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Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
antihistaminics	271	58581-89-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: azelastine azelastine hydrochloride azelastine HCl	Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Azelastine Hydrochloride is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity. Molecular weight: 381.90 Formula: C22H24ClN3O CLOGP: 4.01 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 35.91 ALOGS: -4.62 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

azelastine
azelastine hydrochloride
azelastine HCl

Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Azelastine Hydrochloride is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity.

Molecular weight: 381.90
Formula: C22H24ClN3O
CLOGP: 4.01
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 35.91
ALOGS: -4.62
ROTB: 3

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.56	mg	N
4	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.30 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	15 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	9 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.17 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	22 hours	Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	2.499		Moderate	0.79
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.472		Moderate	0.79
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	33.189	10^-6 cm/s	Moderate	0.79
dh-clint	Dog hepatocyte intrinsic clearance	29.785	uL/min/10^6 cells	Moderate	0.79
dppb	Dog plasma protein binding (% unbound)	13.820	%	Moderate	0.79
fcs-ppb	Fetal calf serum protein binding (% unbound)	23.690	%	Moderate	0.79
herg	hERG pIC50	6.181	pIC50	Moderate	0.79
hh-clint	Human hepatocyte intrinsic clearance	3.972	uL/min/10^6 cells	Moderate	0.79
hlm-clint	Human liver microsomal intrinsic clearance	28.314	uL/min/mg protein	Moderate	0.79
hppb	Human plasma protein binding (% unbound)	13.710	%	Moderate	0.79
kinase-safety-class	ACVR2B,AKT2,AKT3,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK	35
kinase-selectivity-class	AXL,EIF2AK3,PDK4	3
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	0.598		Moderate	0.79
mh-clint	Mouse hepatocyte intrinsic clearance	109.648		Moderate	0.79
mppb	Mouse plasma protein binding (% unbound)	10.750		Moderate	0.79
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	3.981		Moderate	0.79
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	29.470	%	Moderate	0.79
rh-clint	Rat hepatocyte intrinsic clearance	194.536	uL/min/10^6 cells	Moderate	0.79
rh-fuinc	Rat hepatocyte fraction unbound in incubation	44.440	%	Moderate	0.79
rppb	Rat plasma protein binding (% unbound)	12.730	%	Moderate	0.79
solubility-dd	Solubility at pH 7.4 in DMSO	769.130	uM	Moderate	0.79

Approvals:

