ivabradine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
bradycardic agents	3312	155974-00-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: corlanor corlentor ivabradine hydrochloride ivabradine coraxan procoralan ivabradine HCl	Ivabradine is a pure heart rate lowering agent, acting by selective and specific inhibition of the cardiac pacemaker If current that controls the spontaneous diastolic depolarisation in the sinus node and regulates heart rate. The cardiac effects are specific to the sinus node with no effect on intra-atrial, atrioventricular or intraventricular conduction times, nor on myocardial contractility or ventricular repolarisation. Molecular weight: 468.59 Formula: C27H36N2O5 CLOGP: 3.07 LIPINSKI: 0 HAC: 7 HDO: 0 TPSA: 60.47 ALOGS: -4.36 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

corlanor
corlentor
ivabradine hydrochloride
ivabradine
coraxan
procoralan
ivabradine HCl

Ivabradine is a pure heart rate lowering agent, acting by selective and specific inhibition of the cardiac pacemaker If current that controls the spontaneous diastolic depolarisation in the sinus node and regulates heart rate. The cardiac effects are specific to the sinus node with no effect on intra-atrial, atrioventricular or intraventricular conduction times, nor on myocardial contractility or ventricular repolarisation.

Molecular weight: 468.59
Formula: C27H36N2O5
CLOGP: 3.07
LIPINSKI: 0
HAC: 7
HDO: 0
TPSA: 60.47
ALOGS: -4.36
ROTB: 10

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	4 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.46 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	1.66 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	10.27 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.28 %	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company
Sept. 20, 2019	PMDA	Ono Pharmaceutical Co., Ltd.
April 15, 2015	FDA	AMGEN INC
Oct. 25, 2005	EMA	Les Laboratoires Servier

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
Off label use	429.73	18.43	487	8091	673975	62806469
Photopsia	153.64	18.43	46	8532	4463	63475981
Bradycardia	144.03	18.43	101	8477	73126	63407318
Drug interaction	136.41	18.43	161	8417	228970	63251474
Electrocardiogram QT prolonged	107.54	18.43	78	8500	59452	63420992
Torsade de pointes	104.90	18.43	46	8532	13305	63467139
Ischaemic stroke	86.03	18.43	44	8534	17913	63462531
Cardiac failure	85.70	18.43	81	8497	89061	63391383
Syncope	77.24	18.43	87	8491	117298	63363146
Palpitations	76.63	18.43	85	8493	112685	63367759
First trimester pregnancy	73.23	18.43	10	8568	8	63480436
Drug effective for unapproved indication	63.83	18.43	22	8556	3342	63477102
Chest pain	61.57	18.43	107	8471	215852	63264592
Cardiac failure chronic	57.98	18.43	22	8556	4396	63476048
Congestive cardiomyopathy	57.46	18.43	24	8554	6158	63474286
Dizziness	54.78	18.43	154	8424	429771	63050673
Ventricular fibrillation	53.73	18.43	28	8550	11839	63468605
Crush syndrome	53.55	18.43	10	8568	119	63480325
Myoglobin blood increased	50.75	18.43	15	8563	1390	63479054
Apallic syndrome	50.73	18.43	13	8565	708	63479736
Sinus bradycardia	48.38	18.43	28	8550	14523	63465921
Pain	48.24	18.43	20	8558	740608	62739836
Heart rate decreased	46.82	18.43	43	8535	45517	63434927
Ventricular tachycardia	44.99	18.43	30	8548	19949	63460495
Bundle branch block left	44.91	18.43	21	8557	7038	63473406
Language disorder	44.40	18.43	15	8563	2145	63478299
Acute kidney injury	43.39	18.43	104	8474	263311	63217133
Hypotension	42.10	18.43	105	8473	272499	63207945
Sensorimotor disorder	40.33	18.43	10	8568	476	63479968
Ejection fraction decreased	39.68	18.43	29	8549	22303	63458141
Dyspnoea	38.07	18.43	183	8395	661130	62819314
Pneumobilia	34.94	18.43	7	8571	123	63480321
Orthopnoea	31.90	18.43	16	8562	6245	63474199
Angioedema	30.56	18.43	35	8543	47930	63432514
Hyperparathyroidism secondary	29.41	18.43	10	8568	1457	63478987
Genital rash	29.31	18.43	8	8570	556	63479888
Heart rate increased	28.50	18.43	48	8530	94190	63386254
Shock haemorrhagic	27.58	18.43	17	8561	9878	63470566
Visual impairment	26.86	18.43	44	8534	84402	63396042
Cardiogenic shock	26.80	18.43	21	8557	17911	63462533
Tachycardia	26.64	18.43	53	8525	118103	63362341
Lactic acidosis	26.20	18.43	29	8549	38258	63442186
Anaemia folate deficiency	25.61	18.43	6	8572	224	63480220
Alopecia	25.57	18.43	7	8571	337529	63142915
Acute pulmonary oedema	25.27	18.43	15	8563	8143	63472301
Hyperphosphataemia	25.25	18.43	10	8568	2238	63478206
Mitral valve incompetence	25.16	18.43	21	8557	19573	63460871
Joint swelling	24.44	18.43	7	8571	327659	63152785
Gastric antral vascular ectasia	23.99	18.43	7	8571	620	63479824
Lordosis	23.77	18.43	6	8572	307	63480137
Third trimester pregnancy	23.73	18.43	3	8575	0	63480444
Second trimester pregnancy	23.73	18.43	3	8575	0	63480444
Gastrointestinal tract adenoma	23.32	18.43	6	8572	332	63480112
Bronchospasm	23.19	18.43	19	8559	17261	63463183
Tuberculosis of central nervous system	23.14	18.43	6	8572	342	63480102
Angina pectoris	22.71	18.43	24	8554	30054	63450390
Femoral neck fracture	22.13	18.43	14	8564	8509	63471935
Nasopharyngitis	21.81	18.43	4	8574	254253	63226191
Oliguria	21.29	18.43	14	8564	9087	63471357
Drug ineffective	20.97	18.43	72	8506	1044693	62435751
Metabolic acidosis	20.84	18.43	28	8550	45041	63435403
Lupus myocarditis	20.32	18.43	4	8574	64	63480380
Serotonin syndrome	20.10	18.43	22	8556	28660	63451784
Sinus arrest	19.58	18.43	8	8570	1941	63478503
Pneumonia fungal	19.48	18.43	11	8567	5444	63475000
Postural orthostatic tachycardia syndrome	19.03	18.43	7	8571	1282	63479162
Arthralgia	18.84	18.43	30	8548	569680	62910764
Osteochondrosis	18.58	18.43	7	8571	1370	63479074

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
Cardiac failure	313.05	19.95	231	9202	91017	34856481
Bradycardia	121.01	19.95	124	9309	75294	34872204
Computerised tomogram coronary artery abnormal	120.47	19.95	24	9409	193	34947305
Hypotension	116.04	19.95	211	9222	221438	34726060
Ischaemic cardiomyopathy	90.73	19.95	41	9392	6348	34941150
Photopsia	87.58	19.95	29	9404	1939	34945559
Cardiac failure chronic	82.54	19.95	41	9392	7838	34939660
Ventricular dysfunction	71.56	19.95	30	9403	3875	34943623
Dyspnoea at rest	65.47	19.95	28	9405	3800	34943698
Dyspnoea	61.98	19.95	232	9201	376550	34570948
Cardiomyopathy	58.33	19.95	43	9390	16765	34930733
Asthma-chronic obstructive pulmonary disease overlap syndrome	57.40	19.95	19	9414	1268	34946230
N-terminal prohormone brain natriuretic peptide increased	57.03	19.95	23	9410	2692	34944806
Sinus bradycardia	56.21	19.95	38	9395	12925	34934573
Oesophageal obstruction	55.58	19.95	15	9418	493	34947005
Torsade de pointes	54.06	19.95	30	9403	7179	34940319
Bronchial hyperreactivity	52.13	19.95	19	9414	1690	34945808
Pulmonary oedema	51.84	19.95	64	9369	47465	34900033
Oedema peripheral	51.30	19.95	105	9328	119707	34827791
Left ventricular enlargement	50.78	19.95	15	9418	687	34946811
Ventricular arrhythmia	49.84	19.95	26	9407	5502	34941996
Presyncope	49.33	19.95	41	9392	19018	34928480
Ventricular extrasystoles	49.21	19.95	34	9399	11974	34935524
Ejection fraction decreased	49.15	19.95	41	9392	19113	34928385
Venous pressure jugular increased	48.83	19.95	15	9418	786	34946712
Bezoar	47.31	19.95	16	9417	1141	34946357
Blood pressure systolic decreased	45.88	19.95	23	9410	4480	34943018
Electrocardiogram abnormal	44.67	19.95	29	9404	9218	34938280
Pulmonary function test abnormal	44.33	19.95	19	9414	2591	34944907
Base excess decreased	41.24	19.95	10	9423	212	34947286
Glomerular filtration rate decreased	40.18	19.95	31	9402	12930	34934568
Hyperkalaemia	39.85	19.95	69	9364	69320	34878178
Drug interaction	38.52	19.95	141	9292	225805	34721693
Ventricular tachycardia	37.71	19.95	41	9392	26538	34920960
Dyspnoea exertional	37.43	19.95	52	9381	43227	34904271
Venous pressure jugular decreased	37.21	19.95	7	9426	40	34947458
Breath sounds abnormal	36.76	19.95	23	9410	6858	34940640
Blood potassium increased	35.61	19.95	32	9401	16463	34931035
Product prescribing error	35.41	19.95	37	9396	22890	34924608
Oxygen consumption decreased	34.73	19.95	9	9424	252	34947246
Eosinophilia	34.70	19.95	39	9394	26183	34921315
Atrial tachycardia	32.44	19.95	17	9416	3628	34943870
Urticaria chronic	32.22	19.95	7	9426	89	34947409
Angina pectoris	32.21	19.95	41	9392	31322	34916176
Dermatitis exfoliative generalised	32.17	19.95	17	9416	3690	34943808
Brain natriuretic peptide increased	30.44	19.95	19	9414	5640	34941858
Bronchial wall thickening	30.15	19.95	12	9421	1356	34946142
Tricuspid valve incompetence	29.50	19.95	23	9410	9737	34937761
Blood creatinine increased	29.16	19.95	73	9360	94903	34852595
Oculogyric crisis	28.44	19.95	12	9421	1574	34945924
Syncope	27.77	19.95	70	9363	91381	34856117
Eye movement disorder	27.76	19.95	16	9417	4111	34943387
Sinus arrest	27.37	19.95	12	9421	1728	34945770
Palpitations	27.30	19.95	43	9390	39943	34907555
ECG signs of myocardial ischaemia	27.22	19.95	7	9426	190	34947308
Death	27.16	19.95	41	9392	398008	34549490
Acute kidney injury	27.00	19.95	157	9276	304831	34642667
Ventricular enlargement	26.43	19.95	9	9424	655	34946843
Hypertrophy	25.44	19.95	8	9425	453	34947045
Non-compaction cardiomyopathy	25.23	19.95	5	9428	39	34947459
Left ventricular dilatation	25.16	19.95	9	9424	758	34946740
Tracheal atresia	24.48	19.95	4	9429	8	34947490
Status epilepticus	22.48	19.95	22	9411	12592	34934906
Body mass index increased	22.21	19.95	9	9424	1066	34946432
Left ventricular hypertrophy	22.09	19.95	18	9415	8112	34939386
Supraventricular extrasystoles	22.01	19.95	13	9420	3495	34944003
Cardiac failure acute	21.82	19.95	20	9413	10550	34936948
Acute myocardial infarction	21.67	19.95	46	9387	53673	34893825
Blood chloride increased	21.62	19.95	12	9421	2869	34944629
Cardiac ventricular thrombosis	21.55	19.95	9	9424	1151	34946347
Fluid retention	21.31	19.95	31	9402	26856	34920642
Mean cell haemoglobin decreased	21.25	19.95	10	9423	1696	34945802
Blood luteinising hormone increased	21.24	19.95	5	9428	93	34947405
Mitral valve incompetence	21.10	19.95	23	9410	14920	34932578
Concomitant disease aggravated	20.71	19.95	15	9418	5686	34941812
Oesophageal haemorrhage	20.44	19.95	9	9424	1309	34946189
Lichenoid keratosis	20.35	19.95	11	9422	2497	34945001

