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 1640.09 17.99 799 19808 90743 46574712
Wheezing 675.39 17.99 370 20237 53016 46612439
Obstructive airways disorder 500.27 17.99 197 20410 13215 46652240
Forced expiratory volume decreased 331.97 17.99 113 20494 4991 46660464
Pneumonia viral 325.29 17.99 119 20488 6505 46658950
Productive cough 315.30 17.99 224 20383 50491 46614964
Sputum discoloured 280.77 17.99 129 20478 12649 46652806
Dyspnoea 260.98 17.99 647 19960 514901 46150554
Cough 258.82 17.99 405 20202 229844 46435611
Therapeutic product effect incomplete 228.55 17.99 223 20384 77930 46587525
Soft tissue disorder 219.68 17.99 79 20528 4107 46661348
Blood count abnormal 177.48 17.99 106 20501 17772 46647683
Sleep disorder due to a general medical condition 161.21 17.99 60 20547 3439 46662016
Arthritis 159.00 17.99 183 20424 77133 46588322
Herpes zoster 145.21 17.99 164 20443 67708 46597747
Middle insomnia 136.91 17.99 72 20535 9443 46656012
Breath sounds abnormal 132.34 17.99 66 20541 7749 46657706
Chest discomfort 128.74 17.99 178 20429 90091 46575364
Nasopharyngitis 125.16 17.99 235 20372 153763 46511692
Blood cholesterol increased 118.35 17.99 115 20492 39898 46625557
Fibromyalgia 117.73 17.99 110 20497 36353 46629102
Nasal congestion 107.55 17.99 119 20488 47994 46617461
Oral pain 96.22 17.99 83 20524 24714 46640741
Bronchial wall thickening 93.77 17.99 28 20579 803 46664652
Influenza 91.56 17.99 151 20456 89119 46576336
Sleep apnoea syndrome 79.50 17.99 71 20536 22130 46643325
Blood pressure systolic increased 76.35 17.99 78 20529 28709 46636746
Crepitations 76.16 17.99 42 20565 6050 46659405
Heart rate increased 75.99 17.99 126 20481 74665 46590790
Respiratory tract congestion 73.74 17.99 54 20553 12710 46652745
Body temperature decreased 71.36 17.99 54 20553 13355 46652100
Liver function test abnormal 69.71 17.99 94 20513 46393 46619062
Toxicity to various agents 68.51 17.99 7 20600 211759 46453696
Synovitis 67.62 17.99 107 20500 60968 46604487
Death 67.41 17.99 32 20575 335516 46329939
Glaucoma 67.32 17.99 56 20551 15865 46649590
Bronchiectasis 66.83 17.99 45 20562 9271 46656184
Respiratory rate increased 65.21 17.99 48 20559 11385 46654070
Acute kidney injury 62.21 17.99 14 20593 235841 46429614
Peripheral swelling 61.62 17.99 181 20426 157890 46507565
Bronchitis 61.57 17.99 141 20466 105838 46559617
Infection 60.95 17.99 162 20445 133430 46532025
Nasal polyps 60.35 17.99 26 20581 2184 46663271
Diarrhoea 56.21 17.99 101 20506 559501 46105954
Hypoventilation 56.00 17.99 30 20577 4080 46661375
Drug interaction 55.72 17.99 11 20596 203083 46462372
Allergy to animal 53.53 17.99 17 20590 601 46664854
Asthma-chronic obstructive pulmonary disease overlap syndrome 53.12 17.99 16 20591 473 46664982
Dyspnoea exertional 50.08 17.99 84 20523 50205 46615250
Leukopenia 48.93 17.99 99 20508 68244 46597211
Blood immunoglobulin E increased 48.88 17.99 21 20586 1752 46663703
Secretion discharge 48.77 17.99 37 20570 9182 46656273
Respiratory disorder 48.42 17.99 60 20547 27240 46638215
Nausea 47.63 17.99 151 20456 687303 45978152
Lower respiratory tract infection 47.05 17.99 86 20521 55003 46610452
Oropharyngeal pain 46.77 17.99 102 20505 74066 46591389
Bronchial secretion retention 46.49 17.99 17 20590 926 46664529
Neurosensory hypoacusis 46.38 17.99 13 20594 296 46665159
Sensitivity to weather change 45.30 17.99 29 20578 5487 46659968
Sinusitis 45.29 17.99 143 20464 129625 46535830
Peak expiratory flow rate decreased 44.99 17.99 15 20592 620 46664835
Bronchial disorder 44.95 17.99 17 20590 1018 46664437
Sputum purulent 44.54 17.99 16 20591 828 46664627
Thrombocytopenia 44.17 17.99 3 20604 126578 46538877
Rhinitis allergic 43.96 17.99 31 20576 6877 46658578
Humidity intolerance 43.59 17.99 13 20594 371 46665084
Blood test abnormal 43.42 17.99 35 20572 9485 46655970
Rhinitis 42.42 17.99 32 20575 7874 46657581
Nasal turbinate hypertrophy 42.17 17.99 13 20594 416 46665039
Restrictive pulmonary disease 42.15 17.99 17 20590 1209 46664246
Total lung capacity increased 42.08 17.99 15 20592 759 46664696
Pulmonary function test decreased 41.43 17.99 24 20583 3796 46661659
Bronchial haemorrhage 40.56 17.99 12 20595 333 46665122
Tenderness 39.85 17.99 43 20564 16838 46648617
Bronchial neoplasm 39.78 17.99 11 20596 238 46665217
Pneumonia 39.22 17.99 292 20315 376028 46289427
Idiopathic intracranial hypertension 38.99 17.99 20 20587 2489 46662966
Neutropenia 38.75 17.99 8 20599 143196 46522259
Broncholithiasis 38.64 17.99 9 20598 94 46665361
White blood cell count decreased 38.18 17.99 3 20604 112228 46553227
Breast neoplasm 37.89 17.99 16 20591 1279 46664176
Kyphosis 37.67 17.99 19 20588 2282 46663173
Loss of personal independence in daily activities 37.60 17.99 80 20527 57103 46608352
Vomiting 37.56 17.99 91 20516 452703 46212752
Blood pressure increased 37.45 17.99 132 20475 126534 46538921
Respiratory tract inflammation 37.29 17.99 12 20595 443 46665012
Hyper IgE syndrome 36.31 17.99 10 20597 213 46665242
Rales 34.86 17.99 31 20576 9600 46655855
Gastrooesophageal reflux disease 34.72 17.99 91 20516 74253 46591202
Lipohypertrophy 34.69 17.99 13 20594 759 46664696
Hypotension 34.67 17.99 31 20576 232558 46432897
Pulmonary mass 34.52 17.99 41 20566 17816 46647639
Off label use 34.18 17.99 73 20534 379768 46285687
Malaise 33.90 17.99 256 20351 330976 46334479
Limb injury 33.77 17.99 42 20565 19132 46646323
Lymph node calcification 33.65 17.99 9 20598 171 46665284
Bronchospasm 33.61 17.99 38 20569 15669 46649786
Confusional state 32.42 17.99 15 20592 159877 46505578
Mycobacterium avium complex infection 32.40 17.99 18 20589 2630 46662825
Lower respiratory tract congestion 32.34 17.99 16 20591 1845 46663610
Peak expiratory flow rate abnormal 31.81 17.99 8 20599 118 46665337
Hypersensitivity 31.77 17.99 141 20466 150180 46515275
Chronic obstructive pulmonary disease 31.59 17.99 75 20532 57558 46607897
Bacterial disease carrier 31.45 17.99 12 20595 736 46664719
Rheumatoid arthritis 31.26 17.99 36 20571 240179 46425276
Febrile neutropenia 30.90 17.99 3 20604 94624 46570831
Weight decreased 30.67 17.99 178 20429 210671 46454784
Eosinophilia 30.54 17.99 40 20567 19177 46646278
Viral infection 29.42 17.99 50 20557 30185 46635270
Neuropathy peripheral 29.37 17.99 3 20604 90890 46574565
Soft tissue swelling 29.32 17.99 12 20595 886 46664569
Sinus pain 29.03 17.99 15 20592 1895 46663560
Urinary tract infection 28.67 17.99 33 20574 220233 46445222
Endometrial ablation 28.61 17.99 11 20596 689 46664766
Increased bronchial secretion 28.41 17.99 14 20593 1600 46663855
Platelet count decreased 28.30 17.99 5 20602 100019 46565436
Hypokalaemia 28.20 17.99 3 20604 88021 46577434
Upper-airway cough syndrome 27.89 17.99 25 20582 7822 46657633
Treatment failure 27.80 17.99 4 20603 93083 46572372
Reversible airways obstruction 27.32 17.99 10 20597 546 46664909
Rash 26.95 17.99 75 20532 356437 46309018
Eosinophilic granulomatosis with polyangiitis 26.71 17.99 14 20593 1822 46663633
Emphysema 26.70 17.99 26 20581 9028 46656427
Rhinorrhoea 26.09 17.99 62 20545 47603 46617852
Forced vital capacity decreased 25.85 17.99 11 20596 896 46664559
Sarcoidosis 25.74 17.99 20 20587 5139 46660316
Hepatic enzyme increased 25.66 17.99 3 20604 81784 46583671
Lung disorder 25.53 17.99 58 20549 43246 46622209
Pulmonary function test abnormal 25.11 17.99 12 20595 1283 46664172
Seasonal allergy 24.76 17.99 30 20577 13304 46652151
Infusion related reaction 24.73 17.99 7 20600 101201 46564254
Cardiac arrest 24.55 17.99 5 20602 90394 46575061
Ligament pain 24.51 17.99 7 20600 171 46665284
Sepsis 24.28 17.99 15 20592 135999 46529456
Rhonchi 24.24 17.99 14 20593 2201 46663254
Seizure 24.24 17.99 12 20595 123042 46542413
Oral candidiasis 24.08 17.99 34 20573 17498 46647957
Dehydration 24.07 17.99 21 20586 159519 46505936
Sinus congestion 23.54 17.99 29 20578 13080 46652375
Nasal mucosal disorder 22.73 17.99 8 20599 390 46665065
Renal impairment 22.67 17.99 3 20604 74369 46591086
Pancytopenia 22.49 17.99 5 20602 85053 46580402
Respiratory symptom 22.44 17.99 13 20594 2057 46663398
Pulmonary congestion 22.28 17.99 30 20577 14769 46650686
Constipation 21.67 17.99 27 20580 174070 46491385
Blood creatinine increased 21.22 17.99 4 20603 76399 46589056
Macrocytosis 21.15 17.99 13 20594 2290 46663165
Disease progression 21.07 17.99 7 20600 91293 46574162
Respiratory tract infection 20.94 17.99 43 20564 29929 46635526
Eosinophilic bronchitis 20.86 17.99 7 20600 295 46665160
Haemoglobin decreased 20.65 17.99 16 20591 128933 46536522
Product dose omission issue 20.08 17.99 27 20580 168493 46496962
Aspartate aminotransferase increased 20.07 17.99 5 20602 78695 46586760
Oropharyngeal discomfort 19.75 17.99 14 20593 3131 46662324
Ventricular failure 19.62 17.99 7 20600 355 46665100
Stress 19.05 17.99 58 20549 51493 46613962
Symptom recurrence 19.01 17.99 7 20600 389 46665066
Malignant neoplasm progression 18.90 17.99 3 20604 64923 46600532
Presbyacusis 18.74 17.99 13 20594 2809 46662646
Varicella zoster oesophagitis 18.60 17.99 4 20603 28 46665427
Polycystic ovaries 18.57 17.99 10 20597 1374 46664081
Nasal obstruction 18.57 17.99 8 20599 672 46664783
Nocturnal dyspnoea 18.49 17.99 9 20598 1002 46664453
Aphonia 18.33 17.99 20 20587 7925 46657530
Hyponatraemia 18.33 17.99 11 20596 101321 46564134
Psoriasis 18.19 17.99 6 20601 78598 46586857
Sinus operation 18.10 17.99 10 20597 1445 46664010
Pulmonary eosinophilia 18.06 17.99 6 20601 245 46665210
Varicella zoster gastritis 18.02 17.99 4 20603 33 46665422

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 1066.79 25.86 391 7775 35783 29908529
Wheezing 447.09 25.86 201 7965 30737 29913575
Obstructive airways disorder 432.95 25.86 141 8025 8918 29935394
Therapeutic product effect incomplete 290.05 25.86 154 8012 33680 29910632
Blood count abnormal 228.10 25.86 94 8072 11558 29932754
Pulmonary function test decreased 213.72 25.86 69 8097 4226 29940086
Sputum discoloured 213.62 25.86 77 8089 6591 29937721
Cough 188.86 25.86 200 7966 125442 29818870
Forced expiratory volume decreased 169.00 25.86 54 8112 3196 29941116
Asthma-chronic obstructive pulmonary disease overlap syndrome 165.16 25.86 38 8128 631 29943681
Productive cough 144.29 25.86 94 8072 29859 29914453
Nasal congestion 143.47 25.86 79 8087 18487 29925825
Nasal obstruction 143.35 25.86 34 8132 648 29943664
Sinus pain 137.72 25.86 33 8133 658 29943654
Bronchiectasis 136.85 25.86 52 8114 5152 29939160
Chest discomfort 130.10 25.86 104 8062 45376 29898936
Dyspnoea 108.14 25.86 262 7904 333033 29611279
Respiratory disorder 99.43 25.86 61 8105 17433 29926879
Eosinophil count abnormal 86.06 25.86 19 8147 259 29944053
Mycobacterium avium complex infection 85.62 25.86 31 8135 2680 29941632
Sleep disorder due to a general medical condition 78.16 25.86 25 8141 1482 29942830
Lung consolidation 77.11 25.86 34 8132 4918 29939394
Vital capacity decreased 73.82 25.86 18 8148 387 29943925
Emphysema 72.55 25.86 40 8126 9362 29934950
Throat irritation 70.49 25.86 38 8128 8510 29935802
Pulmonary mass 69.80 25.86 41 8125 10821 29933491
Osteopenia 69.43 25.86 31 8135 4617 29939695
Influenza 68.27 25.86 71 8095 43327 29900985
Dust allergy 68.26 25.86 17 8149 400 29943912
Bronchial hyperreactivity 66.79 25.86 21 8145 1177 29943135
Middle insomnia 66.02 25.86 32 8134 5741 29938571
Acute kidney injury 62.33 25.86 3 8163 273839 29670473
Nasal polyps 59.88 25.86 20 8146 1359 29942953
Dyspnoea exertional 59.40 25.86 60 8106 35370 29908942
Breath sounds abnormal 58.38 25.86 28 8138 4907 29939405
Sinusitis 56.87 25.86 57 8109 33288 29911024
Loss of personal independence in daily activities 54.67 25.86 46 8120 21489 29922823
Blood immunoglobulin E increased 51.72 25.86 19 8147 1711 29942601
Sensitivity to weather change 51.10 25.86 18 8148 1436 29942876
Nasopharyngitis 47.87 25.86 69 8097 58780 29885532
Eosinophil count 46.47 25.86 10 8156 120 29944192
Respiratory rate increased 45.37 25.86 29 8137 8886 29935426