Date	Agency	Company	Orphan
Nov. 1, 1996	FDA	MEDA PHARMS

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	210.58	14.64	262	19594	241898	90366693
Treatment failure	154.89	14.64	255	19601	303673	90304918
Sinusitis	153.96	14.64	272	19584	342816	90265775
Impaired quality of life	140.40	14.64	78	19778	23066	90585525
Cough	128.95	14.64	263	19593	368699	90239892
Product dose omission issue	127.87	14.64	229	19627	291458	90317133
COVID-19	101.55	14.64	153	19703	168690	90439901
Injection site pain	91.37	14.64	148	19708	173551	90435040
Dermatitis atopic	73.51	14.64	52	19804	23420	90585171
Illness	73.15	14.64	90	19766	81879	90526712
Product delivery mechanism issue	68.34	14.64	17	19839	499	90608092
Nasal congestion	60.98	14.64	83	19773	83331	90525260
Systemic lupus erythematosus	60.61	14.64	5	19851	361891	90246700
Hepatic enzyme increased	55.20	14.64	7	19849	360729	90247862
No adverse event	53.30	14.64	70	19786	67912	90540679
Bronchitis	53.23	14.64	109	19747	152818	90455773
Glossodynia	52.38	14.64	5	19851	321774	90286817
General physical health deterioration	49.51	14.64	9	19847	355106	90253485
Contraindicated product administered	49.49	14.64	6	19850	320133	90288458
Sinus disorder	48.39	14.64	48	19808	34399	90574192
Toxicity to various agents	48.12	14.64	4	19852	287842	90320749
Dry eye	47.51	14.64	61	19795	57870	90550721
Infusion site erythema	46.82	14.64	32	19824	13638	90594953
Infusion site pain	46.78	14.64	37	19819	19701	90588890
Product dose omission in error	45.54	14.64	37	19819	20466	90588125
Infusion site swelling	43.89	14.64	29	19827	11691	90596900
Headache	42.29	14.64	328	19528	862418	89746173
Eye irritation	41.65	14.64	44	19812	33934	90574657
Drug intolerance	40.42	14.64	24	19832	447567	90161024
Product administration interrupted	39.86	14.64	28	19828	12464	90596127
Wound	39.48	14.64	9	19847	302971	90305620
Upper-airway cough syndrome	37.22	14.64	29	19827	15106	90593485
Multiple allergies	37.20	14.64	29	19827	15117	90593474
Exposure via skin contact	36.52	14.64	25	19831	10680	90597911
Maternal exposure during pregnancy	35.89	14.64	17	19839	360046	90248545
Helicobacter infection	35.68	14.64	4	19852	226846	90381745
Surgery	34.83	14.64	46	19810	44841	90563750
Eye pruritus	34.54	14.64	37	19819	28990	90579601
Injection site swelling	34.19	14.64	53	19803	59786	90548805
Product use in unapproved indication	34.14	14.64	155	19701	336081	90272510
Lower respiratory tract infection	33.56	14.64	7	19849	250652	90357939
Arthropathy	32.55	14.64	20	19836	366222	90242369
Eczema	31.86	14.64	48	19808	52822	90555769
Injection site erythema	31.68	14.64	68	19788	98434	90510157
Dyspnoea	31.21	14.64	312	19544	880643	89727948
Oropharyngeal pain	30.90	14.64	74	19782	115113	90493478
Pre-existing condition improved	30.30	14.64	21	19835	9148	90599443
Rhinorrhoea	29.59	14.64	62	19794	88254	90520337
Drug interaction	29.20	14.64	12	19844	276441	90332150
C-reactive protein increased	29.02	14.64	3	19853	181386	90427205
Joint swelling	28.83	14.64	41	19815	503259	90105332
Seasonal allergy	28.59	14.64	30	19826	22953	90585638
Dry skin	28.55	14.64	61	19795	88012	90520579
Sleep disorder due to a general medical condition	27.50	14.64	41	19815	44697	90563894
Infusion site bruising	27.23	14.64	15	19841	4357	90604234
Nasal discomfort	26.46	14.64	16	19840	5532	90603059
Infusion related reaction	25.85	14.64	32	19824	416748	90191843
Chest discomfort	24.22	14.64	76	19780	138289	90470302
Inappropriate schedule of product administration	24.11	14.64	80	19776	149853	90458738
Injection site rash	23.94	14.64	28	19828	24145	90584446
Infusion site extravasation	23.70	14.64	19	19837	10309	90598282
Alopecia	23.11	14.64	46	19810	495025	90113566
Therapy interrupted	22.72	14.64	40	19816	50068	90558523
Sleep apnoea syndrome	22.30	14.64	31	19825	31716	90576875
Therapeutic product effect decreased	22.19	14.64	17	19839	277554	90331037
Injection site pruritus	21.90	14.64	41	19815	53793	90554798
Device programming error	21.80	14.64	6	19850	263	90608328
Fatigue	21.80	14.64	364	19492	1153659	89454932
Skin swelling	21.51	14.64	15	19841	6599	90601992
Urinary tract infection	21.34	14.64	127	19729	305505	90303086
Productive cough	21.20	14.64	50	19806	77013	90531578
Type 2 diabetes mellitus	21.17	14.64	9	19847	203235	90405356
Ocular hyperaemia	20.81	14.64	31	19825	33767	90574824
Pruritus	20.68	14.64	195	19661	541330	90067261
Neutropenia	20.36	14.64	12	19844	224892	90383699
Injection site urticaria	19.76	14.64	22	19834	17989	90590602
Product taste abnormal	19.75	14.64	10	19846	2450	90606141
Infusion site haemorrhage	19.32	14.64	13	19843	5398	90603193
Back pain	18.55	14.64	126	19730	317049	90291542
Upper respiratory tract infection	18.47	14.64	66	19790	128252	90480339
Throat irritation	18.47	14.64	36	19820	48659	90559932
Rheumatoid arthritis	18.40	14.64	32	19824	362582	90246009
Sinus operation	17.91	14.64	10	19846	2981	90605610
Infusion site mass	17.87	14.64	9	19847	2180	90606411
Therapeutic response unexpected	17.87	14.64	23	19833	21857	90586734
Ear infection	17.82	14.64	44	19812	69731	90538860
Sneezing	17.82	14.64	27	19829	29842	90578749
Paranasal sinus discomfort	17.71	14.64	13	19843	6197	90602394
Hyposmia	17.68	14.64	7	19849	962	90607629
Blister	17.52	14.64	18	19838	254980	90353611
Eye pain	17.17	14.64	33	19823	44135	90564456
Mobility decreased	16.89	14.64	18	19838	250716	90357875
Sinus congestion	16.66	14.64	25	19831	27399	90581192
Febrile neutropenia	16.51	14.64	7	19849	158342	90450249
Acute kidney injury	16.51	14.64	28	19828	320359	90288232
Sleep disorder due to general medical condition, insomnia type	16.40	14.64	4	19852	128690	90479901
Confusional state	16.25	14.64	38	19818	386167	90222424
Potassium hydroxide preparation positive	16.05	14.64	3	19853	21	90608570
Injury	15.88	14.64	12	19844	197337	90411254
Migraine	15.86	14.64	83	19773	190309	90418282
Nasal pruritus	15.75	14.64	6	19850	744	90607847
Conjunctivitis allergic	15.54	14.64	7	19849	1325	90607266
Acute respiratory failure	15.40	14.64	31	19825	42887	90565704
Snoring	15.23	14.64	11	19845	5115	90603476
Thrombocytopenia	15.18	14.64	14	19842	208711	90399880
Incorrect drug administration rate	15.04	14.64	11	19845	5212	90603379
Intentional dose omission	15.01	14.64	19	19837	17764	90590827

