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

Stem definitionDrug idCAS RN
guanylate cyclase activators and stimulators 4807 625115-55-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • adempas
  • BAY 63-2521
  • riociguat
guanylate cyclase stimulator
  • Molecular weight: 422.42
  • Formula: C20H19FN8O2
  • CLOGP: 2.06
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 2
  • TPSA: 138.07
  • ALOGS: -3.79
  • ROTB: 5
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
4.50 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.44 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.74 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 9.10 hours Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

DateAgencyCompanyOrphan
Oct. 8, 2013 FDA BAYER HLTHCARE

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
Hospitalisation 1934.81 20.80 1138 60725 83943 63343216
Death 1408.12 20.80 1771 60092 372610 63054549
Dyspnoea 1174.54 20.80 2207 59656 659106 62768053
Fluid retention 1130.62 20.80 711 61152 58975 63368184
Hypotension 939.28 20.80 1237 60626 271367 63155792
Dyspnoea exertional 911.69 20.80 624 61239 59678 63367481
Pain in jaw 704.69 20.80 470 61393 43026 63384133
Pulmonary arterial hypertension 688.84 20.80 367 61496 22210 63404949
Headache 673.45 20.80 1723 60140 631518 62795641
Drug ineffective 637.37 20.80 125 61738 1044640 62382519
Dizziness 554.44 20.80 1262 60601 428663 62998496
Oedema peripheral 502.61 20.80 760 61103 188751 63238408
Oxygen saturation decreased 400.49 20.80 462 61401 88123 63339036
Dyspepsia 377.30 20.80 481 61382 101715 63325444
Pulmonary hypertension 356.63 20.80 293 61570 36830 63390329
Hypervolaemia 350.47 20.80 260 61603 28153 63399006
Right ventricular failure 345.72 20.80 213 61650 16975 63410184
Blood pressure decreased 315.66 20.80 352 61511 64670 63362489
Oedema 277.64 20.80 405 61458 97217 63329942
Diarrhoea 275.31 20.80 1397 60466 713969 62713190
Transfusion 264.60 20.80 172 61691 15045 63412114
Nasal congestion 262.87 20.80 322 61541 65338 63361821
Off label use 260.62 20.80 169 61694 674293 62752866
Nausea 258.39 20.80 1563 60300 852908 62574251
Infusion related reaction 223.55 20.80 3 61860 245518 63181641
Toxicity to various agents 209.59 20.80 7 61856 247243 63179916
Catheterisation cardiac 205.73 20.80 97 61766 4506 63422653
Chest pain 198.56 20.80 559 61304 215400 63211759
Maternal exposure during pregnancy 194.86 20.80 4 61859 220058 63207101
Epistaxis 194.16 20.80 293 61570 72432 63354727
Pulmonary arterial pressure increased 186.44 20.80 84 61779 3511 63423648
Rheumatoid arthritis 182.58 20.80 18 61845 253801 63173358
Drug hypersensitivity 182.33 20.80 40 61823 310647 63116512
Arthropathy 178.88 20.80 13 61850 234779 63192380
Palpitations 178.79 20.80 361 61502 112409 63314750
Treatment failure 178.73 20.80 3 61860 199040 63228119
Syncope 176.93 20.80 368 61495 117017 63310142
Dizziness postural 175.83 20.80 102 61761 7274 63419885
Contraindicated product administered 174.97 20.80 9 61854 217639 63209520
Cough 174.18 20.80 653 61210 292090 63135069
Alopecia 172.59 20.80 57 61806 337479 63089680
Abdominal distension 170.36 20.80 304 61559 86311 63340848
Infusion site pain 167.94 20.80 136 61727 16733 63410426
Rash 167.69 20.80 180 61683 560691 62866468
Catheter site erythema 166.55 20.80 82 61781 4194 63422965
Pulmonary endarterectomy 164.11 20.80 36 61827 107 63427052
Peripheral swelling 156.30 20.80 591 61272 265351 63161808
Oxygen therapy 156.16 20.80 64 61799 2114 63425045
