROPHYLACTIC THERAPY IN ADULT AND ADOLESCENT PATIENTS 12 YEARS OF AGE AND OLDER. PATENT CLAIMS METHOD FOR TREATING A RESPIRATORY DISEASE IN A CHILD
0.16MG/INH ALVESCO COVIS PHARMA BV N021658 Jan. 10, 2008 RX AEROSOL, METERED INHALATION 8371292 Feb. 1, 2028 MAINTENANCE TREATMENT OF ASTHMA AS PROPHYLACTIC THERAPY IN ADULT AND ADOLESCENT PATIENTS 12 YEARS OF AGE AND OLDER. PATENT CLAIMS METHOD FOR TREATING A RESPIRATORY DISEASE IN A CHILD
0.05MG/INH OMNARIS COVIS PHARMA BV N022004 Oct. 20, 2006 RX SPRAY, METERED NASAL 8371292 Feb. 1, 2028 TREATMENT OF NASAL SYMPTOMS ASSOCIATED WITH SEASONAL ALLERGIC RHINITIS IN ADULTS AND CHILDREN 6 YEARS OF AGE AND OLDER. TREATMENT OF NASAL SYMPTOMS ASSOCIATED W PERENNIAL ALLERGIC RHINITIS IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER
0.037MG/INH ZETONNA COVIS PHARMA BV N202129 Jan. 20, 2012 RX AEROSOL, METERED NASAL 8371292 Feb. 1, 2028 TREATMENT OF SYMPTOMS ASSOCIATED WITH SEASONAL AND PERENNIAL ALLERGIC RHINITIS IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER. PATENT CLAIMS METHODS FOR TREATING A RESPIRATORY DISEASE IN A CHILD

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glucocorticoid receptor Nuclear hormone receptor AGONIST Ki 7.43 WOMBAT-PK CHEMBL
SARS-CoV-2 Virus INHIBITOR IC50 5.36 SCIENTIFIC LITERATURE

External reference:

IDSource
4027427 VUID
N0000179737 NUI
C0907850 UMLSCUI
D01703 KEGG_DRUG
416739001 SNOMEDCT_US
417420004 SNOMEDCT_US
274964 RXNORM
19358 MMSL
d05465 MMSL
4027427 VANDF
008829 NDDF
S59502J185 UNII
6546 INN_ID
DB01410 DRUGBANK_ID
CHEBI:31397 CHEBI
7469 IUPHAR_LIGAND_ID
C120481 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL2040682 ChEMBL_ID
6918155 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Alvesco HUMAN PRESCRIPTION DRUG LABEL 1 54868-5989 AEROSOL, METERED 80 ug RESPIRATORY (INHALATION) NDA 16 sections
Alvesco HUMAN PRESCRIPTION DRUG LABEL 1 54868-5990 AEROSOL, METERED 160 ug RESPIRATORY (INHALATION) NDA 16 sections
Omnaris HUMAN PRESCRIPTION DRUG LABEL 1 54868-6020 SPRAY 50 ug NASAL NDA 13 sections
Omnaris HUMAN PRESCRIPTION DRUG LABEL 1 70515-701 SPRAY 50 ug NASAL NDA 17 sections
Alvesco HUMAN PRESCRIPTION DRUG LABEL 1 70515-711 AEROSOL, METERED 80 ug RESPIRATORY (INHALATION) NDA 17 sections
Alvesco HUMAN PRESCRIPTION DRUG LABEL 1 70515-712 AEROSOL, METERED 160 ug RESPIRATORY (INHALATION) NDA 17 sections
Zetonna HUMAN PRESCRIPTION DRUG LABEL 1 70515-737 AEROSOL, METERED 37 ug NASAL NDA 17 sections