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
Treatment failure	170.26	17.91	119	7785	62505	42550926
Sinusitis	99.35	17.91	77	7827	47215	42566216
Asthma	71.51	17.91	72	7832	62242	42551189
Product delivery mechanism issue	59.52	17.91	13	7891	253	42613178
Impaired quality of life	50.66	17.91	32	7872	14145	42599286
Product dose omission issue	50.30	17.91	97	7807	154268	42459163
Injection site pain	49.11	17.91	57	7847	57741	42555690
Exposure via skin contact	36.20	17.91	18	7886	5020	42608411
Transferrin increased	34.50	17.91	5	7899	5	42613426
Injection site swelling	29.98	17.91	25	7879	16948	42596483
Chorioretinopathy	29.52	17.91	11	7893	1520	42611911
Cough	28.55	17.91	85	7819	178018	42435413
Dermatitis atopic	27.76	17.91	21	7883	12383	42601048
Nasal congestion	26.56	17.91	30	7874	29471	42583960
Product use in unapproved indication	25.83	17.91	84	7820	184372	42429059
Illness	25.30	17.91	27	7877	24903	42588528
Productive cough	22.67	17.91	37	7867	51530	42561901
Thrombocytopenia	22.64	17.91	4	7900	190275	42423156
Eye irritation	20.67	17.91	17	7887	11301	42602130
Wheezing	19.75	17.91	36	7868	54745	42558686
Oesophageal injury	19.11	17.91	5	7899	214	42613217
pH body fluid increased	18.99	17.91	4	7900	65	42613366
Therapy interrupted	18.97	17.91	22	7882	22228	42591203
Ear infection	18.85	17.91	17	7887	12787	42600644
Accidental exposure to product	18.80	17.91	21	7883	20372	42593059
Cardiac valve sclerosis	18.72	17.91	4	7900	70	42613361
Eye pruritus	18.50	17.91	16	7888	11396	42602035
Costovertebral angle tenderness	17.98	17.91	4	7900	85	42613346