Neutropenia 155.63 20.80 3 61860 175002 63252157
Therapy change 152.72 20.80 87 61776 5994 63421165
Catheter management 152.39 20.80 69 61794 2918 63424241
Drug interaction 146.06 20.80 24 61839 229107 63198052
Flushing 145.67 20.80 262 61601 74825 63352334
Haemoptysis 145.32 20.80 159 61704 28567 63398592
Lung transplant 143.13 20.80 67 61796 3061 63424098
Hepatic enzyme increased 138.75 20.80 17 61846 202311 63224848
Catheter site pruritus 134.19 20.80 57 61806 2063 63425096
Oxygen consumption increased 129.36 20.80 67 61796 3817 63423342
Unevaluable event 127.23 20.80 200 61663 51186 63375973
Exposure during pregnancy 123.21 20.80 7 61856 155540 63271619
Blood pressure systolic decreased 122.22 20.80 81 61782 7316 63419843
Gastrooesophageal reflux disease 121.52 20.80 280 61583 95359 63331800
Transplant evaluation 113.30 20.80 43 61820 1154 63426005
Pericarditis 110.47 20.80 4 61859 131575 63295584
Hypersensitivity 109.04 20.80 76 61787 292609 63134550
Hypoxia 106.34 20.80 201 61662 59591 63367568
Catheter site pain 106.33 20.80 63 61800 4672 63422487
Wound 102.02 20.80 18 61845 163245 63263914
Vomiting 100.87 20.80 907 60956 558710 62868449
Musculoskeletal stiffness 99.99 20.80 28 61835 184590 63242569
Endarterectomy 99.69 20.80 26 61837 188 63426971
Systemic lupus erythematosus 95.49 20.80 42 61821 208876 63218283
Presyncope 94.91 20.80 126 61737 27659 63399500
Product use in unapproved indication 93.62 20.80 29 61834 179051 63248108
Dyspnoea at rest 93.50 20.80 55 61808 4024 63423135
Feeling abnormal 93.05 20.80 337 61526 148055 63279104
Vascular device infection 92.56 20.80 68 61795 7244 63419915
Emergency care 92.43 20.80 36 61827 1038 63426121
Malaise 91.86 20.80 706 61157 415248 63011911
Product dose omission issue 90.98 20.80 460 61403 233853 63193306
Central venous catheterisation 84.17 20.80 44 61819 2555 63424604
Catheter site haemorrhage 83.99 20.80 47 61816 3128 63424031
Device related infection 82.87 20.80 108 61755 23284 63403875
Catheter site discharge 82.58 20.80 40 61823 1973 63425186
Therapeutic product effect incomplete 82.14 20.80 12 61851 125044 63302115
Catheter site swelling 81.16 20.80 36 61827 1449 63425710
Blood pressure diastolic decreased 80.69 20.80 105 61758 22601 63404558
Ascites 78.80 20.80 142 61721 40586 63386573
Pericardial effusion 78.59 20.80 120 61743 29938 63397221
Blood cholesterol increased 78.43 20.80 3 61860 94029 63333130
Blood pressure abnormal 78.38 20.80 85 61778 15113 63412046
Heart rate increased 76.88 20.80 234 61629 94004 63333155
Productive cough 75.83 20.80 181 61682 63027 63364132
Walking distance test abnormal 74.38 20.80 26 61837 548 63426611
Impaired healing 74.38 20.80 7 61856 102535 63324624
Cardiac failure 72.39 20.80 221 61642 88921 63338238
Hypertension 72.27 20.80 100 61763 279203 63147956
Drug intolerance 71.69 20.80 119 61744 308542 63118617
Thrombocytopenia 71.27 20.80 29 61834 151128 63276031
Device alarm issue 70.71 20.80 33 61830 1497 63425662
Pneumonia 70.57 20.80 717 61146 456050 62971109
Discomfort 69.86 20.80 38 61825 167336 63259823
Blister 69.69 20.80 20 61843 129794 63297365
Helicobacter infection 68.19 20.80 6 61857 92779 63334380
Decreased appetite 68.03 20.80 448 61415 250604 63176555
Pulmonary thrombosis 65.91 20.80 60 61803 8642 63418517
Rehabilitation therapy 65.32 20.80 32 61831 1618 63425541
Overdose 65.05 20.80 16 61847 115062 63312097
Chest discomfort 64.92 20.80 245 61618 109724 63317435
Pulmonary oedema 64.59 20.80 156 61707 54717 63372442
Catheter site rash 63.32 20.80 25 61838 748 63426411
