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

Stem definitionDrug idCAS RN
bradycardic agents 3312 155974-00-8

Description:

MoleculeDescription

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:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
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
BA (Bioavailability) 40 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.427 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 10.471 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 7.816 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 16.943 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 37.650 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 58.720 % High 1
herg hERG pIC50 5.360 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 3.673 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 100.693 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 31.070 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK 43
kinase-selectivity-class AXL,EIF2AK3,EPHB4,ERBB2,GRK2,PDK4,PIK3CB,PRKDC,SIK2,TEK,TTK 11
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 8.356 High 1
mh-clint Mouse hepatocyte intrinsic clearance 53.211 High 1
mppb Mouse plasma protein binding (% unbound) 32.930 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 26.303 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 59.990 % High 1
rh-clint Rat hepatocyte intrinsic clearance 32.659 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 73 % High 1
rppb Rat plasma protein binding (% unbound) 31.120 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 963.829 uM High 1

Approvals:

DateAgencyCompanyOrphan
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 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
Off label use 343.61 18.42 539 10726 1101713 89515469
Bradycardia 189.11 18.42 122 11143 83725 90533457
Drug interaction 168.64 18.42 189 11076 276264 90340918
Photopsia 165.50 18.42 49 11216 4975 90612207
Cardiac failure 140.22 18.42 113 11152 109383 90507799
Electrocardiogram QT prolonged 110.59 18.42 83 11182 72373 90544809
Torsade de pointes 109.32 18.42 48 11217 15134 90602048
Palpitations 109.08 18.42 108 11157 136620 90480562
Syncope 104.36 18.42 104 11161 132559 90484623
Ischaemic stroke 94.89 18.42 49 11216 22117 90595065
Hypotension 77.24 18.42 142 11123 325255 90291927
Apallic syndrome 70.60 18.42 17 11248 779 90616403
Congestive cardiomyopathy 68.76 18.42 28 11237 7326 90609856
Dizziness 64.00 18.42 189 11076 589095 90028087
Ventricular fibrillation 62.86 18.42 32 11233 14012 90603170
First trimester pregnancy 60.70 18.42 8 11257 4 90617178
Heart rate decreased 59.63 18.42 51 11214 53454 90563728
Myoglobin blood increased 59.34 18.42 17 11248 1535 90615647
Endocarditis enterococcal 59.09 18.42 12 11253 247 90616935
Cardiac failure chronic 57.99 18.42 23 11242 5623 90611559
Chest pain 57.18 18.42 124 11141 319521 90297661
Drug effective for unapproved indication 56.88 18.42 25 11240 7893 90609289
Orthopnoea 53.74 18.42 23 11242 6812 90610370
Serum amyloid A protein increased 51.87 18.42 13 11252 704 90616478
Sinus bradycardia 51.82 18.42 30 11235 16922 90600260
Respiratory syncytial virus test positive 51.49 18.42 14 11251 1044 90616138
Mitral valve replacement 50.87 18.42 12 11253 503 90616679
Ventricular tachycardia 50.86 18.42 34 11231 24674 90592508
Bundle branch block left 47.45 18.42 22 11243 7863 90609319
Crush syndrome 45.66 18.42 10 11255 299 90616883
Vascular stent stenosis 42.71 18.42 11 11254 665 90616517
Language disorder 42.61 18.42 15 11250 2637 90614545
Dyspnoea 42.14 18.42 218 11047 880737 89736445
Pain 41.28 18.42 38 11227 996303 89620879
Acute kidney injury 40.79 18.42 109 11156 320278 90296904
Aortic valve replacement 39.01 18.42 11 11254 938 90616244
Angina pectoris 38.95 18.42 35 11230 39125 90578057
Heart rate increased 38.42 18.42 58 11207 112844 90504338
Ejection fraction decreased 37.65 18.42 29 11236 26224 90590958
Sensorimotor disorder 36.79 18.42 10 11255 745 90616437
Tachycardia 36.30 18.42 68 11197 157605 90459577
Joint swelling 36.24 18.42 9 11256 503291 90113891
Visual impairment 35.47 18.42 61 11204 132304 90484878
Pneumobilia 33.60 18.42 7 11258 164 90617018
Mitral valve incompetence 32.56 18.42 25 11240 22499 90594683
Vision blurred 32.45 18.42 53 11212 110240 90506942
Ventricular hypokinesia 32.44 18.42 15 11250 5326 90611856
Bronchospasm 32.18 18.42 24 11241 20685 90596497
Arrhythmia 31.06 18.42 32 11233 42300 90574882
Cardiogenic shock 30.73 18.42 25 11240 24443 90592739
Varices oesophageal 30.64 18.42 13 11252 3766 90613416
Angioedema 30.58 18.42 39 11226 64837 90552345
Alopecia 30.03 18.42 12 11253 495059 90122123
Postural orthostatic tachycardia syndrome 29.57 18.42 11 11254 2261 90614921
Genital rash 28.81 18.42 8 11257 645 90616537
Spinal pain 28.43 18.42 20 11245 15747 90601435
Hyperparathyroidism secondary 28.22 18.42 10 11255 1791 90615391
Gastric antral vascular ectasia 26.92 18.42 8 11257 821 90616361
Agranulocytosis 26.66 18.42 27 11238 34975 90582207
Shock haemorrhagic 25.56 18.42 17 11248 12228 90604954
Oliguria 25.24 18.42 16 11249 10608 90606574
Serotonin syndrome 24.88 18.42 27 11238 37860 90579322
Hyperphosphataemia 24.35 18.42 11 11254 3700 90613482
Therapeutic product effect decreased 24.22 18.42 3 11262 277568 90339614
Haematoma 24.21 18.42 27 11238 39021 90578161
Acute pulmonary oedema 24.20 18.42 15 11250 9565 90607617
Lordosis 23.87 18.42 6 11259 329 90616853
Infusion related reaction 23.83 18.42 11 11254 416769 90200413
Intentional overdose 23.52 18.42 42 11223 93792 90523390
Blood pressure decreased 23.40 18.42 37 11228 74858 90542324
Tuberculosis of central nervous system 23.37 18.42 6 11259 358 90616824
Tracheal atresia 23.30 18.42 4 11261 31 90617151
Gastrointestinal tract adenoma 23.07 18.42 6 11259 377 90616805
Pneumonia fungal 22.98 18.42 13 11252 7018 90610164
Abdominal discomfort 22.45 18.42 16 11249 477312 90139870
Metabolic acidosis 22.43 18.42 31 11234 55645 90561537
Drug ineffective for unapproved indication 22.32 18.42 34 11231 66610 90550572
Shrinking lung syndrome 22.21 18.42 5 11260 170 90617012
Lactic acidosis 21.70 18.42 29 11236 50434 90566748
Systemic lupus erythematosus 21.56 18.42 9 11256 361887 90255295
Hyperkalaemia 21.56 18.42 33 11232 64931 90552251
Nasopharyngitis 21.40 18.42 12 11253 407092 90210090
Cardiac arrest 21.38 18.42 43 11222 104892 90512290
Tachypnoea 21.10 18.42 19 11246 21290 90595892
Anaemia folate deficiency 20.96 18.42 6 11259 540 90616642
Femoral neck fracture 20.86 18.42 14 11251 10219 90606963
Lethargy 20.85 18.42 32 11233 63107 90554075
Osteochondrosis 20.66 18.42 8 11257 1835 90615347
Lupus myocarditis 20.42 18.42 4 11261 68 90617114
Hypersensitivity 20.40 18.42 16 11249 454661 90162521
Mydriasis 20.26 18.42 16 11249 14996 90602186
Rheumatoid arthritis 20.07 18.42 10 11255 362604 90254578
Atrial fibrillation 19.60 18.42 48 11217 133563 90483619
Sinus arrest 19.48 18.42 8 11257 2138 90615044
Treatment failure 19.02 18.42 7 11258 303921 90313261
Bleeding varicose vein 18.48 18.42 5 11260 366 90616816

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
Cardiac failure 362.31 20.19 263 10641 106593 42503838
Bradycardia 169.26 20.19 154 10750 85330 42525101
Hypotension 141.42 20.19 243 10661 257388 42353043
Ischaemic cardiomyopathy 105.02 20.19 45 10859 6477 42603954
Photopsia 95.28 20.19 32 10872 2360 42608071
Ventricular dysfunction 92.58 20.19 37 10867 4466 42605965
Computerised tomogram coronary artery abnormal 92.41 20.19 18 10886 135 42610296
Cardiac failure chronic 91.32 20.19 46 10858 9555 42600876
N-terminal prohormone brain natriuretic peptide increased 73.17 20.19 29 10875 3424 42607007
Dyspnoea 71.20 20.19 261 10643 442360 42168071
Asthma-chronic obstructive pulmonary disease overlap syndrome 70.68 20.19 23 10881 1536 42608895
Dyspnoea at rest 67.35 20.19 29 10875 4220 42606211
Pulmonary oedema 66.70 20.19 75 10829 53197 42557234
Cardiomyopathy 66.39 20.19 48 10856 19162 42591269
Bronchial hyperreactivity 65.88 20.19 23 10881 1906 42608525
Presyncope 64.16 20.19 50 10854 22337 42588094
Ejection fraction decreased 62.58 20.19 49 10855 22038 42588393
Oedema peripheral 58.74 20.19 116 10788 135960 42474471
Pulmonary function test abnormal 58.39 20.19 23 10881 2671 42607760
Sinus bradycardia 58.02 20.19 40 10864 14813 42595618
Venous pressure jugular increased 54.52 20.19 16 10888 756 42609675
Oesophageal obstruction 53.85 20.19 15 10889 587 42609844
Torsade de pointes 53.27 20.19 31 10873 8563 42601868
Electrocardiogram abnormal 51.02 20.19 32 10872 10113 42600318
Ventricular arrhythmia 50.83 20.19 27 10877 6252 42604179
Ventricular extrasystoles 49.81 20.19 35 10869 13355 42597076
Left ventricular enlargement 49.05 20.19 15 10889 817 42609614
Bezoar 46.61 20.19 16 10888 1260 42609171
Hyperkalaemia 45.32 20.19 77 10827 80381 42530050
Blood pressure systolic decreased 44.81 20.19 23 10881 4964 42605467
Drug interaction 43.18 20.19 158 10746 266841 42343590
Dyspnoea exertional 42.43 20.19 58 10846 50090 42560341
Base excess decreased 42.32 20.19 10 10894 200 42610231
Ventricular tachycardia 42.13 20.19 45 10859 30115 42580316
Blood potassium increased 37.76 20.19 34 10870 18502 42591929
Venous pressure jugular decreased 37.73 20.19 7 10897 39 42610392
Glomerular filtration rate decreased 37.33 20.19 32 10872 16319 42594112
Eosinophilia 37.25 20.19 44 10860 32855 42577576
Breath sounds abnormal 36.80 20.19 28 10876 12065 42598366
Angina pectoris 35.61 20.19 43 10861 32853 42577578
Tricuspid valve incompetence 34.41 20.19 26 10878 11087 42599344
Atrial tachycardia 34.07 20.19 18 10886 4122 42606309
Oxygen consumption decreased 33.64 20.19 9 10895 302 42610129
Brain natriuretic peptide increased 33.15 20.19 21 10883 6749 42603682
Product prescribing error 31.36 20.19 36 10868 26076 42584355
Mitral valve incompetence 31.15 20.19 29 10875 16460 42593971
Bronchial wall thickening 30.84 20.19 12 10892 1348 42609083
Death 30.49 20.19 46 10858 471139 42139292
Fluid retention 30.48 20.19 39 10865 31580 42578851
Blood creatinine increased 29.77 20.19 78 10826 109925 42500506
Urticaria chronic 29.12 20.19 7 10897 151 42610280
Concomitant disease aggravated 28.73 20.19 19 10885 6567 42603864
Left ventricular dilatation 27.88 20.19 10 10894 896 42609535
Cardiac failure acute 27.75 20.19 25 10879 13608 42596823
Syncope 27.42 20.19 71 10833 99335 42511096
ECG signs of myocardial ischaemia 27.31 20.19 7 10897 198 42610233
Ventricular enlargement 26.65 20.19 9 10895 674 42609757
Palpitations 26.47 20.19 47 10857 50750 42559681
Dermatitis exfoliative generalised 25.89 20.19 17 10887 5807 42604624
Sinus arrest 25.52 20.19 12 10892 2144 42608287
Diastolic dysfunction 25.38 20.19 18 10886 6965 42603466
Serum amyloid A protein increased 25.35 20.19 7 10897 265 42610166
Hypertrophy 25.02 20.19 8 10896 505 42609926
Body mass index increased 24.98 20.19 10 10894 1211 42609220
Tracheal atresia 24.69 20.19 4 10900 8 42610423
Dizziness 24.45 20.19 127 10777 249127 42361304
Cardiac ventricular thrombosis 24.24 20.19 11 10893 1811 42608620
Non-compaction cardiomyopathy 23.95 20.19 5 10899 55 42610376
Congestive cardiomyopathy 23.86 20.19 19 10885 8745 42601686
Acute kidney injury 23.82 20.19 168 10736 367169 42243262
Low cardiac output syndrome 23.11 20.19 8 10896 646 42609785
Left ventricular hypertrophy 22.83 20.19 19 10885 9300 42601131
Psoriasis 22.83 20.19 43 10861 48561 42561870
Contraindicated product administered 22.53 20.19 30 10874 25242 42585189
Blood luteinising hormone increased 21.66 20.19 5 10899 90 42610341
Supraventricular extrasystoles 21.06 20.19 13 10891 3993 42606438
Acute myocardial infarction 20.84 20.19 46 10858 58119 42552312
Oesophageal haemorrhage 20.29 20.19 9 10895 1405 42609026

FDA Adverse Event Reporting System (Geriatric)

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
Cardiac failure 488.43 16.05 349 20449 187277 110381224
Bradycardia 334.22 16.05 258 20540 155259 110413242
Off label use 242.35 16.05 721 20077 1499464 109069037
Hypotension 209.31 16.05 362 20436 523487 110045014
Photopsia 197.47 16.05 65 20733 6149 110562352
Drug interaction 193.71 16.05 341 20457 499842 110068659
Torsade de pointes 156.26 16.05 79 20719 22521 110545980
Cardiac failure chronic 146.98 16.05 65 20733 13746 110554755
Ischaemic cardiomyopathy 116.25 16.05 47 20751 7964 110560537
Syncope 112.44 16.05 163 20635 202373 110366128
Dyspnoea 104.17 16.05 447 20351 1106425 109462076
Computerised tomogram coronary artery abnormal 97.82 16.05 18 20780 136 110568365
Ventricular tachycardia 96.53 16.05 78 20720 49931 110518570
Ejection fraction decreased 94.62 16.05 71 20727 40809 110527692
Palpitations 94.02 16.05 132 20666 159080 110409421
Sinus bradycardia 93.31 16.05 62 20736 29421 110539080
Electrocardiogram QT prolonged 88.87 16.05 106 20692 108854 110459647
N-terminal prohormone brain natriuretic peptide increased 85.69 16.05 35 20763 6086 110562415
Cardiomyopathy 79.31 16.05 59 20739 33466 110535035
Ventricular dysfunction 78.79 16.05 35 20763 7476 110561025
Presyncope 77.34 16.05 68 20730 48819 110519682
Serum amyloid A protein increased 74.72 16.05 20 20778 922 110567579
Ischaemic stroke 74.68 16.05 62 20736 41201 110527300
Dizziness 74.12 16.05 293 20505 697900 109870601
Congestive cardiomyopathy 73.64 16.05 41 20757 14178 110554323
Acute kidney injury 71.78 16.05 272 20526 635158 109933343
Bronchial hyperreactivity 69.94 16.05 26 20772 3518 110564983
Ventricular extrasystoles 65.40 16.05 45 20753 22596 110545905
Hyperkalaemia 64.93 16.05 102 20696 135694 110432807
Ventricular fibrillation 64.42 16.05 57 20741 41256 110527245
Mitral valve incompetence 62.23 16.05 51 20747 33278 110535223
Left ventricular enlargement 62.09 16.05 17 20781 854 110567647
Ventricular arrhythmia 60.33 16.05 32 20766 10055 110558446
Dyspnoea at rest 60.10 16.05 30 20768 8316 110560185
Chest pain 59.07 16.05 180 20618 376195 110192306
Apallic syndrome 58.07 16.05 17 20781 1089 110567412
Pulmonary function test abnormal 57.96 16.05 25 20773 4975 110563526
Orthopnoea 57.68 16.05 32 20766 10989 110557512
First trimester pregnancy 57.39 16.05 8 20790 4 110568497
Angina pectoris 56.45 16.05 64 20734 62231 110506270
Pain 55.27 16.05 59 20739 954896 109613605
Dyspnoea exertional 52.30 16.05 80 20718 103980 110464521
Asthma-chronic obstructive pulmonary disease overlap syndrome 52.27 16.05 25 20773 6319 110562182
Pulmonary oedema 51.46 16.05 78 20720 100581 110467920
Bundle branch block left 50.45 16.05 31 20767 12857 110555644
Endocarditis enterococcal 49.65 16.05 12 20786 365 110568136
ECG signs of myocardial ischaemia 48.14 16.05 12 20786 416 110568085
Drug effective for unapproved indication 47.76 16.05 31 20767 14136 110554365
Oesophageal obstruction 47.66 16.05 15 20783 1228 110567273
Glomerular filtration rate decreased 47.25 16.05 41 20757 28915 110539586
Eosinophilia 46.62 16.05 56 20742 57880 110510621
Venous pressure jugular increased 46.42 16.05 15 20783 1337 110567164
Atrial tachycardia 46.26 16.05 26 20772 9152 110559349
Joint swelling 46.26 16.05 13 20785 442832 110125669
Oedema peripheral 45.88 16.05 151 20647 328509 110239992
Mitral valve replacement 43.61 16.05 12 20786 614 110567887
Tricuspid valve incompetence 43.46 16.05 36 20762 23837 110544664
Electrocardiogram abnormal 42.18 16.05 32 20766 18677 110549824
Infusion related reaction 42.08 16.05 10 20788 381152 110187349
Brain natriuretic peptide increased 41.44 16.05 26 20772 11183 110557318
Respiratory syncytial virus test positive 41.01 16.05 14 20784 1480 110567021
Hepatic enzyme increased 40.57 16.05 6 20792 320886 110247615
Blood pressure systolic decreased 39.49 16.05 27 20771 13414 110555087
Crush syndrome 39.10 16.05 10 20788 385 110568116
Cardiac failure acute 39.09 16.05 34 20764 24044 110544457
Base excess decreased 38.88 16.05 10 20788 394 110568107
Musculoskeletal stiffness 38.37 16.05 4 20794 279818 110288683
Acute myocardial infarction 37.38 16.05 61 20737 83716 110484785
Arthropathy 37.23 16.05 5 20793 287517 110280984
Blood potassium increased 36.85 16.05 38 20760 33211 110535290
Ventricular hypokinesia 36.49 16.05 24 20774 11190 110557311
Rhabdomyolysis 36.34 16.05 74 20724 120327 110448174
Myoglobin blood increased 35.85 16.05 17 20781 4215 110564286
Nasopharyngitis 35.28 16.05 15 20783 394346 110174155
Abdominal discomfort 35.20 16.05 15 20783 393843 110174658
Blood creatinine increased 34.99 16.05 94 20704 182795 110385706
Venous pressure jugular decreased 34.81 16.05 7 20791 88 110568413
Arrhythmia 34.26 16.05 53 20745 69522 110498979
Bezoar 33.47 16.05 16 20782 4038 110564463
Sinus arrest 32.78 16.05 16 20782 4226 110564275
Heart rate decreased 32.60 16.05 57 20741 82699 110485802
Aortic valve replacement 32.35 16.05 12 20786 1614 110566887
Diastolic dysfunction 31.98 16.05 23 20775 12381 110556120
Breath sounds abnormal 31.77 16.05 31 20767 25373 110543128
Oxygen consumption decreased 31.66 16.05 9 20789 519 110567982
Blood pressure decreased 31.54 16.05 68 20730 115023 110453478
Body mass index increased 31.51 16.05 13 20785 2317 110566184
Language disorder 31.24 16.05 15 20783 3823 110564678
Rheumatoid arthritis 30.89 16.05 9 20789 299604 110268897
Acute pulmonary oedema 29.63 16.05 25 20773 16971 110551530
Intentional overdose 29.37 16.05 72 20726 132429 110436072
Low cardiac output syndrome 28.94 16.05 10 20788 1096 110567405
Ventricular enlargement 28.86 16.05 9 20789 715 110567786
Sinusitis 28.66 16.05 10 20788 296678 110271823
Drug hypersensitivity 28.56 16.05 26 20772 454064 110114437
Sensorimotor disorder 28.37 16.05 10 20788 1162 110567339
Product prescribing error 27.97 16.05 41 20757 51290 110517211
Alopecia 27.95 16.05 17 20781 364736 110203765
Cardiac ventricular thrombosis 27.76 16.05 13 20785 3134 110565367
Dyspnoea paroxysmal nocturnal 27.34 16.05 12 20786 2490 110566011
Osteochondrosis 27.25 16.05 12 20786 2509 110565992
Rash 26.87 16.05 73 20725 820891 109747610
Cardiac disorder 26.81 16.05 50 20748 76230 110492271
Hypersensitivity 26.78 16.05 22 20776 403976 110164525
Haematoma 26.66 16.05 43 20755 58433 110510068
Wound 26.16 16.05 6 20792 234431 110334070
Pneumobilia 26.14 16.05 7 20791 323 110568178
Vertigo 25.74 16.05 53 20745 86817 110481684
Systemic lupus erythematosus 25.56 16.05 8 20790 254330 110314171
Atrial fibrillation 25.56 16.05 98 20700 229544 110338957
Gastrointestinal disorder 25.44 16.05 7 20791 241945 110326556
Dermatitis exfoliative generalised 25.25 16.05 19 20779 10953 110557548
Non-compaction cardiomyopathy 25.16 16.05 5 20793 59 110568442
Feeling abnormal 25.16 16.05 83 20715 180628 110387873
Acute coronary syndrome 24.86 16.05 26 20772 23086 110545415
Stomatitis 24.61 16.05 10 20788 270232 110298269
Lactic acidosis 24.47 16.05 54 20744 92757 110475744
Urticaria chronic 24.26 16.05 8 20790 760 110567741
Impaired healing 24.12 16.05 4 20794 196713 110371788
Spinal pain 23.91 16.05 23 20775 18492 110550009
Exercise tolerance decreased 23.65 16.05 19 20779 12048 110556453
Vitreous detachment 23.48 16.05 11 20787 2654 110565847
Hypertrophy 22.72 16.05 8 20790 927 110567574
Mean cell haemoglobin decreased 22.48 16.05 15 20783 7159 110561342
Angina unstable 22.34 16.05 21 20777 16411 110552090
Swelling 22.19 16.05 20 20778 351021 110217480
Left ventricular hypertrophy 22.10 16.05 19 20779 13225 110555276
Bronchial wall thickening 21.55 16.05 11 20787 3196 110565305
Circulatory collapse 21.51 16.05 33 20765 42960 110525541
Infection 21.30 16.05 22 20776 362178 110206323
Left ventricular dysfunction 21.04 16.05 24 20774 23469 110545032
Wrong technique in product usage process 21.00 16.05 49 20749 87299 110481202
Hypoaesthesia 20.96 16.05 17 20781 314206 110254295
Irritable bowel syndrome 20.91 16.05 3 20795 164212 110404289
Supraventricular extrasystoles 20.88 16.05 15 20783 8058 110560443
Heart rate increased 20.86 16.05 67 20731 143767 110424734
Arthralgia 20.80 16.05 76 20722 779556 109788945
Gastric antral vascular ectasia 20.79 16.05 8 20790 1189 110567312
Cardiogenic shock 20.67 16.05 38 20760 57300 110511201
International normalised ratio decreased 20.61 16.05 15 20783 8221 110560280
Oesophageal haemorrhage 20.38 16.05 9 20789 1894 110566607
Left ventricular failure 20.36 16.05 17 20781 11372 110557129
Sudden death 20.31 16.05 24 20774 24371 110544130
Shrinking lung syndrome 20.07 16.05 5 20793 173 110568328
Genital rash 19.94 16.05 8 20790 1327 110567174
Mobility decreased 19.72 16.05 10 20788 237412 110331089
Left ventricular dilatation 19.46 16.05 8 20790 1414 110567087
Lordosis 19.36 16.05 6 20792 467 110568034
Conduction disorder 19.12 16.05 11 20787 4044 110564457
Visual impairment 18.93 16.05 62 20736 134366 110434135
Myoclonus 18.92 16.05 27 20771 32971 110535530
Blood luteinising hormone increased 18.90 16.05 5 20793 220 110568281
Atrioventricular block complete 18.81 16.05 21 20777 20061 110548440
Abdominal pain 18.80 16.05 43 20755 512946 110055555
Kyphosis 18.75 16.05 10 20788 3177 110565324
Concomitant disease aggravated 18.67 16.05 19 20779 16345 110552156
Tuberculosis of central nervous system 18.61 16.05 6 20792 531 110567970
Atrioventricular block second degree 18.46 16.05 14 20784 8167 110560334
Hyperparathyroidism secondary 18.41 16.05 10 20788 3294 110565207
Intentional product use issue 18.37 16.05 12 20786 247894 110320607
Atrioventricular block 18.18 16.05 19 20779 16858 110551643
Gastrointestinal tract adenoma 18.08 16.05 6 20792 581 110567920
Wheezing 18.05 16.05 13 20785 255217 110313284
Tachycardia 17.75 16.05 87 20711 226558 110341943
Varices oesophageal 17.74 16.05 13 20785 7202 110561299
Bronchospasm 17.71 16.05 25 20773 30214 110538287
Lupus myocarditis 17.50 16.05 4 20794 95 110568406
Serotonin syndrome 17.42 16.05 36 20762 59117 110509384
Arthritis 17.33 16.05 5 20793 167581 110400920
Postural orthostatic tachycardia syndrome 17.30 16.05 8 20790 1874 110566627
Anaemia folate deficiency 17.04 16.05 6 20792 695 110567806
Iron deficiency anaemia 16.89 16.05 25 20773 31534 110536967
Orthostatic hypotension 16.85 16.05 38 20760 66211 110502290
Blood chloride increased 16.85 16.05 12 20786 6360 110562141
Metabolic acidosis 16.83 16.05 49 20749 99695 110468806
Psoriatic arthropathy 16.77 16.05 8 20790 196753 110371748
Eye movement disorder 16.32 16.05 14 20784 9714 110558787
Completed suicide 16.30 16.05 13 20785 242368 110326133
Extrasystoles 16.10 16.05 13 20785 8305 110560196

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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:35526 hypoglycemic agent
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:38147 cardiotonic drug
CHEBI has role CHEBI:50514 vasoconstrictor agent
CHEBI has role CHEBI:149553 anticoronaviral agent
CHEBI has role CHEBI:176497 geroprotector

Related Drugs by ATC class:

C01EB Other cardiac preparations 15 drugs
acadesineacoramidisadenosinecamphorcreatinolfosfateibuprofenindomethacinmavacamtenmeldoniumphosphocreatineranolazineregadenoson show all 15 →
C07FX Beta blocking agents, other combinations 6 drugs
acetylsalicylic acidbisoprololcarvedilolmetoprololpropranololsotalol

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 8.45 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 5MG BASE CORLANOR AMGEN INC N206143 April 15, 2015 DISCN 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 DISCN 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 DISCN 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 DISCN 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 DISCN 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 DISCN 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 DISCN 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 DISCN 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 DISCN 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 DISCN 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 DISCN 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 DISCN 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
5MG/5ML (1MG/ML) CORLANOR AMGEN INC N209964 April 22, 2019 DISCN 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 DISCN SOLUTION ORAL Oct. 22, 2026 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 Ion channel BLOCKER IC50 5.70 IUPHAR DRUG LABEL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 Ion channel BLOCKER UNKNOWN DRUG LABEL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 3 Ion channel BLOCKER IC50 5.70 IUPHAR DRUG LABEL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 Ion channel EC50 5.37 CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 Ion channel EC50 5.35 CHEMBL
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 Ion channel EC50 5.34 CHEMBL

External reference:

IDSource
D07165 KEGG_DRUG
148849-67-6 SECONDARY_CAS_RN
4034416 VANDF
C0257190 UMLSCUI
CHEBI:85969 CHEBI
VNZ PDB_CHEM_ID
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
272983 MMSL
d05706 MMSL
011156 NDDF
011157 NDDF
420906000 SNOMEDCT_US
421228002 SNOMEDCT_US
421692002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 31722-053 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 31722-054 TABLET, FILM COATED 7.50 mg ORAL ANDA 27 sections
Ivabradine Human Prescription Drug Label 1 46708-679 TABLET, FILM COATED 5 mg ORAL ANDA 31 sections
Ivabradine Human Prescription Drug Label 1 46708-680 TABLET, FILM COATED 7.50 mg ORAL ANDA 31 sections
IVABRADINE HUMAN PRESCRIPTION DRUG LABEL 1 50742-362 TABLET, FILM COATED 5 mg ORAL ANDA 24 sections
IVABRADINE HUMAN PRESCRIPTION DRUG LABEL 1 50742-363 TABLET, FILM COATED 7.50 mg ORAL ANDA 24 sections
IVABRADINE HUMAN PRESCRIPTION DRUG LABEL 1 51407-592 TABLET, FILM COATED 5 mg ORAL ANDA 24 sections
IVABRADINE HUMAN PRESCRIPTION DRUG LABEL 1 51407-593 TABLET, FILM COATED 7.50 mg ORAL ANDA 24 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 55513-813 SOLUTION 5 mg ORAL NDA 31 sections
Corlanor HUMAN PRESCRIPTION DRUG LABEL 1 55513-813 SOLUTION 5 mg ORAL NDA 31 sections
Ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 60687-862 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Ivabradine Human Prescription Drug Label 1 62332-679 TABLET, FILM COATED 5 mg ORAL ANDA 31 sections
Ivabradine Human Prescription Drug Label 1 62332-680 TABLET, FILM COATED 7.50 mg ORAL ANDA 31 sections
ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 69452-190 TABLET, FILM COATED 5 mg ORAL ANDA 28 sections
ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 69452-191 TABLET, FILM COATED 7.50 mg ORAL ANDA 28 sections
ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 70710-1471 TABLET 5 mg ORAL ANDA 26 sections
ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 70710-1472 TABLET 7.50 mg ORAL ANDA 26 sections
ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 70771-1863 TABLET 5 mg ORAL ANDA 2 sections
ivabradine HUMAN PRESCRIPTION DRUG LABEL 1 70771-1864 TABLET 7.50 mg ORAL ANDA 2 sections
Ivabradine Human Prescription Drug Label 1 72205-336 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Ivabradine Human Prescription Drug Label 1 72205-337 TABLET, FILM COATED 7.50 mg ORAL ANDA 27 sections
Ivabradine Human Prescription Drug Label 1 72603-934 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Ivabradine Human Prescription Drug Label 1 72603-935 TABLET, FILM COATED 7.50 mg ORAL ANDA 27 sections