FDA Adverse Event Reporting System (Geriatric)

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	211.13	14.11	247	20486	250044	110318522
Impaired quality of life	154.28	14.11	86	20647	29931	110538635
Sinusitis	121.20	14.11	207	20526	296481	110272085
Product dose omission issue	116.60	14.11	213	20520	321569	110246997
Cough	101.32	14.11	249	20484	461392	110107174
Dermatitis atopic	86.57	14.11	56	20677	25485	110543081
Injection site pain	84.55	14.11	133	20600	177789	110390777
Toxicity to various agents	73.81	14.11	4	20729	480551	110088015
COVID-19	73.69	14.11	150	20583	244910	110323656
Nasal congestion	68.14	14.11	88	20645	98194	110470372
Illness	60.79	14.11	76	20657	82095	110486471
Eye irritation	56.00	14.11	48	20685	33404	110535162
Exposure via skin contact	55.10	14.11	33	20700	13114	110555452
Bronchitis	45.84	14.11	95	20638	156937	110411629
General physical health deterioration	43.26	14.11	13	20720	425282	110143284
Headache	43.25	14.11	298	20435	882079	109686487
Drug interaction	41.48	14.11	21	20712	500162	110068404
Dyspnoea	40.97	14.11	350	20383	1106522	109462044
Injection site swelling	40.75	14.11	54	20679	61736	110506830
Dry eye	40.30	14.11	51	20682	55742	110512824
Fatigue	39.64	14.11	374	20359	1215584	109352982
Eye pruritus	39.24	14.11	39	20694	32736	110535830
Eczema	38.48	14.11	57	20676	72236	110496330
Product administration interrupted	36.40	14.11	24	20709	11268	110557298
Oropharyngeal pain	36.19	14.11	79	20654	135197	110433369
Infusion site pain	35.45	14.11	28	20705	17391	110551175
Sinus disorder	33.86	14.11	36	20697	32692	110535874
Systemic lupus erythematosus	33.82	14.11	4	20729	254334	110314232
Surgery	33.47	14.11	40	20693	41243	110527323
Productive cough	33.17	14.11	69	20664	114236	110454330
Treatment failure	33.07	14.11	6	20727	277228	110291338
Injection site erythema	31.10	14.11	60	20673	94116	110474450
Chest discomfort	30.10	14.11	86	20647	173762	110394804
Drug intolerance	29.53	14.11	20	20713	406492	110162074
Upper-airway cough syndrome	29.11	14.11	24	20709	15833	110552733
Transferrin increased	28.96	14.11	5	20728	25	110568541
Dry skin	28.94	14.11	63	20670	107590	110460976
Hepatic enzyme increased	28.87	14.11	12	20721	320880	110247686
Rhinorrhoea	28.65	14.11	61	20672	102605	110465961
Thrombocytopenia	28.38	14.11	15	20718	348870	110219696
Infusion site erythema	28.23	14.11	21	20712	11938	110556628
Product dose omission in error	28.19	14.11	28	20705	23484	110545082
Pericarditis	27.80	14.11	4	20729	219110	110349456
Sleep disorder due to a general medical condition	27.60	14.11	41	20692	52071	110516495
C-reactive protein increased	27.59	14.11	4	20729	217915	110350651
Injection site rash	26.45	14.11	27	20706	23392	110545174
Impaired healing	26.38	14.11	3	20730	196714	110371852
Therapy interrupted	26.10	14.11	39	20694	49783	110518783
Acute kidney injury	25.84	14.11	50	20683	635380	109933186
Lower respiratory tract infection	25.50	14.11	7	20726	243099	110325467
Chorioretinopathy	25.09	14.11	11	20722	2284	110566282
Product use in unapproved indication	24.81	14.11	156	20577	447221	110121345
Accidental exposure to product	24.58	14.11	38	20695	49970	110518596