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
Cardiac failure	370.91	16.63	288	16704	154554	79572842
Off label use	316.96	16.63	633	16359	906582	78820814
Bradycardia	238.45	16.63	211	16781	135346	79592050
Photopsia	175.24	16.63	59	16933	5277	79722119
Drug interaction	153.68	16.63	298	16694	414885	79312511
Torsade de pointes	149.89	16.63	76	16916	19236	79708160
Hypotension	136.81	16.63	294	16698	440023	79287373
Cardiac failure chronic	136.29	16.63	60	16932	11075	79716321
Computerised tomogram coronary artery abnormal	126.00	16.63	24	16968	194	79727202
Ischaemic cardiomyopathy	95.90	16.63	42	16950	7653	79719743
Syncope	88.19	16.63	146	16846	179303	79548093
Sinus bradycardia	87.76	16.63	59	16933	25188	79702208
Dyspnoea	87.52	16.63	387	16605	856638	78870758
Ventricular tachycardia	83.14	16.63	70	16922	41865	79685531
Palpitations	80.41	16.63	116	16876	126494	79600902
Ejection fraction decreased	79.66	16.63	63	16929	34514	79692882
Electrocardiogram QT prolonged	79.26	16.63	97	16895	90289	79637107
Acute kidney injury	71.68	16.63	258	16734	519146	79208250
Ischaemic stroke	69.19	16.63	57	16935	33074	79694322
First trimester pregnancy	63.78	16.63	9	16983	4	79727392
Ventricular extrasystoles	63.62	16.63	44	16948	19660	79707736
Pain	62.98	16.63	36	16956	703766	79023630
Ventricular dysfunction	62.72	16.63	29	16963	5994	79721402
N-terminal prohormone brain natriuretic peptide increased	62.67	16.63	27	16965	4728	79722668
Left ventricular enlargement	62.60	16.63	17	16975	729	79726667
Chest pain	59.95	16.63	163	16829	282141	79445255
Ventricular fibrillation	58.60	16.63	51	16941	31875	79695521
Ventricular arrhythmia	57.73	16.63	31	16961	8809	79718587
Congestive cardiomyopathy	57.15	16.63	34	16958	11746	79715650
Presyncope	56.78	16.63	56	16936	40998	79686398
Dizziness	56.75	16.63	242	16750	526199	79201197
Angina pectoris	56.18	16.63	62	16930	51670	79675726
Bronchial hyperreactivity	52.71	16.63	21	16971	3019	79724377
Dyspnoea at rest	51.63	16.63	27	16965	7275	79720121
Cardiomyopathy	50.87	16.63	45	16947	28729	79698667
Hyperkalaemia	49.46	16.63	88	16904	114310	79613086
Glomerular filtration rate decreased	49.37	16.63	40	16952	22662	79704734
Oesophageal obstruction	48.65	16.63	15	16977	1011	79726385
ECG signs of myocardial ischaemia	48.52	16.63	12	16980	354	79727042
Asthma-chronic obstructive pulmonary disease overlap syndrome	48.14	16.63	20	16972	3201	79724195
Atrial tachycardia	46.54	16.63	25	16967	7108	79720288
Mitral valve incompetence	45.25	16.63	42	16950	28523	79698873
Bundle branch block left	45.10	16.63	29	16963	11484	79715912
Drug effective for unapproved indication	44.76	16.63	23	16969	5978	79721418
Crush syndrome	44.24	16.63	10	16982	198	79727198
