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

Stem definitionDrug idCAS RN
endothelin receptor antagonists 4337 177036-94-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • LU208075
  • LU 208075
  • ambrisentan
  • letairis
  • volibris
an endothelin receptor antagonist that is selective for the endothelin type-A (ETA) receptor
  • Molecular weight: 378.43
  • Formula: C22H22N2O4
  • CLOGP: 3.75
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 81.54
  • ALOGS: -3.88
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
7.50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.06 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 5 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.38 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
June 20, 2019 EMA MYLAN SAS
June 15, 2007 FDA GILEAD

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
Dyspnoea 3555.46 17.66 4726 89130 510822 46081384
Fluid retention 2055.15 17.66 1278 92578 49768 46542438
Pulmonary arterial hypertension 1757.09 17.66 913 92943 25015 46567191
Nasal congestion 1647.19 17.66 1088 92768 47025 46545181
Headache 1403.11 17.66 3005 90851 475347 46116859
Death 1374.12 17.66 2429 91427 333119 46259087
Pain in jaw 1296.55 17.66 861 92995 37511 46554695
Oedema 1269.24 17.66 1062 92794 66009 46526197
Pulmonary hypertension 988.20 17.66 711 93145 35282 46556924
Unevaluable event 897.49 17.66 743 93113 45432 46546774
Right ventricular failure 837.23 17.66 476 93380 15617 46576589
Oedema peripheral 795.39 17.66 1265 92591 158441 46433765
Flushing 702.23 17.66 753 93103 63861 46528345
Fluid overload 653.67 17.66 496 93360 26689 46565517
Dyspnoea exertional 605.16 17.66 619 93237 49670 46542536
Peripheral swelling 584.44 17.66 1098 92758 156973 46435233
Drug ineffective 541.11 17.66 351 93505 677487 45914719
Chest pain 454.95 17.66 1057 92799 175267 46416939
Infusion site pain 451.70 17.66 271 93585 9836 46582370
Lung transplant 426.76 17.66 175 93681 2717 46589489
Dizziness 416.37 17.66 1563 92293 338851 46253355
Rheumatoid arthritis 376.29 17.66 28 93828 240187 46352019
Catheterisation cardiac 370.27 17.66 175 93681 3872 46588334
Toxicity to various agents 354.87 17.66 17 93839 211749 46380457
Palpitations 332.07 17.66 646 93210 94613 46497593
Oxygen saturation decreased 324.43 17.66 534 93322 68630 46523576
Syncope 307.68 17.66 662 93194 104141 46488065
Catheter site erythema 285.98 17.66 146 93710 3837 46588369
Device related infection 284.26 17.66 276 93580 20765 46571441
Swelling 263.03 17.66 692 93164 123819 46468387
Diarrhoea 262.55 17.66 1970 91886 557632 46034574
Drug interaction 245.72 17.66 54 93802 203040 46389166
Neutropenia 238.17 17.66 12 93844 143192 46449014
Scleroderma 238.14 17.66 136 93720 4493 46587713
Pneumonia 238.14 17.66 1428 92428 374892 46217314
Malaise 237.74 17.66 1300 92556 329932 46262274
Drug hypersensitivity 225.74 17.66 104 93752 243721 46348485
Hospitalisation 218.47 17.66 428 93428 62957 46529249
Infusion site infection 207.50 17.66 86 93770 1373 46590833
Catheter site pruritus 204.13 17.66 93 93763 1886 46590320
Cough 201.56 17.66 956 92900 229293 46362913
Catheter site pain 198.96 17.66 113 93743 3693 46588513
Oxygen consumption increased 197.56 17.66 111 93745 3552 46588654
Central venous catheterisation 192.53 17.66 90 93766 1940 46590266
Infusion site erythema 189.24 17.66 142 93714 7500 46584706
Infusion related reaction 188.03 17.66 3 93853 101205 46491001
Catheter site discharge 185.70 17.66 87 93769 1885 46590321
Hypoxia 180.99 17.66 352 93504 51486 46540720
Cardiac failure 173.44 17.66 449 93407 79499 46512707
Hypotension 173.38 17.66 923 92933 231666 46360540
Febrile neutropenia 170.97 17.66 4 93852 94623 46497583
Respiratory failure 170.41 17.66 497 93359 94319 46497887
Catheter management 168.07 17.66 91 93765 2704 46589502
Cardiac failure congestive 166.88 17.66 483 93373 91267 46500939
Alopecia 163.56 17.66 61 93795 162353 46429853