Contraindicated product administered	24.49	14.11	8	20725	248259	110320307
Glossodynia	24.03	14.11	6	20727	221998	110346568
Insurance issue	23.64	14.11	18	20715	10594	110557972
Back pain	22.87	14.11	133	20600	370863	110197703
Injection site pruritus	22.51	14.11	37	20696	51221	110517345
Febrile neutropenia	22.45	14.11	16	20717	316751	110251815
Ocular hyperaemia	22.39	14.11	32	20701	39254	110529312
Wound	22.35	14.11	8	20725	234429	110334137
Nasal discomfort	22.05	14.11	14	20719	6167	110562399
Sleep apnoea syndrome	21.67	14.11	32	20701	40415	110528151
Off label use	21.62	14.11	179	20554	1500006	109068560
Neutropenia	21.61	14.11	23	20710	374597	110193969
Injection site urticaria	21.57	14.11	21	20712	17194	110551372
Folliculitis	21.40	14.11	3	20730	167650	110400916
Multiple allergies	21.35	14.11	18	20715	12245	110556321
Acute respiratory failure	21.32	14.11	45	20688	75215	110493351
Seasonal allergy	20.94	14.11	22	20711	19700	110548866
Skin swelling	20.91	14.11	15	20718	8065	110560501
Upper respiratory tract infection	20.85	14.11	63	20670	131265	110437301
Device programming error	20.69	14.11	6	20727	373	110568193
Maternal exposure during pregnancy	20.66	14.11	11	20722	254872	110313694
Pruritus	20.41	14.11	182	20551	581378	109987188
Respiratory tract congestion	20.39	14.11	27	20706	30830	110537736
Throat irritation	20.03	14.11	36	20697	53516	110515050
Vision blurred	19.65	14.11	61	20672	128961	110439605
Sinus operation	19.37	14.11	10	20723	2981	110565585
Overdose	19.08	14.11	10	20723	233784	110334782
Acute sinusitis	19.08	14.11	12	20721	5199	110563367
Ear discomfort	18.54	14.11	16	20717	11233	110557333
Dyspnoea exertional	18.51	14.11	52	20681	104008	110464558
No adverse event	18.48	14.11	42	20691	73797	110494769
pH body fluid increased	18.46	14.11	4	20729	74	110568492
Ear infection	18.34	14.11	38	20695	62694	110505872
Infusion site swelling	18.24	14.11	15	20718	9862	110558704
Infusion related reaction	18.23	14.11	27	20706	381135	110187431
Oesophageal injury	17.29	14.11	5	20728	308	110568258
Cardiac valve sclerosis	17.06	14.11	4	20729	107	110568459
Infusion site discharge	16.96	14.11	8	20725	1965	110566601
Multiple organ dysfunction syndrome	16.61	14.11	4	20729	151706	110416860
Influenza	16.40	14.11	69	20664	169032	110399534
Gastrointestinal submucosal tumour	16.19	14.11	4	20729	134	110568432
Nasal septum deviation	16.14	14.11	8	20725	2190	110566376
Conjunctivitis	15.66	14.11	25	20708	33767	110534799
Injection site vesicles	15.63	14.11	10	20723	4461	110564105
Flushing	15.47	14.11	49	20684	104687	110463879
Nasal pruritus	15.34	14.11	6	20727	934	110567632
Type 2 diabetes mellitus	15.34	14.11	7	20726	177225	110391341
Infusion site bruising	14.78	14.11	9	20724	3685	110564881
Sinus congestion	14.76	14.11	23	20710	30436	110538130
Wheezing	14.75	14.11	90	20643	255140	110313426
Feeling abnormal	14.71	14.11	70	20663	180641	110387925
Urinary tract infection	14.62	14.11	108	20625	326174	110242392
Pneumonia	14.60	14.11	238	20495	876476	109692090
Infusion site pruritus	14.60	14.11	10	20723	4998	110563568
Paranasal sinus discomfort	14.57	14.11	11	20722	6394	110562172
Nasal polyps	14.51	14.11	15	20718	13185	110555381
Eye pain	14.24	14.11	30	20703	50069	110518497