Pulmonary function test abnormal	43.30	16.63	20	16972	4124	79723272
Eosinophilia	41.90	16.63	50	16942	45295	79682101
Oedema peripheral	41.42	16.63	133	16859	252155	79475241
Apallic syndrome	41.08	16.63	13	16979	955	79726441
Venous pressure jugular increased	40.79	16.63	14	16978	1326	79726070
Dyspnoea exertional	40.26	16.63	69	16923	87004	79640392
Tricuspid valve incompetence	39.25	16.63	33	16959	19679	79707717
Base excess decreased	38.09	16.63	10	16982	376	79727020
Bezoar	37.86	16.63	16	16976	2672	79724724
Blood pressure systolic decreased	36.38	16.63	25	16967	11051	79716345
Pulmonary oedema	35.74	16.63	66	16926	88188	79639208
Venous pressure jugular decreased	34.24	16.63	7	16985	84	79727312
Brain natriuretic peptide increased	33.83	16.63	22	16970	8878	79718518
Blood potassium increased	33.37	16.63	36	16956	29239	79698157
Sinus arrest	33.29	16.63	16	16976	3606	79723790
Blood creatinine increased	32.33	16.63	89	16903	154968	79572428
Body mass index increased	32.29	16.63	13	16979	1920	79725476
Myoglobin blood increased	32.27	16.63	15	16977	3136	79724260
Language disorder	31.99	16.63	15	16977	3199	79724197
Oxygen consumption decreased	31.78	16.63	9	16983	451	79726945
Orthopnoea	31.36	16.63	22	16970	10051	79717345
Electrocardiogram abnormal	31.24	16.63	27	16965	16710	79710686
Nasopharyngitis	30.87	16.63	8	16984	253873	79473523
Rheumatoid arthritis	30.84	16.63	4	16988	208466	79518930
Dermatitis exfoliative generalised	30.26	16.63	19	16973	7222	79720174
Joint swelling	29.97	16.63	12	16980	288634	79438762
Sensorimotor disorder	29.80	16.63	10	16982	884	79726512
Product prescribing error	29.79	16.63	42	16950	44771	79682625
Arthralgia	29.29	16.63	48	16944	571755	79155641
Acute pulmonary oedema	28.70	16.63	24	16968	14206	79713190
Alopecia	28.69	16.63	7	16985	231348	79496048
Infusion related reaction	28.48	16.63	7	16985	230230	79497166
Cardiac failure acute	28.38	16.63	27	16965	18902	79708494
Ventricular enlargement	27.66	16.63	9	16983	723	79726673
Pneumobilia	27.52	16.63	7	16985	232	79727164
Non-compaction cardiomyopathy	26.41	16.63	5	16987	39	79727357
Breath sounds abnormal	26.28	16.63	24	16968	15960	79711436
Hepatic enzyme increased	25.85	16.63	4	16988	182606	79544790
Diastolic dysfunction	25.54	16.63	20	16972	10791	79716605
Osteochondrosis	25.21	16.63	11	16981	1985	79725411
Urticaria chronic	25.14	16.63	8	16984	598	79726798
Blood pressure decreased	24.73	16.63	61	16931	99405	79627991
Vertigo	24.68	16.63	49	16943	69033	79658363
Low cardiac output syndrome	24.52	16.63	9	16983	1036	79726360
Musculoskeletal stiffness	24.39	16.63	4	16988	175004	79552392
Sinusitis	24.07	16.63	6	16986	195495	79531901
Lactic acidosis	24.06	16.63	49	16943	70310	79657086
Dyspnoea paroxysmal nocturnal	24.05	16.63	11	16981	2217	79725179
Oculogyric crisis	24.02	16.63	12	16980	2940	79724456
Abdominal discomfort	23.56	16.63	12	16980	250715	79476681
Cardiac ventricular thrombosis	23.14	16.63	10	16982	1763	79725633
Heart rate decreased	22.90	16.63	48	16944	70268	79657128
Hypertrophy	22.86	16.63	8	16984	802	79726594
Completed suicide	22.74	16.63	12	16980	245755	79481641
Mean cell haemoglobin decreased	22.72	16.63	15	16977	6209	79721187
Arthropathy	22.66	16.63	5	16987	177106	79550290
Second trimester pregnancy	22.36	16.63	3	16989	0	79727396
Third trimester pregnancy	22.36	16.63	3	16989	0	79727396
Bronchial wall thickening	22.27	16.63	11	16981	2630	79724766
Acute myocardial infarction	22.14	16.63	50	16942	76986	79650410
Infection	22.07	16.63	12	16980	241700	79485696
Exercise tolerance decreased	21.90	16.63	17	16975	9054	79718342
Eye movement disorder	21.52	16.63	16	16976	7995	79719401
Supraventricular extrasystoles	21.15	16.63	15	16977	6972	79720424
Anaemia folate deficiency	21.14	16.63	6	16986	303	79727093
Genital rash	21.00	16.63	8	16984	1020	79726376
Left ventricular hypertrophy	20.78	16.63	18	16974	11173	79716223
Acute coronary syndrome	20.67	16.63	24	16968	21109	79706287
Arrhythmia	20.16	16.63	42	16950	61230	79666166
Oesophageal haemorrhage	19.95	16.63	9	16983	1758	79725638
Haematoma	19.83	16.63	38	16954	52157	79675239
Conduction disorder	19.71	16.63	11	16981	3368	79724028
Muscular weakness	19.65	16.63	5	16987	160724	79566672
Rash	19.45	16.63	61	16931	578297	79149099
Feeling abnormal	19.28	16.63	76	16916	159123	79568273
Hyperparathyroidism secondary	19.27	16.63	10	16982	2650	79724746
International normalised ratio decreased	19.21	16.63	15	16977	8055	79719341
Kyphosis	19.16	16.63	10	16982	2681	79724715
Cardiogenic shock	19.08	16.63	33	16959	41881	79685515
Left ventricular dysfunction	18.96	16.63	22	16970	19339	79708057
Lordosis	18.90	16.63	6	16986	445	79726951
Blood luteinising hormone increased	18.60	16.63	5	16987	206	79727190
Tuberculosis of central nervous system	18.38	16.63	6	16986	487	79726909
Shock haemorrhagic	18.33	16.63	22	16970	20038	79707358
Gastrointestinal tract adenoma	18.28	16.63	6	16986	495	79726901
Cardiac disorder	18.14	16.63	42	16950	65715	79661681
Wrong technique in product usage process	18.03	16.63	45	16947	73830	79653566
Gastric antral vascular ectasia	17.95	16.63	7	16985	951	79726445
Sudden death	17.86	16.63	23	16969	22488	79704908
Blood chloride increased	17.79	16.63	12	16980	5144	79722252
Febrile neutropenia	17.66	16.63	14	16978	230985	79496411
Circulatory collapse	17.60	16.63	30	16962	37638	79689758
Intentional overdose	17.48	16.63	56	16936	105904	79621492
Drug hypersensitivity	17.32	16.63	23	16969	298893	79428503
Lupus myocarditis	17.17	16.63	4	16988	91	79727305

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C01EB17	CARDIOVASCULAR SYSTEM CARDIAC THERAPY OTHER CARDIAC PREPARATIONS Other cardiac preparations
ATC	C07FX05	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents, other combinations
ATC	C07FX06	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents, other combinations
MeSH PA	D002317	Cardiovascular Agents
FDA EPC	N0000191544	Hyperpolarization-activated Cyclic Nucleotide-gated Channel Blocker
FDA MoA	N0000191546	Hyperpolarization-activated Cyclic Nucleotide-gated Channel Antagonists
CHEBI has role	CHEBI:38147	cardiotonic drugs

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

Disease	Relation	SNOMED_ID	DOID
Chronic heart failure	indication	48447003
Angina pectoris	indication	194828000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.45	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 5MG BASE	CORLANOR	AMGEN INC	N206143	April 15, 2015	RX	TABLET	ORAL	7361649	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
EQ 5MG BASE	CORLANOR	AMGEN INC	N206143	April 15, 2015	RX	TABLET	ORAL	7361650	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
EQ 5MG BASE	CORLANOR	AMGEN INC	N206143	April 15, 2015	RX	TABLET	ORAL	7879842	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
EQ 7.5MG BASE	CORLANOR	AMGEN INC	N206143	April 15, 2015	RX	TABLET	ORAL	7361649	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
EQ 7.5MG BASE	CORLANOR	AMGEN INC	N206143	April 15, 2015	RX	TABLET	ORAL	7361650	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
EQ 7.5MG BASE	CORLANOR	AMGEN INC	N206143	April 15, 2015	RX	TABLET	ORAL	7879842	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
5MG/5ML (1MG/ML)	CORLANOR	AMGEN INC	N209964	April 22, 2019	RX	SOLUTION	ORAL	7361649	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
5MG/5ML (1MG/ML)	CORLANOR	AMGEN INC	N209964	April 22, 2019	RX	SOLUTION	ORAL	7361650	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
5MG/5ML (1MG/ML)	CORLANOR	AMGEN INC	N209964	April 22, 2019	RX	SOLUTION	ORAL	7879842	Feb. 22, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
EQ 5MG BASE	CORLANOR	AMGEN INC	N206143	April 15, 2015	RX	TABLET	ORAL	7867996	Dec. 12, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
EQ 7.5MG BASE	CORLANOR	AMGEN INC	N206143	April 15, 2015	RX	TABLET	ORAL	7867996	Dec. 12, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE
5MG/5ML (1MG/ML)	CORLANOR	AMGEN INC	N209964	April 22, 2019	RX	SOLUTION	ORAL	7867996	Dec. 12, 2026	A METHOD FOR TREATING HEART FAILURE IN A HUMAN USING A CRYSTALLINE FORM OF IVABRADINE HYDROCHLORIDE

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
5MG/5ML (1MG/ML)	CORLANOR	AMGEN INC	N209964	April 22, 2019	RX	SOLUTION	ORAL	April 22, 2026	INDICATED FOR THE TREATMENT OF STABLE SYMPTOMATIC HEART FAILURE DUE TO DILATED CARDIOMYOPATHY (DCM) IN PEDIATRIC PATIENTS AGED 6 MONTHS AND OLDER, WHO ARE IN SINUS RHYTHM WITH AN ELEVATED HEART RATE
5MG/5ML (1MG/ML)	CORLANOR	AMGEN INC	N209964	April 22, 2019	RX	SOLUTION	ORAL	Oct. 22, 2026	PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1	Ion channel	O60741	HCN1_HUMAN	BLOCKER	IC50	5.70	IUPHAR	DRUG LABEL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2	Ion channel	Q9UL51	HCN2_HUMAN	BLOCKER			UNKNOWN	DRUG LABEL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 3	Ion channel	Q9P1Z3	HCN3_HUMAN	BLOCKER	IC50	5.70	IUPHAR	DRUG LABEL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4	Ion channel	Q9Y3Q4	HCN4_HUMAN		EC50	5.37	CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1	Ion channel		HCN1_MOUSE		EC50	5.35	CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2	Ion channel		HCN2_MOUSE		EC50	5.34	CHEMBL

External reference:

ID	Source
D07165	KEGG_DRUG
148849-67-6	SECONDARY_CAS_RN
4034416	VANDF
C0257190	UMLSCUI
CHEBI:85969	CHEBI
CHEMBL471737	ChEMBL_ID
CHEMBL2145077	ChEMBL_ID
D000077550	MESH_DESCRIPTOR_UI
DB09083	DRUGBANK_ID
2357	IUPHAR_LIGAND_ID
7523	INN_ID
3H48L0LPZQ	UNII
132999	PUBCHEM_CID
1649479	RXNORM
20884	MMSL
233849	MMSL
d05706	MMSL
011156	NDDF
011157	NDDF
420906000	SNOMEDCT_US
421228002	SNOMEDCT_US
421692002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-800	TABLET, FILM COATED	5 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-800	TABLET, FILM COATED	5 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-800	TABLET, FILM COATED	5 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-810	TABLET, FILM COATED	7.50 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-810	TABLET, FILM COATED	7.50 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-810	TABLET, FILM COATED	7.50 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-813	SOLUTION	5 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-813	SOLUTION	5 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	55513-813	SOLUTION	5 mg	ORAL	NDA	31 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	70518-3309	TABLET, FILM COATED	5 mg	ORAL	NDA	33 sections
Corlanor	HUMAN PRESCRIPTION DRUG LABEL	1	70518-3309	TABLET, FILM COATED	5 mg	ORAL	NDA	33 sections