Rhinorrhoea 43.96 25.86 40 8126 20714 29923598
Vocal cord dysfunction 43.51 25.86 10 8156 165 29944147
Spirometry abnormal 43.08 25.86 11 8155 287 29944025
Seasonal allergy 41.62 25.86 22 8144 4731 29939581
Suffocation feeling 40.47 25.86 12 8154 551 29943761
Eosinophil count increased 39.75 25.86 25 8141 7448 29936864
Lower respiratory tract infection 38.95 25.86 42 8124 26672 29917640
Hypoxia 38.74 25.86 56 8110 47798 29896514
Respiratory tract congestion 38.59 25.86 22 8144 5484 29938828
Body temperature decreased 38.52 25.86 27 8139 9628 29934684
Mycotic allergy 38.11 25.86 9 8157 168 29944144
Blood pressure systolic increased 37.77 25.86 32 8134 15078 29929234
Mite allergy 35.65 25.86 9 8157 224 29944088
Blood pressure increased 35.07 25.86 67 8099 71861 29872451
Toxicity to various agents 34.46 25.86 4 8162 177179 29767133
Upper-airway cough syndrome 33.96 25.86 16 8150 2694 29941618
Pulmonary function test abnormal 33.29 25.86 13 8153 1383 29942929
Conjunctivitis allergic 32.45 25.86 10 8156 524 29943788
Chronic obstructive pulmonary disease 30.30 25.86 49 8117 46077 29898235
Death 30.05 25.86 32 8134 357251 29587061
Sputum increased 29.71 25.86 13 8153 1844 29942468
Decreased activity 29.57 25.86 16 8150 3605 29940707
Peak expiratory flow rate decreased 28.95 25.86 7 8159 145 29944167
Oesophageal carcinoma 28.55 25.86 15 8151 3186 29941126
Gastrooesophageal reflux disease 27.94 25.86 39 8127 32216 29912096
Eosinophilic granulomatosis with polyangiitis 27.03 25.86 11 8155 1304 29943008
Hypoventilation 26.49 25.86 14 8152 3009 29941303
Panic reaction 26.19 25.86 11 8155 1412 29942900
Infective exacerbation of chronic obstructive airways disease 25.93 25.86 11 8155 1447 29942865
Hypersensitivity 25.91 25.86 50 8116 53978 29890334

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)

None

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
D01703 KEGG_DRUG
4027427 VANDF
C1174745 UMLSCUI
CHEBI:31397 CHEBI
CHEMBL2040682 ChEMBL_ID
DB01410 DRUGBANK_ID
6918155 PUBCHEM_CID
C120481 MESH_SUPPLEMENTAL_RECORD_UI
7469 IUPHAR_LIGAND_ID
6546 INN_ID
S59502J185 UNII
274964 RXNORM
132906 MMSL
19358 MMSL
89965 MMSL
d05465 MMSL
008829 NDDF
416739001 SNOMEDCT_US
417420004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Alvesco HUMAN PRESCRIPTION DRUG LABEL 1 54868-5989 AEROSOL, METERED 80 ug RESPIRATORY (INHALATION) NDA 27 sections
Alvesco HUMAN PRESCRIPTION DRUG LABEL 1 54868-5990 AEROSOL, METERED 160 ug RESPIRATORY (INHALATION) NDA 27 sections
Omnaris HUMAN PRESCRIPTION DRUG LABEL 1 54868-6020 SPRAY 50 ug NULLSAL NDA 13 sections
Omnaris HUMAN PRESCRIPTION DRUG LABEL 1 70515-701 SPRAY 50 ug NULLSAL NDA 27 sections
Alvesco HUMAN PRESCRIPTION DRUG LABEL 1 70515-711 AEROSOL, METERED 80 ug RESPIRATORY (INHALATION) NDA 26 sections
Alvesco HUMAN PRESCRIPTION DRUG LABEL 1 70515-712 AEROSOL, METERED 160 ug RESPIRATORY (INHALATION) NDA 26 sections
Zetonna HUMAN PRESCRIPTION DRUG LABEL 1 70515-737 AEROSOL, METERED 37 ug NULLSAL NDA 26 sections