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R01AC03	RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Antiallergic agents, excl. corticosteroids
ATC	R06AX19	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
ATC	S01GX07	SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
CHEBI has role	CHEBI:35523	bronchodilator agent
CHEBI has role	CHEBI:37955	H<small><sub>1</sub></small>-receptor antagonist
CHEBI has role	CHEBI:49167	anti-asthmatic drug
CHEBI has role	CHEBI:50427	platelet aggregation inhibitor
CHEBI has role	CHEBI:50857	anti-allergic agent
CHEBI has role	CHEBI:64964	EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor
CHEBI has role	CHEBI:77715	nasal decongestant
CHEBI has role	CHEBI:66981	ophthalmology drug
MeSH PA	D001993	Bronchodilator Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D016859	Lipoxygenase Inhibitors
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018494	Histamine Agents
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D018927	Anti-Asthmatic Agents
MeSH PA	D019141	Respiratory System Agents
MeSH PA	D039563	Histamine H1 Antagonists, Non-Sedating
FDA EPC	N0000175587	Histamine-1 Receptor Antagonist

Related Drugs by ATC class:

R01AC Antiallergic agents, excl. corticosteroids 7 drugs

antazoline cromoglicic acid levocabastine nedocromil olopatadine spaglumic acid thonzylamine

R06AX Other antihistamines for systemic use 26 drugs

acrivastine antazoline astemizole azatadine bamipine bilastine cyproheptadine deptropine desloratadine ebastine epinastine fexofenadine show all 26 →

S01GX Other antiallergics 12 drugs

alcaftadine bilastine cetirizine cromoglicic acid emedastine epinastine ketotifen levocabastine lodoxamide nedocromil olopatadine spaglumic acid

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Vasomotor rhinitis	indication	8229003	DOID:4730
Allergic rhinitis	indication	61582004
Seasonal allergic rhinitis	indication	367498001
Allergic conjunctivitis	indication	473460002	DOID:11204
Kidney disease	contraindication	90708001	DOID:557
Drowsy	contraindication	271782001
Ocular Irritation	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.91	Basic

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])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	8.17	WOMBAT-PK	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	5.93	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.84	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	6.82	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	7	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.64	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.70	CHEMBL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.30	CHEMBL
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.68	CHEMBL
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	6.41	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7.30	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.64	CHEMBL
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.20	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		IC50	5.20	CHEMBL
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	5.37	CHEMBL
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	6.05	CHEMBL
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.48	CHEMBL
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	7.30	CHEMBL
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN		Ki	5.27	CHEMBL
Histamine H3 receptor	GPCR	Q9Y5N1	HRH3_HUMAN		Ki	6.83	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.24	CHEMBL
Transmembrane protein 97	Enzyme	Q5BJF2	TMM97_HUMAN		Ki	7.50	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		Ki	7.30	CHEMBL
Spike glycoprotein	Glycoprotein		SPIKE_SARS2		Kd	6.59	CHEMBL

External reference:

ID	Source
4024042	VUID
N0000022047	NUI
D00659	KEGG_DRUG
79307-93-0	SECONDARY_CAS_RN
18603	RXNORM
C0052762	UMLSCUI
CHEBI:2950	CHEBI
CHEMBL639	ChEMBL_ID
CHEMBL1200809	ChEMBL_ID
DB00972	DRUGBANK_ID
C020976	MESH_SUPPLEMENTAL_RECORD_UI
2267	PUBCHEM_CID
7121	IUPHAR_LIGAND_ID
4074	INN_ID
ZQI909440X	UNII
169403	MMSL
4237	MMSL
8899	MMSL
4021001	VANDF
4024042	VANDF
003931	NDDF
003932	NDDF
108644000	SNOMEDCT_US
108646003	SNOMEDCT_US
372520005	SNOMEDCT_US
ZQI909440X	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
DYMISTA	HUMAN PRESCRIPTION DRUG LABEL	2	0037-0245	SPRAY, METERED	137 ug	NASAL	NDA	29 sections
Astepro Allergy	HUMAN OTC DRUG LABEL	1	0280-0065	SPRAY, METERED	205.50 ug	NASAL	NDA	16 sections
Children Astepro Allergy	HUMAN OTC DRUG LABEL	1	0280-0066	SPRAY, METERED	205.50 ug	NASAL	NDA	16 sections
Azelastine Hydrochloride	HUMAN OTC DRUG LABEL	1	0363-0653	SPRAY, METERED	205.50 ug	NASAL	ANDA	15 sections
Azelastine Hydrochloride and Fluticasone Propionate	HUMAN PRESCRIPTION DRUG LABEL	2	0378-3458	SPRAY, METERED	137 ug	NASAL	NDA authorized generic	29 sections
Azelastine Hydrochloride and Fluticasone Propionate	HUMAN PRESCRIPTION DRUG LABEL	2	0480-2157	SPRAY, METERED	137 ug	NASAL	ANDA	28 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42291-094	SPRAY, METERED	1 mg	NASAL	ANDA	27 sections
AZELASTINE HYDROCHLORIDE AND FLUTICASONE PROPIONATE	HUMAN PRESCRIPTION DRUG LABEL	2	45802-066	SPRAY, METERED	137 ug	NASAL	ANDA	28 sections
AZELASTINE HYDROCHLORIDE	Human Prescription Drug Label	1	46708-506	SOLUTION/ DROPS	0.50 mg	OPHTHALMIC	ANDA	16 sections
Azelastine Hydrochloride	Human Prescription Drug Label	1	47335-779	SPRAY, METERED	137 ug	NASAL	ANDA	25 sections
Azelastine Hydrochloride	Human Prescription Drug Label	1	47335-938	SOLUTION/ DROPS	0.50 mg	INTRAOCULAR	ANDA	17 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-2330	SPRAY, METERED	137 ug	NASAL	ANDA	19 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-2330	SPRAY, METERED	137 ug	NASAL	ANDA	19 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3833	SPRAY, METERED	1 mg	NASAL	ANDA	27 sections
AZELASTINE HYDROCHLORIDE	Human Prescription Drug Label	1	50090-7461	SPRAY, METERED	137 ug	NASAL	ANDA	26 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50383-942	SPRAY, METERED	1.50 mg	NASAL	ANDA	25 sections
Azelastine Hydrochloride	HUMAN OTC DRUG LABEL	1	51316-840	SPRAY, METERED	205.50 ug	NASAL	ANDA	15 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53002-1279	SPRAY, METERED	137 ug	NASAL	ANDA	19 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53002-1803	SOLUTION/ DROPS	0.50 mg	INTRAOCULAR	ANDA	16 sections
Azelastine Hydrochloride	Human Prescription Drug Label	1	53002-2279	SPRAY, METERED	137 ug	NASAL	ANDA	25 sections
AZELASTINE HYDROCHLORIDE	Human Prescription Drug Label	1	53002-5279	SPRAY, METERED	137 ug	NASAL	ANDA	26 sections
Astelin	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5072	SPRAY, METERED	137 ug	NASAL	NDA	22 sections
Azelastine Hydrochloride	Human prescription drug label	1	54868-6131	SPRAY, METERED	137 ug	NASAL	ANDA	19 sections
AZELASTINE HYDROCHLORIDE	Human OTC Drug Label	1	58602-020	SPRAY, METERED	205.50 ug	NASAL	ANDA	15 sections
AZELASTINE HYDROCHLORIDE	Human Prescription Drug Label	1	59651-214	SPRAY, METERED	137 ug	NASAL	ANDA	26 sections
AZELASTINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	60505-0578	SOLUTION/ DROPS	0.50 mg	INTRAOCULAR	ANDA	17 sections
AZELASTINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	60505-0578	SOLUTION/ DROPS	0.50 mg	INTRAOCULAR	ANDA	17 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	60505-0833	SPRAY, METERED	137 ug	NASAL	ANDA	19 sections
Azelastine hydrochloride and Fluticasone propionate	HUMAN PRESCRIPTION DRUG LABEL	2	60505-0953	SPRAY, METERED	137 ug	NASAL	ANDA	27 sections
Azelastine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	61314-308	SOLUTION/ DROPS	0.50 mg	INTRAOCULAR	ANDA	16 sections

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azelastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

Drug Use | Suggest Off label Use Form| |View source of the data|

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: