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

Stem definitionDrug idCAS RN
endothelin receptor antagonists 392 147536-97-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bosentan hydrate
  • bosentan monohydrate
  • stayveer
  • bosentan
  • actelion
  • tracleer
  • bosentan anhydrous
a specific and competitive antagonist at endothelin receptor types ETA and ETB, has a slightly higher affinity for ETA receptors than for ETB receptors, indicated for the treatment of pulmonary arterial hypertension
  • Molecular weight: 551.62
  • Formula: C27H29N5O6S
  • CLOGP: 4.17
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 2
  • TPSA: 145.65
  • ALOGS: -4.79
  • ROTB: 10

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.25 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 6.47 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 50 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.29 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.04 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 20, 2001 FDA ACTELION PHARMS LTD

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
Pulmonary arterial hypertension 2512.08 13.40 1136 85386 24792 46574748
Death 2061.22 13.40 2799 83723 332749 46266791
Dyspnoea 1502.41 13.40 3076 83446 512472 46087068
Right ventricular failure 1271.91 13.40 613 85909 15480 46584060
Pulmonary hypertension 1035.87 13.40 709 85813 35284 46564256
Aspartate aminotransferase increased 814.74 13.40 860 85662 77840 46521700
Fluid retention 811.80 13.40 707 85815 50339 46549201
Alanine aminotransferase increased 723.90 13.40 855 85667 87596 46511944
Drug ineffective 623.33 13.40 241 86281 677597 45921943
Transfusion 600.26 13.40 348 86174 12883 46586657
Blood alkaline phosphatase increased 551.15 13.40 509 86013 39100 46560440
Liver function test abnormal 522.00 13.40 531 85991 45956 46553584
Lung transplant 375.36 13.40 156 86366 2736 46596804
Cardiac failure 373.17 13.40 589 85933 79359 46520181
Pneumonia 342.98 13.40 1491 85031 374829 46224711
Syncope 328.17 13.40 648 85874 104155 46495385
Dyspnoea exertional 315.23 13.40 426 86096 49863 46549677
Rheumatoid arthritis 309.75 13.40 40 86482 240175 46359365
Fluid overload 302.21 13.40 309 86213 26876 46572664
Device related infection 299.53 13.40 274 86248 20767 46578773
Disease progression 293.64 13.40 571 85951 90729 46508811
Hospitalisation 287.44 13.40 461 86061 62924 46536616
Pulmonary oedema 283.14 13.40 408 86114 50697 46548843
Scleroderma 279.34 13.40 147 86375 4482 46595058
Cardiac operation 277.42 13.40 123 86399 2543 46596997
Blood bilirubin increased 276.74 13.40 329 86193 33855 46565685
Oedema 272.14 13.40 464 86058 66607 46532933
Cardiac pacemaker insertion 271.31 13.40 134 86388 3565 46595975
Drug hypersensitivity 263.66 13.40 64 86458 243761 46355779
Completed suicide 241.99 13.40 6 86516 145914 46453626
Oxygen saturation decreased 241.38 13.40 448 86074 68716 46530824
Cardiac failure congestive 237.64 13.40 525 85997 91225 46508315
Condition aggravated 234.17 13.40 986 85536 244066 46355474
Toxicity to various agents 224.21 13.40 58 86464 211708 46387832
Catheterisation cardiac 223.06 13.40 121 86401 3926 46595614
Rash 220.56 13.40 202 86320 356310 46243230
Oedema peripheral 201.22 13.40 702 85820 159004 46440536
Concomitant disease aggravated 200.22 13.40 144 86378 7738 46591802
Neutropenia 196.65 13.40 19 86503 143185 46456355
Off label use 192.21 13.40 254 86268 379587 46219953
Hypoxia 191.22 13.40 344 86178 51494 46548046
Pulmonary arterial pressure increased 190.28 13.40 102 86420 3230 46596310
Alopecia 188.96 13.40 36 86486 162378 46437162
Product dose omission issue 186.33 13.40 710 85812 167810 46431730
Respiratory failure 181.64 13.40 483 86039 94333 46505207
Dialysis 180.78 13.40 150 86372 9966 46589574
Pain in jaw 175.11 13.40 280 86242 38092 46561448
Infusion related reaction 168.37 13.40 4 86518 101204 46498336
Catheter site pain 156.54 13.40 94 86428 3712 46595828
Febrile neutropenia 156.42 13.40 4 86518 94623 46504917
Cardiac disorder 150.32 13.40 282 86240 43576 46555964
Catheter site erythema 147.52 13.40 92 86430 3891 46595649
Treatment failure 146.52 13.40 6 86516 93081 46506459
Catheter site infection 144.56 13.40 97 86425 4656 46594884
Disease complication 143.63 13.40 82 86440 2943 46596597
Arthralgia 142.98 13.40 288 86234 364315 46235225
Chest pain 139.97 13.40 672 85850 175652 46423888
Pain 137.42 13.40 441 86081 476507 46123033
Maternal exposure during pregnancy 134.63 13.40 16 86506 102533 46497007
Gamma-glutamyltransferase increased 130.50 13.40 221 86301 31519 46568021
Mechanical ventilation 126.69 13.40 57 86465 1221 46598319
Cardioversion 122.60 13.40 54 86468 1098 46598442
Depression 121.80 13.40 83 86439 170021 46429519
Therapeutic product effect decreased 121.59 13.40 8 86514 82593 46516947
Psoriasis 120.65 13.40 6 86516 78598 46520942
Musculoskeletal stiffness 119.87 13.40 19 86503 97974 46501566
Pulmonary hypertensive crisis 116.85 13.40 33 86489 159 46599381
Drug intolerance 114.61 13.40 65 86457 146984 46452556
Catheter management 112.28 13.40 68 86454 2727 46596813
Cardiac ablation 111.75 13.40 52 86470 1207 46598333
Chronic obstructive pulmonary disease 111.71 13.40 295 86227 57338 46542202
Cough 108.37 13.40 764 85758 229485 46370055
Joint swelling 107.39 13.40 90 86432 165983 46433557
Tracheostomy 105.68 13.40 40 86482 541 46598999
Pericardial effusion 105.19 13.40 178 86344 25365 46574175
Drug interaction 101.26 13.40 137 86385 202957 46396583
Urticaria 100.99 13.40 46 86476 117846 46481694
Haemoptysis 100.64 13.40 177 86345 26012 46573528
Stent placement 99.66 13.40 69 86453 3487 46596053
Malignant neoplasm progression 96.41 13.40 6 86516 64920 46534620
Nasal congestion 95.00 13.40 248 86274 47865 46551675
Exercise tolerance decreased 94.80 13.40 74 86448 4503 46595037
Pruritus 93.51 13.40 193 86329 242159 46357381
Injection site pain 93.04 13.40 41 86481 107111 46492429
Pregnancy 92.35 13.40 174 86348 26963 46572577
Atrial fibrillation 91.83 13.40 408 86114 103182 46496358
Congestive hepatopathy 91.60 13.40 57 86465 2401 46597139
Finger amputation 91.25 13.40 35 86487 492 46599048
Drug abuse 90.84 13.40 7 86515 63401 46536139
Oxygen consumption increased 88.65 13.40 65 86457 3598 46595942
Device leakage 88.54 13.40 76 86446 5289 46594251
Therapeutic product effect incomplete 87.34 13.40 19 86503 78134 46521406
Biopsy liver 87.26 13.40 32 86490 394 46599146
Catheter site discharge 87.10 13.40 51 86471 1921 46597619
Overdose 87.01 13.40 40 86482 101939 46497601
Flushing 85.54 13.40 289 86233 64325 46535215
Acute kidney injury 84.24 13.40 196 86326 235659 46363881
Catheter placement 82.58 13.40 49 86473 1892 46597648
Cyanosis 81.86 13.40 123 86399 15848 46583692
Paraesthesia 81.78 13.40 59 86463 117378 46482162
Intentional overdose 80.76 13.40 12 86510 64932 46534608
Cor pulmonale 79.93 13.40 48 86474 1895 46597645
Injection site erythema 79.39 13.40 20 86502 74407 46525133
Atrial flutter 77.22 13.40 90 86432 9058 46590482
Pulmonary veno-occlusive disease 75.47 13.40 36 86486 885 46598655
Systemic scleroderma 74.49 13.40 35 86487 831 46598709
Hernia repair 73.99 13.40 38 86484 1100 46598440
Fall 73.70 13.40 932 85590 328165 46271375
White blood cell count decreased 73.53 13.40 60 86462 112171 46487369
Lung disorder 73.32 13.40 211 86311 43093 46556447
Hypersensitivity 73.28 13.40 103 86419 150218 46449322
Packed red blood cell transfusion 72.72 13.40 47 86475 2116 46597424
Atrial septal defect repair 72.46 13.40 24 86498 213 46599327
Catheter site swelling 71.42 13.40 39 86483 1282 46598258
Suicidal ideation 71.08 13.40 10 86512 56372 46543168
Influenza 70.53 13.40 340 86182 88930 46510610
Heart transplant 68.20 13.40 27 86495 415 46599125
Leukopenia 67.99 13.40 21 86501 68322 46531218
Hyponatraemia 67.85 13.40 53 86469 101279 46498261
Endotracheal intubation 67.80 13.40 45 86477 2120 46597420
Electrocardiogram QT prolonged 67.36 13.40 8 86514 51317 46548223
Product use in unapproved indication 67.34 13.40 42 86480 90231 46509309
Arthropathy 66.59 13.40 37 86485 84663 46514877
Hip fracture 66.44 13.40 150 86372 26406 46573134
Patent ductus arteriosus repair 65.45 13.40 14 86508 12 46599528
Concomitant disease progression 65.45 13.40 44 86478 2118 46597422
Injection site reaction 63.94 13.40 7 86515 47842 46551698
Infusion site pain 63.84 13.40 86 86436 10021 46589519
Anaphylactic reaction 63.37 13.40 11 86511 53101 46546439
Hypertension 63.22 13.40 172 86350 196184 46403356
Neuropathy peripheral 62.83 13.40 46 86476 90847 46508693
Neutrophil count decreased 61.62 13.40 5 86517 43421 46556119
Transplant evaluation 61.61 13.40 33 86489 1043 46598497
Heart valve replacement 61.52 13.40 26 86496 476 46599064
Dizziness 61.14 13.40 927 85595 339487 46260053
Stomatitis 61.08 13.40 25 86497 68272 46531268
Plasma cell myeloma 60.74 13.40 6 86516 44472 46555068
Ascites 60.72 13.40 177 86345 36407 46563133
Suicide attempt 60.24 13.40 14 86508 55022 46544518
Somnolence 60.01 13.40 125 86397 156396 46443144
Mucosal inflammation 59.72 13.40 3 86519 38973 46560567
Hypoaesthesia 59.38 13.40 80 86442 118789 46480751
Confusional state 59.38 13.40 130 86392 159762 46439778
Brain natriuretic peptide increased 59.32 13.40 57 86465 4593 46594947
Wrong technique in product usage process 59.26 13.40 14 86508 54408 46545132
Central venous catheterisation 58.33 13.40 40 86482 1990 46597550
Cardiac pacemaker replacement 58.23 13.40 22 86500 296 46599244
Presyncope 57.72 13.40 135 86387 24319 46575221
Epistaxis 55.98 13.40 252 86270 64053 46535487
Gastrointestinal haemorrhage 54.97 13.40 286 86236 77087 46522453
Blood pressure increased 54.83 13.40 94 86428 126572 46472968
Catheter site pruritus 54.52 13.40 38 86484 1941 46597599
Catheter site haemorrhage 54.38 13.40 43 86479 2666 46596874
Deep vein thrombosis 54.32 13.40 41 86481 79732 46519808
Walking distance test abnormal 54.22 13.40 24 86498 494 46599046
Product quality issue 53.81 13.40 3 86519 35645 46563895
Osteoarthritis 53.40 13.40 24 86498 62001 46537539
Blood cholesterol increased 53.10 13.40 6 86516 40007 46559533
Infusion site erythema 51.30 13.40 67 86455 7575 46591965
Catheter site inflammation 50.95 13.40 25 86497 655 46598885
Palpitations 50.62 13.40 326 86196 94933 46504607
Acute respiratory failure 50.31 13.40 143 86379 28995 46570545
Terminal state 50.09 13.40 38 86484 2216 46597324
Systemic-pulmonary artery shunt 50.05 13.40 12 86510 25 46599515
Mobility decreased 49.78 13.40 25 86497 60569 46538971
Chemotherapy 49.49 13.40 31 86491 1321 46598219
Malaise 49.41 13.40 875 85647 330357 46269183
Rhabdomyolysis 49.30 13.40 9 86513 41900 46557640
Viral infection 48.94 13.40 145 86377 30090 46569450
Device alarm issue 48.70 13.40 31 86491 1359 46598181
Thrombocytopenia 48.58 13.40 101 86421 126480 46473060
Balloon atrial septostomy 48.34 13.40 14 86508 75 46599465
Intentional product misuse 47.74 13.40 14 86508 47114 46552426
Device occlusion 47.71 13.40 57 86465 5888 46593652
Tracheostomy malfunction 47.45 13.40 12 86510 34 46599506
Angioedema 47.26 13.40 8 86514 39334 46560206
Chronic respiratory failure 46.91 13.40 33 86489 1711 46597829
Right-to-left cardiac shunt 46.61 13.40 16 86506 160 46599380
Sudden death 45.61 13.40 71 86451 9433 46590107
Cognitive disorder 45.42 13.40 7 86515 36876 46562664
Gout 45.25 13.40 78 86444 11278 46588262
Hip surgery 45.04 13.40 37 86485 2423 46597117
Heart and lung transplant 44.80 13.40 14 86508 101 46599439
Oxygen saturation abnormal 43.83 13.40 38 86484 2680 46596860
Injection site pruritus 43.71 13.40 10 86512 39733 46559807
Glossodynia 43.48 13.40 14 86508 44359 46555181
Rhinovirus infection 43.44 13.40 43 86479 3593 46595947
Transplant 42.89 13.40 22 86500 635 46598905
Implantable defibrillator insertion 42.66 13.40 19 86503 397 46599143
Pulmonary haemorrhage 42.07 13.40 56 86466 6449 46593091
Muscle spasms 40.99 13.40 106 86416 123007 46476533
Pancytopenia 40.71 13.40 59 86463 84999 46514541
Anxiety 40.68 13.40 186 86336 181771 46417769
Hypotension 40.36 13.40 630 85892 231959 46367581
Infusion site infection 40.16 13.40 28 86494 1431 46598109
Leg amputation 39.82 13.40 32 86490 2031 46597509
Swollen tongue 39.77 13.40 4 86518 29228 46570312
Pulmonary resection 39.63 13.40 10 86512 28 46599512
Mastectomy 39.61 13.40 28 86494 1463 46598077
Device related sepsis 39.51 13.40 39 86483 3248 46596292
Constipation 39.50 13.40 177 86345 173920 46425620
Hypokalaemia 39.31 13.40 64 86458 87960 46511580
Right ventricular dysfunction 39.16 13.40 28 86494 1490 46598050
Limb operation 39.00 13.40 39 86483 3299 46596241
Angioplasty 38.87 13.40 26 86496 1241 46598299
Oxygen therapy 38.40 13.40 30 86492 1827 46597713
Respiratory distress 38.10 13.40 138 86384 31778 46567762
Bone marrow failure 38.01 13.40 5 86517 29664 46569876
Colon operation 37.71 13.40 16 86506 296 46599244
Inappropriate schedule of product administration 37.53 13.40 39 86483 64974 46534566
Complication associated with device 37.27 13.40 86 86436 15355 46584185
Skin ulcer 36.78 13.40 138 86384 32320 46567220
Renal disorder 36.75 13.40 121 86401 26565 46572975
Scleroderma renal crisis 36.45 13.40 15 86507 256 46599284
Bilirubin conjugated increased 36.18 13.40 34 86488 2664 46596876
Heart rate increased 36.13 13.40 250 86272 74541 46524999
Agitation 35.81 13.40 30 86492 55385 46544155
Mouth ulceration 35.66 13.40 4 86518 26828 46572712
Hypoglycaemia 35.65 13.40 29 86493 54320 46545220
Intentional product use issue 34.82 13.40 28 86494 52752 46546788
Cholecystectomy 34.58 13.40 61 86461 8981 46590559
Coronary arterial stent insertion 34.57 13.40 34 86488 2819 46596721
Gastrointestinal tube insertion 34.34 13.40 23 86499 1100 46598440
Abortion induced 33.92 13.40 65 86457 10195 46589345
Mineral supplementation 33.60 13.40 18 86504 569 46598971
Aortic valve replacement 33.20 13.40 19 86503 685 46598855
Hypocalcaemia 33.18 13.40 5 86517 26780 46572760
Haemorrhage 33.05 13.40 194 86328 54675 46544865
Injection site swelling 32.58 13.40 17 86505 40310 46559230
Cardiopulmonary failure 32.49 13.40 37 86485 3632 46595908
Cardiomegaly 32.35 13.40 88 86434 17394 46582146
Multiple sclerosis 32.19 13.40 4 86518 24787 46574753
Blood pressure systolic increased 32.15 13.40 7 86515 28780 46570760
Ventricular assist device insertion 32.08 13.40 8 86514 21 46599519
Pulmonary vein stenosis 32.02 13.40 10 86512 72 46599468
Hospice care 31.84 13.40 44 86478 5251 46594289
Biopsy kidney 31.78 13.40 11 86511 113 46599427
Right ventricular systolic pressure increased 31.75 13.40 17 86505 537 46599003
Generalised tonic-clonic seizure 31.52 13.40 6 86516 27116 46572424
Ventricular septal defect repair 31.28 13.40 7 86515 9 46599531
Pulmonary arterial pressure abnormal 31.25 13.40 16 86506 460 46599080
Therapy non-responder 31.23 13.40 155 86367 40997 46558543
Lymphocyte count decreased 31.19 13.40 5 86517 25584 46573956
Loss of personal independence in daily activities 31.14 13.40 36 86486 57147 46542393
Therapeutic response decreased 30.90 13.40 21 86501 43124 46556416
Radiotherapy 30.90 13.40 14 86508 305 46599235
Head injury 30.66 13.40 108 86414 24528 46575012
Coma 30.42 13.40 38 86484 58311 46541229
Liver function test increased 30.10 13.40 102 86420 22724 46576816
Fibromyalgia 30.01 13.40 15 86507 36448 46563092
Pulmonary congestion 29.93 13.40 77 86445 14722 46584818
Hepatic cirrhosis 29.92 13.40 80 86442 15652 46583888
Drug withdrawal syndrome 29.89 13.40 7 86515 27377 46572163
Dyspnoea at rest 29.78 13.40 35 86487 3553 46595987
Catheter removal 29.73 13.40 14 86508 334 46599206
Lower respiratory tract infection 29.65 13.40 35 86487 55054 46544486
Emotional distress 29.53 13.40 10 86512 30697 46568843
Injury 29.49 13.40 23 86499 44004 46555536
Tricuspid valve repair 29.33 13.40 6 86516 3 46599537
Heart valve operation 29.18 13.40 11 86511 147 46599393
Sedation 29.02 13.40 4 86518 22906 46576634
Upper limb fracture 28.98 13.40 79 86443 15634 46583906
Autoimmune hepatitis 28.97 13.40 52 86470 7762 46591778
Lung assist device therapy 28.79 13.40 9 86513 65 46599475
Pulmonary valve replacement 28.70 13.40 6 86516 4 46599536
Cardiac output decreased 28.66 13.40 19 86503 893 46598647
Psychotic disorder 28.53 13.40 4 86518 22617 46576923
Sleep study 28.46 13.40 7 86515 17 46599523
Mitral valve replacement 28.43 13.40 12 86510 219 46599321
Gait disturbance 28.17 13.40 156 86366 145107 46454433
Toe amputation 28.09 13.40 26 86496 1998 46597542
Depressed level of consciousness 28.07 13.40 28 86494 47541 46551999
Paracentesis 28.05 13.40 19 86503 926 46598614
Infusion site discharge 28.00 13.40 16 86506 575 46598965
Lactic acidosis 27.83 13.40 14 86508 33895 46565645
Drug reaction with eosinophilia and systemic symptoms 27.77 13.40 10 86512 29538 46570002
Echocardiogram abnormal 27.55 13.40 19 86503 954 46598586
Gastritis hypertrophic 27.45 13.40 8 86514 44 46599496
Bone pain 27.21 13.40 28 86494 46862 46552678
Knee arthroplasty 27.13 13.40 101 86421 23564 46575976
Headache 27.04 13.40 1113 85409 477239 46122301
Sepsis 26.92 13.40 377 86145 135637 46463903
Localised infection 26.80 13.40 101 86421 23700 46575840
Tremor 26.55 13.40 117 86405 115522 46484018
Carbon dioxide increased 26.55 13.40 20 86502 1154 46598386
Aggression 26.50 13.40 5 86517 22739 46576801
Left ventricular failure 26.38 13.40 39 86483 4951 46594589
Adverse drug reaction 26.30 13.40 26 86496 44336 46555204
Knee operation 26.28 13.40 38 86484 4728 46594812
Erythema 26.28 13.40 156 86366 142664 46456876
Skin operation 26.28 13.40 6 86516 9 46599531
Aortic valve repair 26.28 13.40 6 86516 9 46599531
Bursitis 26.26 13.40 3 86519 19839 46579701
Muscular weakness 26.23 13.40 85 86437 91759 46507781
Catheter site related reaction 26.03 13.40 17 86505 779 46598761
Disturbance in attention 25.95 13.40 13 86509 31547 46567993
Dysarthria 25.87 13.40 19 86503 37479 46562061
Gastrostomy 25.73 13.40 15 86507 560 46598980
Device infusion issue 25.47 13.40 19 86503 1080 46598460
Rash maculo-papular 25.25 13.40 10 86512 27864 46571676
Skin exfoliation 25.00 13.40 15 86507 32923 46566617
Platelet transfusion 24.90 13.40 16 86506 713 46598827
Pleural effusion 24.86 13.40 249 86273 82703 46516837
Haemodynamic test abnormal 24.74 13.40 7 86515 34 46599506
Infusion site irritation 24.71 13.40 14 86508 495 46599045
Endarterectomy 24.61 13.40 10 86512 165 46599375
Nocturnal dyspnoea 24.60 13.40 18 86504 993 46598547
Lower limb fracture 24.55 13.40 64 86458 12334 46587206
Gallbladder operation 24.51 13.40 23 86499 1799 46597741
Endothelial dysfunction 24.24 13.40 9 86513 115 46599425
Rehabilitation therapy 24.10 13.40 19 86503 1173 46598367
Pulmonary artery aneurysm 24.09 13.40 7 86515 38 46599502
Tracheostomy infection 23.99 13.40 6 86516 16 46599524
Type 2 diabetes mellitus 23.96 13.40 4 86518 19871 46579669
Dysphagia 23.89 13.40 69 86453 77243 46522297
Sopor 23.88 13.40 4 86518 19824 46579716
Osteoporosis 23.84 13.40 24 86498 40584 46558956
Abnormal behaviour 23.76 13.40 5 86517 21053 46578487
Renal failure 23.75 13.40 318 86204 113276 46486264
Mitral valve repair 23.67 13.40 10 86512 183 46599357
Full blood count decreased 23.62 13.40 6 86516 22205 46577335
Right ventricular hypertrophy 23.51 13.40 15 86507 660 46598880
Cancer surgery 23.41 13.40 13 86509 442 46599098
Chest tube insertion 23.37 13.40 7 86515 43 46599497
Atrial tachycardia 23.36 13.40 24 86498 2096 46597444
Blister 23.34 13.40 29 86493 44602 46554938
Lip swelling 23.18 13.40 9 86513 25386 46574154
Insomnia 23.08 13.40 195 86327 164729 46434811
Respiratory syncytial virus infection 23.03 13.40 36 86486 4799 46594741
Delirium 23.03 13.40 21 86501 37207 46562333
Productive cough 23.01 13.40 167 86355 50548 46548992
Pulmonary artery therapeutic procedure 23.00 13.40 6 86516 20 46599520
Ulcer haemorrhage 22.72 13.40 30 86492 3428 46596112
Vascular operation 22.63 13.40 8 86514 88 46599452
Cellulitis 22.54 13.40 214 86308 70074 46529466
Pulmonary artery banding 22.53 13.40 5 86517 6 46599534
CREST syndrome 22.47 13.40 12 86510 377 46599163
Gangrene 22.42 13.40 35 86487 4660 46594880
Infected skin ulcer 22.40 13.40 24 86498 2201 46597339
C-reactive protein increased 22.25 13.40 47 86475 58543 46540997
Drug eruption 22.22 13.40 6 86516 21323 46578217
Cataract 22.22 13.40 31 86491 45384 46554156
Abortion spontaneous 22.16 13.40 29 86493 43617 46555923
Biopsy bone marrow 22.02 13.40 11 86511 300 46599240
Encephalopathy 21.93 13.40 18 86504 33571 46565969
Amputation 21.85 13.40 9 86513 154 46599386
Hypercalcaemia 21.78 13.40 6 86516 21040 46578500
Protein-losing gastroenteropathy 21.75 13.40 9 86513 156 46599384
Stevens-Johnson syndrome 21.70 13.40 8 86514 23289 46576251
Blood iron decreased 21.68 13.40 57 86465 11040 46588500
Hallucination 21.66 13.40 37 86485 49914 46549626
Drug level increased 21.60 13.40 4 86518 18437 46581103
Infusion site cellulitis 21.59 13.40 9 86513 159 46599381
Dysgeusia 21.50 13.40 26 86496 40465 46559075
Colonoscopy 21.46 13.40 18 86504 1213 46598327
Generalised oedema 21.37 13.40 67 86455 14332 46585208
Hyperhidrosis 21.33 13.40 89 86433 89219 46510321
Diabetic ketoacidosis 21.22 13.40 4 86518 18206 46581334
Withdrawal syndrome 21.10 13.40 4 86518 18130 46581410
Systemic sclerosis pulmonary 20.99 13.40 5 86517 10 46599530
Internal haemorrhage 20.98 13.40 33 86489 4422 46595118
Aspiration pleural cavity 20.85 13.40 15 86507 806 46598734
Seizure 20.78 13.40 138 86384 122916 46476624
Pulmonary fibrosis 20.78 13.40 83 86439 20009 46579531
Discomfort 20.76 13.40 34 86488 46636 46552904
Hallucination, visual 20.67 13.40 4 86518 17869 46581671
Aspartate aminotransferase 20.67 13.40 7 86515 67 46599473
Cholelithotomy 20.44 13.40 6 86516 34 46599506
Therapy change 20.33 13.40 35 86487 5055 46594485
Urinary incontinence 20.28 13.40 14 86508 28516 46571024
Exercise test abnormal 20.26 13.40 8 86514 122 46599418
Hepatomegaly 20.18 13.40 56 86466 11197 46588343
Cataract operation 20.17 13.40 31 86491 4072 46595468
Infusion site abscess 20.04 13.40 9 86513 192 46599348
Agranulocytosis 20.03 13.40 8 86514 22177 46577363
N-terminal prohormone brain natriuretic peptide increased 20.01 13.40 20 86502 1691 46597849
Aortic stenosis 20.01 13.40 32 86490 4350 46595190
Herpes zoster 19.95 13.40 62 86460 67810 46531730
Product supply issue 19.95 13.40 15 86507 863 46598677
Pulmonary thrombosis 19.85 13.40 43 86479 7359 46592181
Thrombosis in device 19.81 13.40 26 86496 2953 46596587
Pulmonary vascular resistance abnormality 19.74 13.40 6 86516 39 46599501
Hyperlipidaemia 19.73 13.40 5 86517 18534 46581006
Human metapneumovirus test positive 19.61 13.40 6 86516 40 46599500
Cyst removal 19.57 13.40 11 86511 383 46599157
Carpal tunnel syndrome 19.55 13.40 3 86519 15856 46583684
Tracheitis 19.53 13.40 14 86508 748 46598792
Exposure during pregnancy 19.48 13.40 119 86403 108093 46491447
Red blood cell sedimentation rate increased 19.47 13.40 9 86513 22880 46576660
Ear tube insertion 19.40 13.40 7 86515 82 46599458
Rash erythematous 19.38 13.40 21 86501 34329 46565211
Catheter site warmth 19.34 13.40 9 86513 209 46599331
Vascular device infection 19.34 13.40 28 86494 3489 46596051
Therapeutic embolisation 19.31 13.40 8 86514 139 46599401
Oral pain 19.24 13.40 11 86511 24786 46574754
Hyperglycaemia 19.18 13.40 22 86500 35049 46564491
Foot amputation 19.14 13.40 10 86512 300 46599240
Polycythaemia 19.14 13.40 14 86508 772 46598768
Treatment noncompliance 19.13 13.40 107 86415 29624 46569916
Dry skin 19.08 13.40 29 86493 40987 46558553
Blood pressure fluctuation 19.04 13.40 17 86505 30431 46569109
Arterial aneurysm repair 18.94 13.40 4 86518 3 46599537
Resuscitation 18.77 13.40 16 86506 1103 46598437
Bilevel positive airway pressure 18.66 13.40 5 86517 19 46599521
Alanine aminotransferase 18.55 13.40 6 86516 49 46599491
Pulmonary pain 18.52 13.40 19 86503 1657 46597883
Bradycardia 18.48 13.40 62 86460 66236 46533304
Colitis ulcerative 18.45 13.40 5 86517 17727 46581813
Cavopulmonary anastomosis 18.41 13.40 4 86518 4 46599536
Cardiac septal defect repair 18.41 13.40 4 86518 4 46599536
Tracheostomy tube removal 18.41 13.40 4 86518 4 46599536
Hepatic function abnormal 18.39 13.40 118 86404 34303 46565237
Shoulder operation 18.37 13.40 20 86502 1868 46597672
Joint range of motion decreased 18.33 13.40 3 86519 15121 46584419
Irritability 18.30 13.40 16 86506 28930 46570610
Emergency care 18.28 13.40 14 86508 828 46598712
Dyskinesia 18.27 13.40 16 86506 28909 46570631
Drug dependence 18.25 13.40 7 86515 19894 46579646
Urinary retention 18.24 13.40 13 86509 26048 46573492
Injection site mass 18.19 13.40 3 86519 15037 46584503
Abdominal distension 18.18 13.40 212 86310 73139 46526401
Impaired healing 18.06 13.40 25 86497 36718 46562822
Metastases to bone 18.05 13.40 5 86517 17471 46582069
Rash pruritic 18.05 13.40 34 86488 44181 46555359
Cardiac arrest 18.05 13.40 251 86271 90148 46509392
Blood viscosity abnormal 17.94 13.40 4 86518 5 46599535
Skin lesion 17.83 13.40 14 86508 26699 46572841
Heart rate irregular 17.80 13.40 75 86447 18516 46581024
Disease recurrence 17.79 13.40 6 86516 18465 46581075
Dry eye 17.71 13.40 18 86504 30304 46569236
Orthostatic hypotension 17.66 13.40 12 86510 24646 46574894
Scleroderma associated digital ulcer 17.52 13.40 4 86518 6 46599534
Infusion site swelling 17.50 13.40 35 86487 5664 46593876
Catheter site rash 17.39 13.40 13 86509 741 46598799
Ischaemic skin ulcer 17.39 13.40 5 86517 26 46599514
Medication error 17.33 13.40 19 86503 30892 46568648
Acute myeloid leukaemia 17.29 13.40 4 86518 15774 46583766
Hysterectomy 17.24 13.40 42 86480 7764 46591776
Cerebral infarction 17.24 13.40 11 86511 23355 46576185
Supraventricular tachycardia 17.23 13.40 59 86463 13211 46586329
Dysentery 17.23 13.40 13 86509 752 46598788
Altered state of consciousness 17.21 13.40 11 86511 23337 46576203
Administration site infection 17.14 13.40 4 86518 7 46599533
Blood potassium decreased 17.07 13.40 125 86397 37938 46561602
Living in residential institution 17.02 13.40 10 86512 379 46599161
Hypomagnesaemia 17.02 13.40 10 86512 22200 46577340
Cor pulmonale chronic 16.95 13.40 8 86514 192 46599348
Ischaemic stroke 16.87 13.40 5 86517 16717 46582823
Bone disorder 16.85 13.40 8 86514 20025 46579515
Low cardiac output syndrome 16.76 13.40 9 86513 286 46599254
Acne 16.69 13.40 8 86514 19911 46579629
Palliative care 16.67 13.40 9 86513 289 46599251
Aneurysm repair 16.65 13.40 5 86517 31 46599509
Hyperkalaemia 16.60 13.40 44 86478 50665 46548875
Laboratory test abnormal 16.52 13.40 11 86511 22836 46576704
Abdominal discomfort 16.42 13.40 190 86332 150975 46448565
Pneumothorax 16.40 13.40 62 86460 14567 46584973
Device connection issue 16.35 13.40 12 86510 665 46598875
Immunoglobulin G4 related disease 16.35 13.40 6 86516 74 46599466
Disorientation 16.32 13.40 27 86495 36891 46562649
Cardiac failure acute 16.30 13.40 42 86480 8036 46591504
Pulmonary artery dilatation 16.29 13.40 8 86514 210 46599330
Eye operation 16.25 13.40 18 86504 1714 46597826
Mood swings 16.14 13.40 5 86517 16247 46583293
Amnesia 16.14 13.40 33 86489 41598 46557942
Dialysis related complication 16.14 13.40 6 86516 77 46599463
Staphylococcus test positive 16.13 13.40 26 86496 3558 46595982
Sinus bradycardia 16.12 13.40 3 86519 13779 46585761
Injection site warmth 16.10 13.40 3 86519 13769 46585771
Basal cell carcinoma 16.02 13.40 9 86513 20478 46579062
Congenital coronary artery malformation 16.01 13.40 5 86517 36 46599504
Sterilisation 15.88 13.40 3 86519 0 46599540
Electrocardiogram ambulatory 15.88 13.40 3 86519 0 46599540
Phlebotomy 15.88 13.40 3 86519 0 46599540
Cardiac pacemaker evaluation 15.88 13.40 3 86519 0 46599540
Blood glucose increased 15.84 13.40 74 86448 71939 46527601
Catheterisation cardiac abnormal 15.63 13.40 8 86514 230 46599310
Orthopnoea 15.59 13.40 34 86488 5846 46593694
Thromboembolectomy 15.55 13.40 5 86517 40 46599500
Dizziness exertional 15.51 13.40 9 86513 333 46599207
Body temperature decreased 15.51 13.40 3 86519 13406 46586134
Pericardial drainage 15.50 13.40 8 86514 234 46599306
Injection site rash 15.47 13.40 5 86517 15808 46583732
Blood culture positive 15.43 13.40 29 86493 4483 46595057
Chest discomfort 15.42 13.40 244 86278 90025 46509515
Pancreatitis acute 15.42 13.40 14 86508 24858 46574682
Pericardiotomy 15.41 13.40 4 86518 13 46599527
Pericarditis 15.40 13.40 13 86509 23914 46575626
Polypectomy 15.36 13.40 11 86511 587 46598953
Skin neoplasm excision 15.32 13.40 11 86511 589 46598951
Gastric operation 15.25 13.40 9 86513 344 46599196
Staphylococcal infection 15.21 13.40 116 86406 35655 46563885
Medical device change 15.20 13.40 9 86513 346 46599194
Therapeutic response unexpected 15.17 13.40 5 86517 15611 46583929
Restlessness 15.08 13.40 15 86507 25509 46574031
Musculoskeletal disorder 15.06 13.40 5 86517 15540 46584000
Mixed connective tissue disease 15.02 13.40 9 86513 354 46599186
Colitis 15.00 13.40 29 86493 37318 46562222
Visual impairment 14.98 13.40 68 86454 66621 46532919
Burning sensation 14.95 13.40 38 86484 44373 46555167
International normalised ratio abnormal 14.88 13.40 23 86499 3036 46596504
Dry mouth 14.88 13.40 52 86470 54874 46544666
Liver disorder 14.85 13.40 119 86403 37127 46562413
Arteriovenous fistula operation 14.84 13.40 8 86514 256 46599284
Metapneumovirus infection 14.82 13.40 12 86510 770 46598770
Respiratory tract haemorrhage 14.77 13.40 9 86513 365 46599175
Biopsy lung 14.75 13.40 7 86515 170 46599370
Breast conserving surgery 14.70 13.40 12 86510 779 46598761
Lymphopenia 14.67 13.40 5 86517 15288 46584252
Hepatic cancer 14.67 13.40 23 86499 3074 46596466
International normalised ratio increased 14.66 13.40 142 86380 46741 46552799
Brain tumour operation 14.57 13.40 4 86518 17 46599523
Plasmapheresis 14.51 13.40 8 86514 268 46599272
Unevaluable event 14.51 13.40 140 86382 46035 46553505
Acute right ventricular failure 14.49 13.40 7 86515 177 46599363
Oral herpes 14.48 13.40 9 86513 19381 46580159
Teething 14.39 13.40 4 86518 18 46599522
Fracture treatment 14.34 13.40 6 86516 107 46599433
Diuretic therapy 14.34 13.40 6 86516 107 46599433
Pneumonitis 14.30 13.40 19 86503 28401 46571139
Oesophageal haemorrhage 14.26 13.40 10 86512 516 46599024
Osteonecrosis 14.24 13.40 16 86506 25728 46573812
Bacteraemia 14.20 13.40 58 86464 14121 46585419
Renal stone removal 14.19 13.40 6 86516 110 46599430
Anaemia 14.13 13.40 594 85928 255185 46344355
Catheter site induration 14.06 13.40 5 86517 56 46599484
Cardiac resynchronisation therapy 14.04 13.40 4 86518 20 46599520
Product prescribing error 14.03 13.40 10 86512 20037 46579503
Smooth muscle antibody positive 13.99 13.40 6 86516 114 46599426
Breast cancer metastatic 13.97 13.40 4 86518 13674 46585866
Skin graft 13.92 13.40 10 86512 536 46599004
Jejunostomy 13.80 13.40 3 86519 3 46599537
Intestinal polypectomy 13.80 13.40 3 86519 3 46599537
Removal of transplanted organ 13.80 13.40 3 86519 3 46599537
Myringotomy 13.80 13.40 3 86519 3 46599537
Emotional disorder 13.75 13.40 3 86519 12321 46587219
Vascular cauterisation 13.75 13.40 5 86517 60 46599480
Nasopharyngitis 13.67 13.40 378 86144 153620 46445920
Bronchitis 13.67 13.40 274 86248 105705 46493835
Peritonitis 13.64 13.40 11 86511 20703 46578837
Blood creatine phosphokinase increased 13.49 13.40 19 86503 27705 46571835
Dilatation ventricular 13.48 13.40 20 86502 2547 46596993
Heart valve incompetence 13.44 13.40 19 86503 2316 46597224
Gastrointestinal surgery 13.43 13.40 7 86515 209 46599331

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
Pulmonary arterial hypertension 1266.30 17.62 432 27626 8869 29915551
Death 788.01 17.62 1280 26778 356003 29568417
Right ventricular failure 616.79 17.62 245 27813 7791 29916629
Pulmonary hypertension 563.26 17.62 299 27759 18737 29905683
Fluid retention 456.89 17.62 287 27771 24711 29899709
Dyspnoea 425.60 17.62 949 27109 332346 29592074
Lung transplant 225.67 17.62 80 27978 1836 29922584
Aspartate aminotransferase increased 217.49 17.62 282 27776 63140 29861280
Catheterisation cardiac 185.03 17.62 72 27986 2159 29922261
Alanine aminotransferase increased 173.27 17.62 275 27783 74001 29850419
Cardiac operation 172.25 17.62 71 27987 2481 29921939
Liver function test abnormal 152.99 17.62 166 27892 30784 29893636
Concomitant disease aggravated 147.09 17.62 79 27979 5050 29919370
Condition aggravated 144.36 17.62 365 27693 137501 29786919
Oxygen saturation decreased 140.80 17.62 188 27870 43252 29881168
Drug ineffective 132.07 17.62 78 27980 340309 29584111
Transfusion 131.96 17.62 84 27974 7377 29917043
Cardiac failure 131.30 17.62 260 27798 83158 29841262
Oedema 127.14 17.62 178 27880 42815 29881605
Hospitalisation 122.97 17.62 178 27880 44141 29880279
Toxicity to various agents 122.88 17.62 12 28046 177171 29747249
Disease progression 120.95 17.62 245 27813 79629 29844791
Pulmonary hypertensive crisis 101.00 17.62 25 28033 149 29924271
Pulmonary arterial pressure increased 100.01 17.62 38 28020 1066 29923354
Infusion site pain 99.67 17.62 49 28009 2601 29921819
Fluid overload 98.87 17.62 105 27953 18987 29905433
Blood alkaline phosphatase increased 97 17.62 133 27925 31354 29893066
Heart transplant 90.34 17.62 29 28029 485 29923935
Device related infection 85.32 17.62 92 27966 16923 29907497
Catheter placement 76.83 17.62 28 28030 697 29923723
Catheter site erythema 76.46 17.62 32 28026 1162 29923258
Cor pulmonale 76.09 17.62 28 28030 717 29923703
Respiratory failure 74.27 17.62 235 27823 100407 29824013
Pain in jaw 74.09 17.62 73 27985 12083 29912337
Cardiac pacemaker insertion 72.40 17.62 39 28019 2506 29921914
Oedema peripheral 71.68 17.62 240 27818 105592 29818828
Catheter management 70.73 17.62 28 28030 879 29923541
Cardiac failure congestive 70.62 17.62 206 27852 84201 29840219
Tracheostomy 69.57 17.62 26 28032 696 29923724
Heart and lung transplant 69.51 17.62 16 28042 66 29924354
Cardiac ablation 66.95 17.62 24 28034 569 29923851
Acute kidney injury 66.63 17.62 96 27962 273746 29650674
Infusion site erythema 66.61 17.62 32 28026 1614 29922806
Viral infection 65.65 17.62 76 27982 15109 29909311
Blood bilirubin increased 63.42 17.62 119 27939 36517 29887903
Mechanical ventilation 62.40 17.62 31 28027 1683 29922737
Oxygen consumption increased 61.26 17.62 28 28030 1260 29923160
Neutropenia 61.19 17.62 22 28036 128518 29795902
Disease complication 60.75 17.62 35 28023 2564 29921856
Stent placement 60.29 17.62 43 28015 4553 29919867
Dyspnoea exertional 59.98 17.62 114 27944 35316 29889104
Pulmonary vein stenosis 59.68 17.62 13 28045 39 29924381
Catheter site infection 59.57 17.62 34 28024 2447 29921973
Systemic scleroderma 59.10 17.62 18 28040 251 29924169
Balloon atrial septostomy 58.10 17.62 11 28047 11 29924409
Syncope 57.86 17.62 193 27865 84710 29839710
Overdose 57.63 17.62 6 28052 84331 29840089
Scleroderma 57.37 17.62 27 28031 1300 29923120
Drug interaction 54.61 17.62 64 27994 199504 29724916
Cyanosis 53.73 17.62 61 27997 11874 29912546
Central venous catheterisation 51.83 17.62 23 28035 965 29923455
Atrial septal defect repair 50.84 17.62 13 28045 90 29924330
Catheter site pain 50.12 17.62 23 28035 1045 29923375
Respiratory syncytial virus infection 50.00 17.62 34 28024 3334 29921086
Malignant neoplasm progression 49.76 17.62 5 28053 72282 29852138
Hypoxia 49.16 17.62 126 27932 47728 29876692
Respiratory distress 48.46 17.62 100 27958 32872 29891548
Cardioversion 48.15 17.62 21 28037 845 29923575
Terminal state 47.92 17.62 34 28024 3570 29920850
Transplant evaluation 47.17 17.62 18 28040 511 29923909
Brain natriuretic peptide increased 46.70 17.62 35 28023 4000 29920420
Haemoptysis 46.55 17.62 95 27963 30983 29893437
Cardiac disorder 46.22 17.62 110 27948 39783 29884637
Rhinovirus infection 44.83 17.62 30 28028 2865 29921555
Rhabdomyolysis 44.81 17.62 4 28054 63576 29860844
Pregnancy of partner 44.61 17.62 15 28043 292 29924128
Flushing 43.99 17.62 90 27968 29402 29895018
Pulmonary oedema 43.33 17.62 114 27944 43861 29880559
Exercise tolerance decreased 41.76 17.62 32 28026 3780 29920640
Liver function test increased 41.70 17.62 52 28006 11164 29913256
Biopsy liver 41.12 17.62 12 28046 143 29924277
Catheter site swelling 39.71 17.62 13 28045 232 29924188
Pneumonia 39.53 17.62 482 27576 333824 29590596
Catheter site discharge 39.38 17.62 16 28042 538 29923882
Cough 39.36 17.62 226 27832 125416 29799004
Neuropathy peripheral 39.14 17.62 9 28049 70466 29853954
Infusion site infection 38.97 17.62 14 28044 334 29924086
Rash 38.52 17.62 76 27982 191813 29732607
Dialysis 37.75 17.62 49 28009 10947 29913473
Tracheitis 37.72 17.62 16 28042 601 29923819
Ventricular septal defect repair 37.49 17.62 7 28051 6 29924414
Product administered to patient of inappropriate age 36.16 17.62 25 28033 2518 29921902
Patent ductus arteriosus repair 36.04 17.62 7 28051 9 29924411
Confusional state 36.03 17.62 44 28014 134790 29789630
White blood cell count decreased 35.67 17.62 17 28041 83930 29840490
Chronic obstructive pulmonary disease 35.15 17.62 109 27949 46017 29878403
Heart disease congenital 35.01 17.62 19 28039 1239 29923181
Hernia repair 34.46 17.62 18 28040 1086 29923334
Nasal congestion 34.24 17.62 62 27996 18504 29905916
Swelling 34.16 17.62 92 27966 35883 29888537
Concomitant disease progression 34.03 17.62 24 28034 2496 29921924
Product dose omission issue 33.52 17.62 172 27886 91459 29832961
Complication associated with device 32.36 17.62 33 28025 5687 29918733
Device occlusion 32.27 17.62 34 28024 6086 29918334
Drug hypersensitivity 32.11 17.62 12 28046 68507 29855913
Right ventricular systolic pressure increased 31.30 17.62 12 28046 345 29924075
Product use in unapproved indication 31.19 17.62 15 28043 73678 29850742
Hypertension 30.96 17.62 41 28017 121313 29803107
Infusion site discharge 30.73 17.62 8 28050 60 29924360
Depression 30.51 17.62 24 28034 90413 29834007
Endotracheal intubation 30.03 17.62 22 28036 2428 29921992
Micrococcus test positive 29.61 17.62 6 28052 11 29924409
Catheter removal 29.58 17.62 10 28048 198 29924222
Hyponatraemia 29.49 17.62 13 28045 67189 29857231
Thrombocytopenia 29.49 17.62 52 28006 136992 29787428
No adverse event 29.40 17.62 56 28002 17363 29907057
Catheter site pruritus 29.27 17.62 11 28047 299 29924121
Right ventricular dysfunction 29.09 17.62 15 28043 881 29923539
Acute myocardial infarction 28.92 17.62 7 28051 52932 29871488
Walking distance test abnormal 28.82 17.62 9 28049 137 29924283
Infusion site cellulitis 28.68 17.62 7 28051 39 29924381
Hyperkalaemia 28.60 17.62 13 28045 65997 29858423
Lung disorder 28.40 17.62 79 27979 31390 29893030
Endarterectomy 28.18 17.62 9 28049 148 29924272
Congestive hepatopathy 27.74 17.62 19 28039 1885 29922535
Ascites 27.46 17.62 85 27973 35836 29888584
Hypoglycaemia 27.35 17.62 7 28051 50974 29873446
Abdominal distension 26.02 17.62 98 27960 45611 29878809
Tracheostomy infection 25.83 17.62 6 28052 26 29924394
Plasma cell myeloma 25.66 17.62 9 28049 53453 29870967
Pleural mass 25.66 17.62 7 28051 64 29924356
Infusion site swelling 25.63 17.62 17 28041 1599 29922821
Localised oedema 25.61 17.62 22 28036 3054 29921366
Influenza 25.50 17.62 94 27964 43304 29881116
Acute respiratory failure 25.44 17.62 67 27991 25783 29898637
Pulmonary veno-occlusive disease 25.28 17.62 11 28047 440 29923980
Delirium 25.07 17.62 4 28054 40627 29883793
Sickle cell anaemia 25 17.62 9 28049 216 29924204
Medical device change 24.74 17.62 8 28050 137 29924283
Carbon dioxide increased 24.48 17.62 14 28044 1011 29923409
Transplant 24.35 17.62 12 28046 640 29923780
Haematuria 24.35 17.62 6 28052 44828 29879592
Foetal exposure during pregnancy 24.23 17.62 3 28055 36868 29887552
Implantable defibrillator replacement 24.07 17.62 5 28053 11 29924409
Adenotonsillectomy 24.06 17.62 6 28052 37 29924383
Pulmonary artery therapeutic procedure 23.90 17.62 4 28054 0 29924420
Pancytopenia 23.51 17.62 27 28031 85025 29839395
Chemotherapy 23.38 17.62 11 28047 529 29923891
Oxygen therapy 23.30 17.62 12 28046 703 29923717
High frequency ablation 23.22 17.62 8 28050 168 29924252
Biopsy lung 22.96 17.62 7 28051 98 29924322
Hallucination 22.31 17.62 9 28049 49050 29875370
Systemic-pulmonary artery shunt 21.66 17.62 4 28054 3 29924417
Biopsy lymph gland 21.51 17.62 6 28052 60 29924360
Arthralgia 21.45 17.62 61 27997 135730 29788690
Pneumothorax 21.34 17.62 47 28011 16146 29908274
Right-to-left cardiac shunt 21.28 17.62 5 28053 23 29924397
Respiratory disorder 21.08 17.62 49 28009 17445 29906975
Headache 21.06 17.62 262 27796 182044 29742376
Cardiac flutter 20.84 17.62 15 28043 1611 29922809
Pulmonary fibrosis 20.80 17.62 46 28012 15844 29908576
Weight increased 20.39 17.62 130 27928 74783 29849637
Urticaria 20.37 17.62 13 28045 54593 29869827
Choking sensation 20.26 17.62 13 28045 1156 29923264
Exercise test abnormal 20.24 17.62 4 28054 6 29924414
Implantable defibrillator insertion 20.22 17.62 11 28047 721 29923699
Treatment failure 20.12 17.62 4 28054 34675 29889745
Device infusion issue 20.11 17.62 10 28048 544 29923876
Product supply issue 19.80 17.62 8 28050 265 29924155
Epistaxis 19.73 17.62 100 27958 52881 29871539
Resuscitation 19.64 17.62 13 28045 1219 29923201
Adverse event 19.62 17.62 44 28014 15297 29909123
Intentional product use issue 19.55 17.62 5 28053 36435 29887985
Cyanosis central 19.55 17.62 6 28052 86 29924334
Pulmonary haemorrhage 19.43 17.62 33 28025 9359 29915061
Surgery 19.32 17.62 37 28021 11514 29912906
Suicidal ideation 19.29 17.62 5 28053 36109 29888311
Deep vein thrombosis 19.23 17.62 17 28041 60484 29863936
Exposure via body fluid 19.23 17.62 6 28052 91 29924329
Gastrointestinal tube insertion 19.18 17.62 13 28045 1268 29923152
Infusion site inflammation 19.03 17.62 5 28053 39 29924381
Microcytic anaemia 19.00 17.62 16 28042 2162 29922258
Radiotherapy to brain 18.92 17.62 5 28053 40 29924380
Normal newborn 18.85 17.62 7 28051 184 29924236
Dysarthria 18.81 17.62 3 28055 30487 29893933
Hypoaesthesia 18.78 17.62 14 28044 54216 29870204
Infusion site haemorrhage 18.67 17.62 9 28049 457 29923963
Gallbladder operation 18.64 17.62 9 28049 459 29923961
Hyperglycaemia 18.56 17.62 5 28053 35195 29889225
Dyspnoea at rest 18.44 17.62 17 28041 2589 29921831
Blood creatine phosphokinase increased 18.43 17.62 9 28049 43839 29880581
Catheter site granuloma 18.36 17.62 4 28054 12 29924408
Phlebotomy 18.36 17.62 4 28054 12 29924408
Respiratory tract infection viral 18.04 17.62 12 28046 1134 29923286
Tracheostomy malfunction 18.02 17.62 5 28053 49 29924371
Infusion 17.92 17.62 3 28055 0 29924420
Oxygen consumption 17.92 17.62 3 28055 0 29924420
Scleroderma associated digital ulcer 17.92 17.62 3 28055 0 29924420
Aneurysm repair 17.92 17.62 3 28055 0 29924420
Cardiopulmonary bypass 17.92 17.62 3 28055 0 29924420
Spinal cord operation 17.92 17.62 3 28055 0 29924420
Cavopulmonary anastomosis 17.92 17.62 3 28055 0 29924420
Right ventricular dilatation 17.92 17.62 9 28049 500 29923920
Angioedema 17.91 17.62 5 28053 34379 29890041
Muscular weakness 17.80 17.62 20 28038 63625 29860795
Bronchopulmonary dysplasia 17.69 17.62 9 28049 514 29923906

Pharmacologic Action:

SourceCodeDescription
ATC C02KX01 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
OTHER ANTIHYPERTENSIVES
Antihypertensives for pulmonary arterial hypertension
FDA MoA N0000175364 Endothelin Receptor Antagonists
FDA EPC N0000175581 Endothelin Receptor Antagonist
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D065128 Endothelin Receptor Antagonists
FDA MoA N0000185507 Cytochrome P450 2C9 Inducers
FDA MoA N0000190118 Cytochrome P450 3A Inducers
CHEBI has role CHEBI:35674 antihypertensive
CHEBI has role CHEBI:51451 era

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Pulmonary arterial hypertension indication 11399002
Pulmonary hypertension indication 70995007 DOID:6432
Systemic sclerosis indication 89155008 DOID:418
Hyperbilirubinemia contraindication 14783006 DOID:2741
Pulmonary edema contraindication 19242006 DOID:11396
Hepatic failure contraindication 59927004
Pulmonary veno-occlusive disease contraindication 89420002 DOID:5453
Liver function tests abnormal contraindication 166603001
Decompensated cardiac failure contraindication 195111005
Disease of liver contraindication 235856003 DOID:409
Drug-induced hepatitis contraindication 235876009
Edema contraindication 267038008
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.84 acidic
pKa2 2.87 Basic
pKa3 1.44 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
32MG TRACLEER ACTELION N209279 Sept. 5, 2017 RX TABLET, FOR SUSPENSION ORAL Sept. 5, 2024 TREATMENT OF PULMONULLRY ARTERIAL HYPERTENSION (PAH) (WHO GROUP 1) IN PEDIATRIC PATIENTS AGED 3 YRS AND OLDER WITH IDIOPATHIC OR CONGENITAL PAH TO IMPROVE PULMONULLRY VASCULAR RESISTANCE (PVR), WHICH IS EXPECTED TO RESULT IN AN IMPROVEMENT IN EXERCISE ABILITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Endothelin B receptor GPCR ANTAGONIST Ki 7.10 CHEMBL CHEMBL
Endothelin-1 receptor GPCR ANTAGONIST Ki 8.19 CHEMBL CHEMBL
Bile salt export pump Transporter IC50 4.42 CHEMBL
Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor WOMBAT-PK
Endothelin-1 receptor GPCR IC50 8.12 CHEMBL
Bile salt export pump Unclassified IC50 4.51 CHEMBL
Endothelin B receptor Unclassified IC50 7.02 CHEMBL
Endothelin-1 receptor GPCR Ki 8.19 CHEMBL

External reference:

IDSource
Q326023R30 UNII
D01227 KEGG_DRUG
157212-55-0 SECONDARY_CAS_RN
4021289 VANDF
C0252643 UMLSCUI
CHEBI:51450 CHEBI
K86 PDB_CHEM_ID
104865 PUBCHEM_CID
CHEMBL957 ChEMBL_ID
DB00559 DRUGBANK_ID
D000077300 MESH_DESCRIPTOR_UI
7195 INN_ID
3494 IUPHAR_LIGAND_ID
1468845 RXNORM
16217 MMSL
230939 MMSL
33033 MMSL
42472 MMSL
d04782 MMSL
009514 NDDF
385558007 SNOMEDCT_US
385559004 SNOMEDCT_US
725734005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 0054-0520 TABLET 62.50 mg ORAL ANDA 25 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 0054-0521 TABLET 125 mg ORAL ANDA 25 sections
bosentan HUMAN PRESCRIPTION DRUG LABEL 1 0591-2511 TABLET, FILM COATED 62.50 mg ORAL ANDA 27 sections
bosentan HUMAN PRESCRIPTION DRUG LABEL 1 0591-2512 TABLET, FILM COATED 125 mg ORAL ANDA 27 sections
bosentan HUMAN PRESCRIPTION DRUG LABEL 1 10148-125 TABLET, FILM COATED 125 mg ORAL NDA AUTHORIZED GENERIC 30 sections
bosentan HUMAN PRESCRIPTION DRUG LABEL 1 10148-625 TABLET, FILM COATED 62.50 mg ORAL NDA AUTHORIZED GENERIC 30 sections
Bosentan Human Prescription Drug Label 1 46708-383 TABLET, FILM COATED 62.50 mg ORAL ANDA 26 sections
Bosentan Human Prescription Drug Label 1 46708-384 TABLET, FILM COATED 125 mg ORAL ANDA 26 sections
Bosentan Human Prescription Drug Label 1 47335-038 TABLET, FILM COATED 62.50 mg ORAL ANDA 27 sections
Bosentan Human Prescription Drug Label 1 47335-039 TABLET, FILM COATED 125 mg ORAL ANDA 27 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 47781-270 TABLET, FILM COATED 62.50 mg ORAL ANDA 27 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 47781-271 TABLET, FILM COATED 125 mg ORAL ANDA 27 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 49884-058 TABLET, FILM COATED 62.50 mg ORAL ANDA 26 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 49884-059 TABLET, FILM COATED 125 mg ORAL ANDA 26 sections
Bosentan Human Prescription Drug Label 1 62332-383 TABLET, FILM COATED 62.50 mg ORAL ANDA 26 sections
Bosentan Human Prescription Drug Label 1 62332-384 TABLET, FILM COATED 125 mg ORAL ANDA 26 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 65162-873 TABLET, FILM COATED 62.50 mg ORAL ANDA 23 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 65162-874 TABLET, FILM COATED 125 mg ORAL ANDA 23 sections
Tracleer HUMAN PRESCRIPTION DRUG LABEL 1 66215-101 TABLET, FILM COATED 62.50 mg ORAL NDA 30 sections
Tracleer HUMAN PRESCRIPTION DRUG LABEL 1 66215-102 TABLET, FILM COATED 125 mg ORAL NDA 30 sections
Tracleer HUMAN PRESCRIPTION DRUG LABEL 1 66215-103 TABLET, SOLUBLE 32 mg ORAL NDA 30 sections
Bosentan Human Prescription Drug Label 1 68180-386 TABLET 125 mg ORAL ANDA 27 sections
Bosentan Human Prescription Drug Label 1 68180-387 TABLET 62.50 mg ORAL ANDA 27 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 68382-446 TABLET, COATED 62.50 mg ORAL ANDA 25 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 68382-447 TABLET, COATED 125 mg ORAL ANDA 25 sections
BOSENTAN HUMAN PRESCRIPTION DRUG LABEL 1 69097-377 TABLET, FILM COATED 62.50 mg ORAL ANDA 24 sections
BOSENTAN HUMAN PRESCRIPTION DRUG LABEL 1 69097-378 TABLET, FILM COATED 125 mg ORAL ANDA 24 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 70771-1017 TABLET 62.50 mg ORAL ANDA 1 sections
Bosentan HUMAN PRESCRIPTION DRUG LABEL 1 70771-1018 TABLET 125 mg ORAL ANDA 1 sections