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

Stem definition	Drug id	CAS RN
steroids for topical use, acetal derivatives	633	126544-47-6

Description:

Molecule	Description
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:

Dose	Unit	Route
0.20	mg	N
0.16	mg	Inhal.aerosol

ADMET properties:

Property	Value	Reference
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 µM/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:

Date	Agency	Company	Orphan
Oct. 20, 2006	FDA	TAKEDA GMBH

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	12.78	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN	AGONIST	Ki	7.43		WOMBAT-PK	CHEMBL
SARS-CoV-2	Virus			INHIBITOR	IC50	5.36		SCIENTIFIC LITERATURE

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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