Vascular device infection 161.52 17.66 96 93760 3421 46588785
Contraindicated product administered 145.91 17.66 3 93853 79944 46512262
Psoriasis 139.44 17.66 4 93852 78600 46513606
Catheter placement 138.91 17.66 71 93785 1870 46590336
Product use in unapproved indication 137.04 17.66 12 93844 90261 46501945
White blood cell count decreased 135.30 17.66 30 93826 112201 46480005
Nasopharyngitis 134.22 17.66 639 93217 153359 46438847
Therapeutic product effect decreased 133.93 17.66 8 93848 82593 46509613
Device leakage 133.52 17.66 100 93756 5265 46586941
Infusion site swelling 128.16 17.66 100 93756 5599 46586607
Transfusion 124.19 17.66 143 93713 13088 46579118
Pulmonary arterial pressure increased 120.20 17.66 78 93778 3254 46588952
Infusion site discharge 119.74 17.66 45 93811 546 46591660
Off label use 116.42 17.66 384 93472 379457 46212749
Myalgia 113.26 17.66 519 93337 122569 46469637
Intentional overdose 112.70 17.66 4 93852 64940 46527266
Acute kidney injury 111.75 17.66 189 93667 235666 46356540
Exposure during pregnancy 111.68 17.66 39 93817 108173 46484033
Therapy change 111.62 17.66 88 93768 5002 46587204
Malignant neoplasm progression 109.30 17.66 5 93851 64921 46527285
Maternal exposure during pregnancy 109.25 17.66 35 93821 102514 46489692
Acute respiratory failure 109.23 17.66 204 93652 28934 46563272
Intentional dose omission 108.93 17.66 73 93783 3217 46588989
Dermatitis contact 108.64 17.66 106 93750 8017 46584189
Hypertension 107.91 17.66 142 93714 196214 46395992
Transplant evaluation 106.07 17.66 49 93807 1027 46591179
Catheter site infection 106.01 17.66 83 93773 4670 46587536
Chest discomfort 103.48 17.66 407 93449 89862 46502344
Therapeutic product effect incomplete 102.42 17.66 17 93839 78136 46514070
Pain in extremity 100.99 17.66 875 92981 257805 46334401
C-reactive protein increased 100.33 17.66 4 93852 58586 46533620
Drug abuse 100.24 17.66 7 93849 63401 46528805
Epistaxis 99.51 17.66 320 93536 63985 46528221
Nausea 99.23 17.66 1933 91923 685521 45906685
Sinus congestion 99.13 17.66 127 93729 12982 46579224
Depression 98.68 17.66 118 93738 169986 46422220
Hyponatraemia 93.97 17.66 43 93813 101289 46490917
Catheter site haemorrhage 91.84 17.66 61 93795 2648 46589558
Neuropathy peripheral 91.67 17.66 34 93822 90859 46501347
Rash 91.19 17.66 388 93468 356124 46236082
Pancytopenia 90.65 17.66 29 93827 85029 46507177
Thrombocytopenia 90.49 17.66 73 93783 126508 46465698
Electrocardiogram QT prolonged 89.62 17.66 3 93853 51322 46540884
Blood pressure increased 89.37 17.66 74 93782 126592 46465614
Catheter site rash 89.18 17.66 39 93817 715 46591491
Deep vein thrombosis 89.01 17.66 25 93831 79748 46512458
Device dislocation 88.50 17.66 158 93698 21644 46570562
Catheter site swelling 87.86 17.66 46 93810 1275 46590931
Presyncope 87.68 17.66 168 93688 24286 46567920
Stomatitis 86.99 17.66 16 93840 68281 46523925
Device alarm issue 85.65 17.66 46 93810 1344 46590862
Injection site pain 85.46 17.66 55 93801 107097 46485109
Leukopenia 84.95 17.66 17 93839 68326 46523880
Injection site discharge 84.89 17.66 31 93825 345 46591861
Overdose 84.59 17.66 50 93806 101929 46490277
Confusional state 84.41 17.66 119 93737 159773 46432433
Musculoskeletal stiffness 84.21 17.66 46 93810 97947 46494259
Suicide attempt 81.68 17.66 8 93848 55028 46537178
Arthropathy 81.60 17.66 34 93822 84666 46507540
Infusion site haemorrhage 81.15 17.66 52 93804 2122 46590084
Cor pulmonale 78.85 17.66 49 93807 1894 46590312
Abdominal distension 78.67 17.66 324 93532 73027 46519179
Anaphylactic reaction 78.10 17.66 8 93848 53104 46539102
Osteoarthritis 77.99 17.66 15 93841 62010 46530196
Haemoptysis 76.20 17.66 165 93691 26024 46566182
Oxygen therapy 75.79 17.66 47 93809 1810 46590396
Bradycardia 73.54 17.66 21 93835 66277 46525929
Urticaria 71.35 17.66 79 93777 117813 46474393
Injection site reaction 70.89 17.66 7 93849 47842 46544364
Seizure 68.56 17.66 88 93768 122966 46469240
Multiple sclerosis relapse 68.51 17.66 4 93852 42121 46550085
Agitation 68.42 17.66 14 93842 55401 46536805
Exercise tolerance decreased 67.42 17.66 63 93793 4514 46587692
Cardiac disorder 66.70 17.66 217 93639 43641 46548565
Infusion site pruritus 66.13 17.66 53 93803 3085 46589121
Weight increased 65.98 17.66 560 93296 163913 46428293
Pulmonary oedema 64.78 17.66 238 93618 50867 46541339
Somnolence 64.75 17.66 136 93720 156385 46435821
Plasma cell myeloma 64.62 17.66 7 93849 44471 46547735
Suicidal ideation 64.15 17.66 17 93839 56365 46535841
Device infusion issue 63.91 17.66 35 93821 1064 46591142
Coma 63.77 17.66 19 93837 58330 46533876
Blood cholesterol increased 61.58 17.66 5 93851 40008 46552198
Injection site erythema 61.00 17.66 37 93819 74390 46517816
Therapy non-responder 60.24 17.66 201 93655 40951 46551255
Heart rate increased 59.80 17.66 303 93553 74488 46517718
Glossodynia 59.60 17.66 9 93847 44364 46547842
Catheter site inflammation 57.92 17.66 28 93828 652 46591554
Blood glucose increased 57.36 17.66 37 93819 71976 46520230
Hallucination 56.94 17.66 15 93841 49936 46542270
Metabolic acidosis 56.60 17.66 6 93850 38774 46553432
Mechanical ventilation 56.39 17.66 34 93822 1244 46590962
Catheter site vesicles 55.64 17.66 21 93835 258 46591948
Pulmonary veno-occlusive disease 55.41 17.66 30 93826 891 46591315
Pulmonary embolism 54.17 17.66 84 93772 108501 46483705
Therapy cessation 54.06 17.66 146 93710 26483 46565723
Lactic acidosis 52.85 17.66 4 93852 33905 46558301
Sinus disorder 52.41 17.66 108 93748 16455 46575751
Fatigue 52.38 17.66 1596 92260 607101 45985105
Abortion spontaneous 51.90 17.66 12 93844 43634 46548572
Therapy interrupted 51.43 17.66 84 93772 10707 46581499
Endotracheal intubation 50.88 17.66 39 93817 2126 46590080
Alanine aminotransferase increased 50.57 17.66 62 93794 88389 46503817
Complication associated with device 50.41 17.66 102 93754 15339 46576867
Dialysis 49.92 17.66 80 93776 10036 46582170
Cardiac operation 49.84 17.66 42 93814 2624 46589582
Pericardial effusion 49.81 17.66 138 93718 25405 46566801
Abdominal pain upper 49.70 17.66 478 93378 144827 46447379
Terminal state 49.49 17.66 39 93817 2215 46589991
Emergency care 49.47 17.66 27 93829 815 46591391
Walking distance test abnormal 49.23 17.66 23 93833 495 46591711
Device connection issue 49.13 17.66 25 93831 652 46591554
Hypoglycaemia 48.92 17.66 24 93832 54325 46537881
Upper respiratory tract congestion 48.88 17.66 36 93820 1847 46590359
Infusion site induration 47.91 17.66 26 93830 776 46591430
Hyperkalaemia 47.80 17.66 21 93835 50688 46541518
Bone marrow failure 47.69 17.66 3 93853 29666 46562540
Depressed level of consciousness 47.60 17.66 18 93838 47551 46544655
Transplant 46.92 17.66 24 93832 633 46591573
Delirium 46.80 17.66 9 93847 37219 46554987
Liver function test abnormal 46.45 17.66 201 93655 46286 46545920
Hot flush 45.68 17.66 191 93665 43326 46548880
Hypothyroidism 45.35 17.66 5 93851 31333 46560873
Hypoaesthesia 45.29 17.66 108 93748 118761 46473445
Injury 45.17 17.66 16 93840 44011 46548195
Lung disorder 44.62 17.66 189 93667 43115 46549091
Ear discomfort 44.19 17.66 61 93795 6700 46585506
Emotional distress 44.18 17.66 5 93851 30702 46561504
Feeling abnormal 44.04 17.66 414 93442 124646 46467560
Product quality issue 44.01 17.66 9 93847 35639 46556567
Dizziness postural 43.40 17.66 59 93797 6387 46585819
Inappropriate schedule of product administration 43.38 17.66 40 93816 64973 46527233
Blood pressure systolic increased 43.20 17.66 4 93852 28783 46563423
Platelet count decreased 42.97 17.66 85 93771 99939 46492267
Dyspnoea at rest 42.79 17.66 44 93812 3544 46588662
Device occlusion 42.45 17.66 56 93800 5889 46586317
Blood creatinine increased 42.16 17.66 55 93801 76348 46515858
Intentional product misuse 42.13 17.66 21 93835 47107 46545099
Therapeutic response decreased 42.06 17.66 17 93839 43128 46549078
Blood pressure decreased 41.84 17.66 226 93630 56933 46535273
Herpes zoster 41.58 17.66 45 93811 67827 46524379
Catheter site irritation 41.56 17.66 20 93836 461 46591745
No adverse event 41.53 17.66 9 93847 34222 46557984
Paracentesis 41.33 17.66 25 93831 920 46591286
Hypokalaemia 41.18 17.66 71 93785 87953 46504253
Sickle cell anaemia 40.47 17.66 21 93835 571 46591635
Paranasal sinus discomfort 40.26 17.66 37 93819 2595 46589611
Arthralgia 39.74 17.66 506 93350 364097 46228109
Mouth ulceration 39.55 17.66 4 93852 26828 46565378
Paraesthesia 39.18 17.66 114 93742 117323 46474883
Central venous catheter removal 39.06 17.66 17 93839 308 46591898
Cognitive disorder 38.53 17.66 13 93843 36870 46555336
Ear congestion 38.36 17.66 30 93826 1685 46590521
Localised oedema 38.15 17.66 49 93807 5020 46587186
Mobility decreased 37.31 17.66 40 93816 60554 46531652
Femur fracture 37.02 17.66 14 93842 36983 46555223
Oxygen consumption 36.92 17.66 12 93844 91 46592115
Disturbance in attention 36.89 17.66 9 93847 31551 46560655
Atrial flutter 36.74 17.66 66 93790 9082 46583124
Encephalopathy 36.58 17.66 11 93845 33578 46558628
Throat irritation 36.11 17.66 134 93722 28767 46563439
Injection site swelling 36.00 17.66 18 93838 40309 46551897
Chronic respiratory failure 35.78 17.66 29 93827 1715 46590491
Stevens-Johnson syndrome 35.60 17.66 3 93853 23294 46568912
Urinary tract infection 35.54 17.66 278 93578 219988 46372218
Influenza 35.24 17.66 303 93553 88967 46503239
Inflammation 35.00 17.66 28 93828 48753 46543453
Sedation 34.87 17.66 3 93853 22907 46569299
Infusion site cellulitis 34.79 17.66 13 93843 155 46592051
Joint swelling 34.65 17.66 194 93662 165879 46426327
Drug-induced liver injury 34.40 17.66 5 93851 25363 46566843
Breast cancer 34.09 17.66 25 93831 45493 46546713
Hyperglycaemia 33.89 17.66 14 93842 35057 46557149
Oxygen saturation abnormal 33.63 17.66 34 93822 2684 46589522
Hypomagnesaemia 33.56 17.66 3 93853 22207 46569999
Wrong technique in product usage process 33.42 17.66 36 93820 54386 46537820
Pneumonitis 33.42 17.66 8 93848 28412 46563794
Impaired healing 33.41 17.66 16 93840 36727 46555479
Premature delivery 33.29 17.66 3 93853 22066 46570140
Generalised tonic-clonic seizure 33.17 17.66 7 93849 27115 46565091
Osteonecrosis 32.84 17.66 6 93850 25738 46566468
Infusion site warmth 32.79 17.66 24 93832 1219 46590987
Infusion site oedema 32.54 17.66 17 93839 469 46591737
Drug intolerance 32.21 17.66 169 93687 146880 46445326
Osteoporosis 32.14 17.66 21 93835 40587 46551619
Angioedema 31.61 17.66 20 93836 39322 46552884
Catheter site warmth 31.51 17.66 13 93843 205 46592001
Nasal dryness 31.46 17.66 37 93819 3463 46588743
Pruritus 31.18 17.66 324 93532 242028 46350178
Disorientation 30.74 17.66 18 93838 36900 46555306
Systemic scleroderma 30.57 17.66 20 93836 846 46591360
Brain natriuretic peptide increased 30.46 17.66 42 93814 4608 46587598
Jaundice 30.43 17.66 10 93846 28835 46563371
Eczema 30.17 17.66 3 93853 20397 46571809
General physical health deterioration 30.10 17.66 125 93731 115644 46476562
Nocturnal dyspnoea 30.08 17.66 21 93835 990 46591216
Lower respiratory tract infection 30.04 17.66 40 93816 55049 46537157
Aphasia 29.96 17.66 10 93846 28557 46563649
Device related sepsis 29.96 17.66 35 93821 3252 46588954
Diabetes mellitus 29.77 17.66 34 93822 50031 46542175
Aggression 29.67 17.66 5 93851 22739 46569467
Generalised oedema 29.27 17.66 79 93777 14320 46577886
Device breakage 29.26 17.66 62 93794 9630 46582576
Pancreatitis acute 29.25 17.66 7 93849 24865 46567341
Type 2 diabetes mellitus 29.20 17.66 3 93853 19872 46572334
Cardiac failure high output 29.11 17.66 13 93843 251 46591955
Multiple sclerosis 29.11 17.66 7 93849 24784 46567422
Infusion site irritation 29.02 17.66 16 93840 493 46591713
Abnormal behaviour 28.91 17.66 4 93852 21054 46571152
Fibromyalgia 28.67 17.66 19 93837 36444 46555762
Metastases to liver 28.66 17.66 3 93853 19582 46572624
Skin lesion 28.64 17.66 9 93847 26704 46565502
Altered state of consciousness 28.61 17.66 6 93850 23342 46568864
Gamma-glutamyltransferase increased 28.59 17.66 14 93842 31726 46560480
White blood cell count increased 28.57 17.66 28 93828 44191 46548015
Infusion site rash 28.42 17.66 20 93836 955 46591251
Oral herpes 28.29 17.66 3 93853 19387 46572819
Basal cell carcinoma 27.87 17.66 4 93852 20483 46571723
Hepatitis 27.84 17.66 15 93841 32200 46560006
Infusion site vesicles 27.69 17.66 14 93842 360 46591846
Hepatotoxicity 27.58 17.66 8 93848 25001 46567205
Disseminated intravascular coagulation 27.58 17.66 3 93853 19002 46573204
Tremor 27.56 17.66 129 93727 115510 46476696
Hypersensitivity 27.48 17.66 183 93673 150138 46442068
Psychotic disorder 27.33 17.66 6 93850 22615 46569591
Dysphagia 27.30 17.66 73 93783 77239 46514967
Portopulmonary hypertension 27.25 17.66 10 93846 113 46592093
Dyskinesia 27.22 17.66 12 93844 28913 46563293
Gastric disorder 27.08 17.66 116 93740 26589 46565617
Injection site pruritus 27.05 17.66 24 93832 39719 46552487
Ascites 27.00 17.66 145 93711 36439 46555767
Chronic obstructive pulmonary disease 26.75 17.66 203 93653 57430 46534776
Toxic epidermal necrolysis 26.73 17.66 6 93850 22272 46569934
Cerebral infarction 26.66 17.66 7 93849 23359 46568847
Hypercalcaemia 26.64 17.66 5 93851 21041 46571165
Hepatocellular injury 26.62 17.66 13 93843 29509 46562697
Full blood count decreased 26.62 17.66 6 93850 22205 46570001
Arthritis 26.55 17.66 74 93782 77242 46514964
Catheter site cellulitis 26.53 17.66 12 93844 239 46591967
Diabetic ketoacidosis 26.11 17.66 3 93853 18207 46573999
Liver transplant 25.90 17.66 28 93828 2389 46589817
Infusion site abscess 25.75 17.66 11 93845 190 46592016
Catheter removal 25.69 17.66 13 93843 335 46591871
Hallucination, visual 25.49 17.66 3 93853 17870 46574336
Epilepsy 25.44 17.66 8 93848 23730 46568476
Infusion site inflammation 25.34 17.66 11 93845 198 46592008
Infusion site haematoma 25.19 17.66 11 93845 201 46592005
Pulmonary pain 24.55 17.66 23 93833 1653 46590553
Tracheostomy 24.46 17.66 15 93841 566 46591640
Medication error 24.44 17.66 16 93840 30895 46561311
CREST syndrome 24.32 17.66 13 93843 376 46591830
Middle ear effusion 24.09 17.66 24 93832 1861 46590345
Peritonitis 24.03 17.66 6 93850 20708 46571498
Drug titration error 23.97 17.66 15 93841 587 46591619
Haematuria 23.96 17.66 12 93844 26846 46565360
Respiratory tract congestion 23.94 17.66 68 93788 12696 46579510
Anxiety 23.90 17.66 242 93614 181715 46410491
Asthma 23.69 17.66 99 93757 91443 46500763
Dry eye 23.57 17.66 16 93840 30306 46561900
Loss of personal independence in daily activities 23.35 17.66 50 93806 57133 46535073
Anaemia 23.28 17.66 676 93180 255103 46337103
Ejection fraction decreased 23.27 17.66 4 93852 17933 46574273
Biopsy liver 23.22 17.66 13 93843 413 46591793
Osteomyelitis 23.19 17.66 8 93848 22375 46569831
Aspartate aminotransferase increased 23.02 17.66 81 93775 78619 46513587
Dizziness exertional 23.00 17.66 12 93844 330 46591876
Application site pruritus 22.98 17.66 34 93822 3979 46588227
Product prescribing error 22.88 17.66 6 93850 20041 46572165
Renal impairment 22.80 17.66 75 93781 74297 46517909
Thrombosis in device 22.74 17.66 29 93827 2950 46589256
Treatment noncompliance 22.73 17.66 119 93737 29612 46562594
Hepatic steatosis 22.59 17.66 10 93846 24032 46568174
Cardio-respiratory arrest 22.31 17.66 55 93801 59814 46532392
Gait disturbance 22.18 17.66 186 93670 145077 46447129
Hepatic enzyme increased 22.08 17.66 87 93769 81700 46510506
Right ventricular enlargement 21.93 17.66 11 93845 278 46591928
Injection site infection 21.76 17.66 21 93835 1566 46590640
Pulmonary artery dilatation 21.71 17.66 10 93846 208 46591998
Pulmonary vein occlusion 21.28 17.66 6 93850 26 46592180
Heart valve replacement 21.24 17.66 13 93843 489 46591717
Mitral valve replacement 21.16 17.66 10 93846 221 46591985
Hemiparesis 21.09 17.66 7 93849 20062 46572144
Coronary artery disease 21.09 17.66 22 93834 33730 46558476
Echocardiogram 20.92 17.66 6 93850 28 46592178
Faeces soft 20.89 17.66 30 93826 3418 46588788
Pericarditis 20.88 17.66 11 93845 23916 46568290
Catheterisation cardiac abnormal 20.88 17.66 10 93846 228 46591978
Migraine 20.86 17.66 224 93632 69802 46522404
Lymphopenia 20.77 17.66 3 93853 15290 46576916
Dysarthria 20.67 17.66 27 93829 37471 46554735
Fracture 20.66 17.66 4 93852 16467 46575739
Heart and lung transplant 20.58 17.66 8 93848 107 46592099
Biopsy lung 20.43 17.66 9 93847 168 46592038
Blood alkaline phosphatase increased 20.36 17.66 30 93826 39579 46552627
Injection site mass 20.31 17.66 3 93853 15037 46577169
Catheter site related reaction 20.17 17.66 15 93841 781 46591425
Acute right ventricular failure 20.10 17.66 9 93847 175 46592031
Skin exfoliation 19.99 17.66 22 93834 32916 46559290
Urinary retention 19.92 17.66 14 93842 26047 46566159
Tubulointerstitial nephritis 19.85 17.66 3 93853 14785 46577421
Drug eruption 19.84 17.66 9 93847 21320 46570886
Emergency care examination 19.75 17.66 7 93849 71 46592135
Catheter site scab 19.73 17.66 9 93847 183 46592023
Muscle twitching 19.64 17.66 3 93853 14669 46577537
Carpal tunnel syndrome 19.58 17.66 4 93852 15855 46576351
Hypophagia 19.58 17.66 18 93838 29288 46562918
Wound 19.58 17.66 35 93821 42767 46549439
Intracardiac pressure increased 19.39 17.66 6 93850 38 46592168
Myelodysplastic syndrome 19.32 17.66 4 93852 15707 46576499
Head discomfort 19.27 17.66 55 93801 10296 46581910
Myocardial infarction 19.22 17.66 116 93740 97412 46494794
Balance disorder 19.14 17.66 66 93790 64455 46527751
Musculoskeletal disorder 19.03 17.66 4 93852 15541 46576665
Blood pressure fluctuation 18.85 17.66 20 93836 30428 46561778
Swelling face 18.83 17.66 176 93680 52883 46539323
Foot deformity 18.82 17.66 4 93852 15421 46576785
Dysentery 18.46 17.66 14 93842 751 46591455
Ventilation perfusion mismatch 18.41 17.66 9 93847 215 46591991
Gastritis hypertrophic 18.40 17.66 6 93850 46 46592160
International normalised ratio increased 18.32 17.66 42 93814 46841 46545365
Metapneumovirus infection 18.19 17.66 14 93842 768 46591438
Discomfort 18.08 17.66 42 93814 46628 46545578
Pyrexia 17.99 17.66 549 93307 348253 46243953
Atrial septal defect repair 17.92 17.66 9 93847 228 46591978
Orthostatic hypotension 17.88 17.66 14 93842 24644 46567562
Breast cancer metastatic 17.85 17.66 3 93853 13675 46578531
Hypertensive crisis 17.74 17.66 3 93853 13612 46578594

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
Dyspnoea 1177.77 23.86 1458 25388 331837 29593795
Fluid retention 886.79 23.86 437 26409 24561 29901071
Pulmonary arterial hypertension 731.35 23.86 285 26561 9016 29916616
Death 647.06 23.86 1145 25701 356138 29569494
Oedema 535.01 23.86 382 26464 42611 29883021
Nasal congestion 528.36 23.86 280 26566 18286 29907346
Pulmonary hypertension 518.98 23.86 279 26567 18757 29906875
Headache 500.59 23.86 709 26137 181597 29744035
Pain in jaw 458.91 23.86 222 26624 11934 29913698
Right ventricular failure 359.37 23.86 165 26681 7871 29917761
Peripheral swelling 340.91 23.86 342 26504 60732 29864900
Oedema peripheral 313.83 23.86 428 26418 105404 29820228
Flushing 241.95 23.86 205 26641 29287 29896345
Fluid overload 240.18 23.86 171 26675 18921 29906711
Unevaluable event 199.51 23.86 190 26656 31595 29894037
Lung transplant 195.06 23.86 71 26775 1845 29923787
Swelling 188.68 23.86 195 26651 35780 29889852
Toxicity to various agents 144.35 23.86 3 26843 177180 29748452
Dyspnoea exertional 143.97 23.86 168 26678 35262 29890370
Infusion site pain 142.69 23.86 62 26784 2588 29923044
Oxygen saturation decreased 141.09 23.86 184 26662 43256 29882376
Drug interaction 127.19 23.86 15 26831 199553 29726079
Dizziness 123.37 23.86 419 26427 194490 29731142
Weight increased 100.44 23.86 213 26633 74700 29850932
Catheter site erythema 98.75 23.86 38 26808 1156 29924476
Neutropenia 98.00 23.86 4 26842 128536 29797096
Pain in extremity 93.81 23.86 263 26583 109958 29815674
Catheterisation cardiac 90.97 23.86 43 26803 2188 29923444
Catheter management 90.05 23.86 33 26813 874 29924758
Device related infection 86.91 23.86 91 26755 16924 29908708
Syncope 76.56 23.86 207 26639 84696 29840936
Cardiac failure congestive 74.32 23.86 204 26642 84203 29841429
Malaise 74.17 23.86 321 26525 166641 29758991
Thrombocytopenia 70.47 23.86 18 26828 137026 29788606
Catheter site pruritus 70.12 23.86 21 26825 289 29925343
Hypoxia 69.88 23.86 141 26705 47713 29877919
Catheter site discharge 69.58 23.86 24 26822 530 29925102
Central venous catheterisation 66.17 23.86 27 26819 961 29924671
Myalgia 63.25 23.86 181 26665 76486 29849146
Cardiac failure 60.36 23.86 188 26658 83230 29842402
Respiratory failure 59.64 23.86 212 26634 100430 29825202
Drug abuse 55.20 23.86 5 26841 82067 29843565
Hospitalisation 53.62 23.86 121 26725 44198 29881434
Cough 53.01 23.86 238 26608 125404 29800228
Infusion site erythema 52.98 23.86 27 26819 1619 29924013
Acute kidney injury 52.52 23.86 104 26742 273738 29651894
Cor pulmonale 52.09 23.86 21 26825 724 29924908
Device alarm issue 51.21 23.86 21 26825 757 29924875
Pulmonary veno-occlusive disease 50.74 23.86 18 26828 433 29925199
Abdominal discomfort 50.14 23.86 125 26721 48666 29876966
Oxygen consumption increased 49.99 23.86 24 26822 1264 29924368
White blood cell count decreased 49.40 23.86 8 26838 83939 29841693
Transplant evaluation 47.94 23.86 18 26828 511 29925121
Acute respiratory failure 47.43 23.86 84 26762 25766 29899866
Liver transplant 46.94 23.86 30 26816 2772 29922860
Diarrhoea 45.59 23.86 478 26368 333625 29592007
Overdose 45.44 23.86 10 26836 84327 29841305
Rhabdomyolysis 45.21 23.86 3 26843 63577 29862055
Confusional state 45.16 23.86 33 26813 134801 29790831
Therapy non-responder 44.42 23.86 88 26758 29365 29896267
Palpitations 44.39 23.86 95 26751 33478 29892154
Product use in unapproved indication 43.40 23.86 7 26839 73686 29851946
Catheter site rash 42.56 23.86 13 26833 192 29925440
Therapy interrupted 42.34 23.86 34 26812 4495 29921137
Vascular device infection 42.31 23.86 24 26822 1785 29923847
Therapy change 41.40 23.86 27 26819 2582 29923050
Sinus congestion 41.09 23.86 34 26812 4688 29920944
Transfusion 40.06 23.86 41 26805 7420 29918212
Infusion site haemorrhage 39.14 23.86 15 26831 451 29925181
Hypertension 37.73 23.86 32 26814 121322 29804310
Pancytopenia 36.92 23.86 15 26831 85037 29840595
Plasma cell myeloma 36.64 23.86 3 26843 53459 29872173
Migraine 36.36 23.86 51 26795 12823 29912809
Ventilation perfusion mismatch 36.28 23.86 9 26837 57 29925575
Dermatitis contact 36.19 23.86 27 26819 3204 29922428
Infusion site infection 35.81 23.86 13 26833 335 29925297
Catheter site inflammation 35.72 23.86 12 26834 244 29925388
Exercise tolerance decreased 34.33 23.86 28 26818 3784 29921848
Drug ineffective 33.70 23.86 174 26672 340213 29585419
Platelet count decreased 32.96 23.86 28 26818 106101 29819531
Catheter site pain 32.87 23.86 17 26829 1051 29924581
Hypotension 32.65 23.86 298 26548 200267 29725365
Hyponatraemia 32.32 23.86 10 26836 67192 29858440
Chest pain 31.75 23.86 197 26649 117430 29808202
Device dislocation 31.37 23.86 30 26816 5001 29920631
Abdominal distension 31.17 23.86 101 26745 45608 29880024
Pyrexia 31.16 23.86 147 26699 294342 29631290
Paracentesis 30.73 23.86 12 26834 380 29925252
Faeces soft 30.66 23.86 21 26825 2178 29923454
Seizure 30.56 23.86 26 26820 98449 29827183
Neuropathy peripheral 29.66 23.86 13 26833 70462 29855170
Lung disorder 29.59 23.86 78 26768 31391 29894241
Pulmonary arterial pressure increased 29.52 23.86 16 26830 1088 29924544
Infusion site swelling 28.81 23.86 18 26828 1598 29924034
Liver function test abnormal 28.38 23.86 76 26770 30874 29894758
Epistaxis 28.30 23.86 108 26738 52873 29872759
Infusion site warmth 28.02 23.86 8 26838 92 29925540
Feeding tube user 28.00 23.86 7 26839 46 29925586
Pulmonary arterial pressure abnormal 27.36 23.86 9 26837 171 29925461
Fatigue 27.06 23.86 420 26426 320253 29605379
Infusion site vesicles 26.99 23.86 8 26838 106 29925526
Catheter site discolouration 26.47 23.86 6 26840 24 29925608
Infusion site discharge 26.27 23.86 7 26839 61 29925571
C-reactive protein increased 25.88 23.86 4 26842 43469 29882163
Acute myocardial infarction 25.24 23.86 8 26838 52931 29872701
Sickle cell anaemia with crisis 24.53 23.86 19 26827 2383 29923249
Dialysis 24.52 23.86 39 26807 10957 29914675
Scleroderma 24.21 23.86 15 26831 1312 29924320
Hallucination 24.13 23.86 7 26839 49052 29876580
Rheumatoid arthritis 24.05 23.86 4 26842 41193 29884439

Pharmacologic Action:

SourceCodeDescription
ATC C02KX02 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
OTHER ANTIHYPERTENSIVES
Antihypertensives for pulmonary arterial hypertension
ATC C02KX52 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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Pulmonary arterial hypertension indication 11399002
Body fluid retention contraindication 43498006
Chronic heart failure contraindication 48447003
Oligozoospermia contraindication 88311004
Pulmonary veno-occlusive disease contraindication 89420002 DOID:5453
Liver function tests abnormal contraindication 166603001
Edema contraindication 267038008
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.3 acidic
pKa2 2.68 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Endothelin-1 receptor GPCR ANTAGONIST Ki 9.65 WOMBAT-PK DRUG LABEL
Endothelin B receptor GPCR ANTAGONIST Ki 6.98 WOMBAT-PK

External reference:

IDSource
HW6NV07QEC UNII
4026238 VUID
N0000179774 NUI
D07077 KEGG_DRUG
4026238 VANDF
C1176329 UMLSCUI
CHEBI:135949 CHEBI
CHEMBL1111 ChEMBL_ID
DB06403 DRUGBANK_ID
6918493 PUBCHEM_CID
8128 INN_ID
C467894 MESH_SUPPLEMENTAL_RECORD_UI
3951 IUPHAR_LIGAND_ID
358274 RXNORM
111024 MMSL
23940 MMSL
313847 MMSL
d06841 MMSL
012216 NDDF
427735003 SNOMEDCT_US
428159003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 0378-4270 TABLET, FILM COATED 5 mg ORAL ANDA 29 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 0378-4271 TABLET, FILM COATED 10 mg ORAL ANDA 29 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 0591-2405 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 0591-2406 TABLET, FILM COATED 10 mg ORAL ANDA 27 sections
AMBRISENTAN HUMAN PRESCRIPTION DRUG LABEL 1 42794-051 TABLET, FILM COATED 5 mg ORAL ANDA 19 sections
AMBRISENTAN HUMAN PRESCRIPTION DRUG LABEL 1 42794-052 TABLET, FILM COATED 10 mg ORAL ANDA 19 sections
ambrisentan Human Prescription Drug Label 1 47335-236 TABLET, FILM COATED 5 mg ORAL ANDA 30 sections
ambrisentan Human Prescription Drug Label 1 47335-237 TABLET, FILM COATED 10 mg ORAL ANDA 30 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 49884-353 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 49884-354 TABLET, FILM COATED 10 mg ORAL ANDA 27 sections
Letairis HUMAN PRESCRIPTION DRUG LABEL 1 61958-0801 TABLET, FILM COATED 5 mg ORAL NDA 31 sections
Letairis HUMAN PRESCRIPTION DRUG LABEL 1 61958-0802 TABLET, FILM COATED 10 mg ORAL NDA 31 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 69097-386 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 69097-387 TABLET, FILM COATED 10 mg ORAL ANDA 27 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 70710-1179 TABLET, FILM COATED 5 mg ORAL ANDA 23 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 70710-1180 TABLET, FILM COATED 10 mg ORAL ANDA 23 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 70771-1363 TABLET, FILM COATED 5 mg ORAL ANDA 1 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 70771-1364 TABLET, FILM COATED 10 mg ORAL ANDA 1 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 76282-684 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Ambrisentan HUMAN PRESCRIPTION DRUG LABEL 1 76282-685 TABLET, FILM COATED 10 mg ORAL ANDA 27 sections