Lower respiratory tract infection 63.00 20.80 25 61838 132282 63294877
Psoriasis 62.89 20.80 6 61857 86951 63340208
Blood potassium decreased 62.35 20.80 131 61732 41895 63385264
Medical procedure 61.33 20.80 20 61843 338 63426821
Angioplasty 61.18 20.80 29 61834 1363 63425796
Pruritus 60.11 20.80 168 61695 361285 63065874
Product use issue 60.04 20.80 76 61787 220444 63206715
Urticaria 59.15 20.80 45 61818 165757 63261402
Osteoarthritis 58.49 20.80 11 61852 95332 63331827
C-reactive protein increased 57.94 20.80 11 61852 94696 63332463
Infusion site infection 57.04 20.80 30 61833 1764 63425395
Infusion site erythema 56.21 20.80 63 61800 11616 63415543
Catheter site infection 56.19 20.80 43 61820 4871 63422288
Confusional state 55.91 20.80 90 61773 236290 63190869
Acute kidney injury 55.36 20.80 108 61755 263307 63163852
Localised oedema 54.88 20.80 44 61819 5334 63421825
Brain natriuretic peptide increased 53.94 20.80 43 61820 5170 63421989
Mineral supplementation 53.67 20.80 22 61841 727 63426432
Abdominal pain upper 53.25 20.80 364 61499 206080 63221079
Anaphylactic reaction 52.24 20.80 3 61860 66097 63361062
Device occlusion 52.20 20.80 49 61814 7338 63419821
Internal haemorrhage 52.16 20.80 42 61821 5123 63422036
Cardiac failure congestive 52.14 20.80 203 61660 92230 63334929
Diastolic hypotension 51.11 20.80 13 61850 84 63427075
Constipation 50.73 20.80 384 61479 224559 63202600
White blood cell count decreased 50.58 20.80 37 61826 139067 63288092
Hyponatraemia 50.30 20.80 23 61840 111877 63315282
Mobility decreased 48.41 20.80 29 61834 121130 63306029
Pain in extremity 47.62 20.80 513 61350 330973 63096186
Infection 46.39 20.80 96 61767 229077 63198082
Depressed level of consciousness 45.65 20.80 4 61859 62074 63365085
Injection site reaction 45.21 20.80 3 61860 58521 63368638
Catheter placement 45.13 20.80 28 61835 2256 63424903
Pancytopenia 45.03 20.80 19 61844 96914 63330245
Retching 44.84 20.80 63 61800 14582 63412577
Dialysis 44.72 20.80 53 61810 10374 63416785
Scleroderma 44.01 20.80 39 61824 5423 63421736
Irritable bowel syndrome 43.67 20.80 13 61850 82399 63344760
Pulmonary artery therapeutic procedure 42.90 20.80 9 61854 20 63427139
Acute respiratory failure 42.70 20.80 100 61763 34385 63392774
Haemoglobin decreased 42.67 20.80 265 61598 145220 63281939
Infusion site discharge 41.80 20.80 18 61845 674 63426485
Myalgia 41.79 20.80 265 61598 146264 63280895
Suicidal ideation 40.95 20.80 6 61857 62415 63364744
Device leakage 40.70 20.80 42 61821 7054 63420105
Dizziness exertional 40.52 20.80 15 61848 375 63426784
Lung disorder 39.48 20.80 142 61721 62119 63365040
Liver injury 39.28 20.80 6 61857 60514 63366645
Catheter site related reaction 39.25 20.80 19 61844 936 63426223
Flatulence 39.07 20.80 97 61766 34605 63392554
Asthma 39.00 20.80 40 61823 127521 63299638
Paracentesis 38.96 20.80 19 61844 951 63426208
Catheter site irritation 38.88 20.80 16 61847 534 63426625
Disease complication 38.72 20.80 29 61834 3180 63423979
General physical health deterioration 38.57 20.80 87 61776 201315 63225844
Depression 38.35 20.80 84 61779 196408 63230751
Blood pressure increased 38.02 20.80 62 61801 162000 63265159
Rales 37.96 20.80 54 61809 12643 63414516
Hypoaesthesia 37.15 20.80 67 61796 168326 63258833
Fibromyalgia 36.97 20.80 16 61847 80404 63346755
Joint swelling 36.85 20.80 179 61684 327487 63099672
Product supply issue 35.91 20.80 22 61841 1733 63425426
Therapeutic response decreased 35.86 20.80 8 61855 61517 63365642
Drug titration error 35.72 20.80 17 61846 806 63426353
Pain 35.69 20.80 508 61355 740120 62687039
Device infusion issue 35.33 20.80 23 61840 2015 63425144
Paraesthesia 35.03 20.80 62 61801 156904 63270255
Gout 34.71 20.80 53 61810 13218 63413941
Dermatitis contact 34.67 20.80 48 61815 10960 63416199
Injury 34.59 20.80 14 61849 73233 63353926
Arthralgia 34.49 20.80 372 61491 569338 62857821
Deep vein thrombosis 33.55 20.80 20 61843 83780 63343379
Fatigue 33.51 20.80 1115 60748 886913 62540246
Liver function test abnormal 33.11 20.80 4 61859 48177 63378982
Seizure 32.77 20.80 49 61814 132585 63294574
Coma 32.59 20.80 11 61852 64353 63362806
Device dislocation 32.32 20.80 75 61788 25630 63401529
Asthenia 32.30 20.80 539 61324 383065 63044094
Catheter site vesicles 32.23 20.80 12 61851 305 63426854
Ill-defined disorder 32.05 20.80 20 61843 81735 63345424
Renal disorder 31.82 20.80 87 61776 32887 63394272
Incorrect product administration duration 31.46 20.80 47 61816 11499 63415660
Head injury 31.29 20.80 77 61786 27319 63399840
Alanine aminotransferase increased 31.20 20.80 33 61830 103737 63323422
Intentional product use issue 30.87 20.80 48 61815 127844 63299315
Exercise tolerance decreased 30.56 20.80 32 61831 5465 63421694
Lung operation 30.17 20.80 11 61852 263 63426896
Abortion spontaneous 29.91 20.80 5 61858 47190 63379969
Loss of consciousness 29.66 20.80 207 61656 117914 63309245
Weight increased 29.63 20.80 386 61477 260406 63166753
Seasonal allergy 29.56 20.80 64 61799 20886 63406273
No adverse event 29.56 20.80 3 61860 41402 63385757
Choking 29.51 20.80 42 61821 9837 63417322
Cardiac operation 29.51 20.80 25 61838 3273 63423886
Generalised oedema 29.13 20.80 54 61809 15764 63411395
Gastrointestinal haemorrhage 29.10 20.80 156 61707 81020 63346139
Concomitant disease aggravated 29.10 20.80 40 61823 9072 63418087
Complication associated with device 28.84 20.80 56 61807 16922 63410237
Weight decreased 28.70 20.80 403 61460 276395 63150764
Osteoporosis 28.68 20.80 10 61853 57328 63369831
Hospice care 28.68 20.80 37 61826 7895 63419264
Medication error 28.15 20.80 8 61855 52276 63374883
Hepatitis 28.10 20.80 3 61860 39785 63387374
Nasal dryness 27.88 20.80 28 61835 4553 63422606
Pyrexia 26.93 20.80 311 61552 470167 62956992
Lactic acidosis 26.75 20.80 3 61860 38284 63388875
Delirium 26.72 20.80 8 61855 50533 63376626
Injection site erythema 26.67 20.80 25 61838 83149 63344010
Cerebrovascular accident 26.59 20.80 40 61823 107984 63319175
Product availability issue 26.59 20.80 26 61837 4095 63423064
Cardiac pacemaker insertion 26.56 20.80 26 61837 4100 63423059
Pulmonary pain 26.30 20.80 24 61839 3466 63423693
Cardiac failure acute 26.28 20.80 39 61824 9484 63417675
Knee arthroplasty 26.19 20.80 10 61853 54196 63372963
Biopsy liver 26.11 20.80 11 61852 390 63426769
Bradycardia 25.94 20.80 20 61843 73207 63353952
Sinusitis 25.94 20.80 123 61740 226530 63200629
Critical illness 25.78 20.80 9 61854 189 63426970
Arthritis 25.67 20.80 46 61817 115875 63311284
Clostridium difficile infection 25.04 20.80 75 61788 29847 63397312
Right ventricular dilatation 25.01 20.80 16 61847 1360 63425799
Vascular device occlusion 24.54 20.80 8 61855 135 63427024
Jugular vein distension 24.47 20.80 14 61849 972 63426187
Dry eye 24.37 20.80 5 61858 40756 63386403
Gastric disorder 24.35 20.80 86 61777 37283 63389876
Infusion site induration 24.20 20.80 15 61848 1207 63425952
Infusion site swelling 24.13 20.80 38 61825 9732 63417427
Wrong dose 23.96 20.80 15 61848 1228 63425931
Drug-induced liver injury 23.91 20.80 5 61858 40217 63386942
Catheter site extravasation 23.72 20.80 10 61853 355 63426804
Myocardial infarction 23.62 20.80 38 61825 99855 63327304
Hallucination 23.51 20.80 12 61851 54805 63372354
Device connection issue 23.51 20.80 12 61851 663 63426496
Product prescribing issue 23.21 20.80 20 61843 2679 63424480
Loss of personal independence in daily activities 23.01 20.80 37 61826 97253 63329906
Pulmonary veno-occlusive disease 22.81 20.80 14 61849 1107 63426052
Injection site pain 22.52 20.80 59 61804 129741 63297418
Pulmonary congestion 22.10 20.80 51 61812 17367 63409792
Blood iron decreased 21.96 20.80 46 61817 14675 63412484
Sinus congestion 21.83 20.80 52 61811 18071 63409088
Blood glucose increased 21.61 20.80 30 61833 83726 63343433
Hyperkalaemia 21.60 20.80 13 61850 54190 63372969
Influenza 21.40 20.80 180 61683 108542 63318617
Angioedema 21.33 20.80 10 61853 47955 63379204
Cardioversion 21.30 20.80 14 61849 1246 63425913
Ear discomfort 21.28 20.80 32 61831 7874 63419285
Infusion site cellulitis 21.24 20.80 8 61855 210 63426949
Pulmonary arterial wedge pressure increased 21.23 20.80 9 61854 324 63426835
Right ventricular dysfunction 20.98 20.80 16 61847 1803 63425356

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
Death 698.84 24.59 974 18631 397075 34540251
Hospitalisation 698.23 24.59 420 19185 56482 34880844
Fluid retention 477.01 24.59 253 19352 26634 34910692
Dyspnoea 390.77 24.59 728 18877 376054 34561272
Dyspnoea exertional 274.81 24.59 213 19392 43066 34894260
Hypotension 266.46 24.59 458 19147 221191 34716135
Pulmonary arterial hypertension 262.61 24.59 118 19487 8621 34928705
Pain in jaw 240.34 24.59 126 19479 12914 34924412
Pulmonary hypertension 224.21 24.59 142 19463 20782 34916544
Headache 223.26 24.59 401 19204 200234 34737092
Right ventricular failure 206.21 24.59 100 19505 8684 34928642
Oedema 179.58 24.59 171 19434 45570 34891756
Oedema peripheral 170.98 24.59 268 19337 119544 34817782
Peripheral swelling 170.24 24.59 212 19393 76329 34860997
Dizziness 166.33 24.59 373 19232 218148 34719178
Hypervolaemia 165.68 24.59 115 19490 19594 34917732
Pulmonary endarterectomy 151.25 24.59 28 19577 55 34937271
Oxygen saturation decreased 151.07 24.59 168 19437 53650 34883676
Dyspepsia 130.40 24.59 130 19475 36602 34900724
Drug ineffective 113.02 24.59 58 19547 456693 34480633
Nasal congestion 105.56 24.59 94 19511 22963 34914363
Drug interaction 84.45 24.59 13 19592 225933 34711393
Off label use 83.60 24.59 68 19537 419456 34517870
Endarterectomy 71.73 24.59 17 19588 148 34937178
Haemoptysis 68.33 24.59 91 19514 34915 34902411
Transfusion 67.24 24.59 48 19557 8537 34928789
Syncope 65.78 24.59 153 19452 91298 34846028
Catheter management 63.79 24.59 23 19582 942 34936384
Weight increased 62.96 24.59 152 19453 92881 34844445
Abdominal distension 62.23 24.59 115 19490 58377 34878949
Blood pressure decreased 62.14 24.59 107 19498 51408 34885918
Swelling 60.55 24.59 95 19510 42271 34895055
Oxygen consumption increased 59.45 24.59 24 19581 1342 34935984
Infusion site pain 59.16 24.59 33 19572 3818 34933508
Nausea 57.69 24.59 356 19249 339552 34597774
Lung transplant 56.57 24.59 26 19579 1998 34935328
Oxygen therapy 54.19 24.59 20 19585 876 34936450
Epistaxis 52.76 24.59 107 19498 58144 34879182
Blood pressure systolic decreased 51.81 24.59 32 19573 4471 34932855
Pulmonary arterial pressure increased 50.86 24.59 21 19584 1244 34936082
Pain in extremity 49.75 24.59 170 19435 126343 34810983
Thrombocytopenia 48.09 24.59 14 19591 156233 34781093
Infusion site erythema 47.74 24.59 24 19581 2249 34935077
Cough 47.48 24.59 188 19417 149952 34787374
Catheterisation cardiac 46.83 24.59 25 19580 2652 34934674
Blood pressure abnormal 45.15 24.59 37 19568 8069 34929257
Abdominal discomfort 45.07 24.59 102 19503 59733 34877593
Gastrooesophageal reflux disease 44.71 24.59 78 19527 37846 34899480
Gastrointestinal disorder 44.22 24.59 73 19532 33875 34903451
Diarrhoea 42.27 24.59 367 19238 389545 34547781
Drug abuse 41.12 24.59 4 19601 99092 34838234
Dizziness postural 40.48 24.59 31 19574 6133 34931193
Product use in unapproved indication 37.12 24.59 10 19595 117489 34819837
Unevaluable event 37.08 24.59 66 19539 32524 34904802
Transplant evaluation 37.01 24.59 13 19592 493 34936833
Thrombectomy 36.94 24.59 9 19596 89 34937237
Catheter site pain 36.80 24.59 17 19588 1321 34936005
Lung disorder 36.60 24.59 68 19537 34628 34902698
Surgery 35.93 24.59 42 19563 14115 34923211
Therapy change 35.74 24.59 22 19583 3055 34934271
Pulmonary thrombosis 35.48 24.59 31 19574 7376 34929950
Seizure 34.92 24.59 8 19597 104849 34832477
Dialysis 34.90 24.59 37 19568 11171 34926155
Angioplasty 34.72 24.59 15 19590 995 34936331
Blood pressure diastolic decreased 33.74 24.59 33 19572 9061 34928265
Dyspnoea at rest 33.70 24.59 23 19582 3805 34933521
Flushing 33.52 24.59 63 19542 32357 34904969
Malaise 33.52 24.59 198 19407 185627 34751699
Terminal state 33.13 24.59 23 19582 3911 34933415
Cardiac operation 33.03 24.59 21 19584 3086 34934240
Overdose 32.27 24.59 6 19599 91053 34846273
Pyrexia 32.04 24.59 89 19516 332924 34604402
Feeling abnormal 31.25 24.59 92 19513 63143 34874183
Acute kidney injury 29.71 24.59 81 19524 304907 34632419
Chest pain 29.58 24.59 145 19460 126617 34810709
Productive cough 27.95 24.59 64 19541 37749 34899577
Lung operation 27.50 24.59 7 19598 84 34937242
Infusion site discharge 26.18 24.59 7 19598 103 34937223
Chronic right ventricular failure 25.95 24.59 4 19601 0 34937326
Catheter site pruritus 25.93 24.59 9 19596 329 34936997
Concomitant disease aggravated 25.59 24.59 23 19582 5678 34931648
Drug hypersensitivity 25.15 24.59 7 19598 80522 34856804

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
Hospitalisation 2334.21 20.33 1310 72644 92926 79577508
Death 1921.91 20.33 2481 71473 564033 79106401
Fluid retention 1420.50 20.33 855 73099 68954 79601480
Dyspnoea 1354.81 20.33 2646 71308 854379 78816055
Dyspnoea exertional 1007.56 20.33 751 73203 86322 79584112
Hypotension 885.32 20.33 1513 72441 438804 79231630
Headache 848.89 20.33 1866 72088 651906 79018528
Pulmonary arterial hypertension 810.04 20.33 434 73520 27932 79642502
Pain in jaw 788.08 20.33 506 73448 45645 79624789
Dizziness 650.72 20.33 1475 72479 524966 79145468
Oedema peripheral 600.42 20.33 937 73017 251351 79419083
Drug ineffective 551.83 20.33 161 73793 1080752 78589682
Pulmonary hypertension 509.89 20.33 394 73560 47686 79622748
Right ventricular failure 490.70 20.33 293 73661 23204 79647230
Hypervolaemia 457.39 20.33 352 73602 42338 79628096
Oxygen saturation decreased 454.91 20.33 579 73375 128468 79541966
Dyspepsia 446.74 20.33 527 73427 108160 79562274
Oedema 409.59 20.33 529 73425 119051 79551383
Off label use 356.81 20.33 200 73754 907015 78763419
Toxicity to various agents 356.77 20.33 7 73947 421533 79248901
Blood pressure decreased 308.10 20.33 419 73535 99047 79571387
Transfusion 301.41 20.33 208 73746 21122 79649312
Peripheral swelling 297.30 20.33 724 73230 268893 79401541
Nasal congestion 292.78 20.33 358 73596 76194 79594240
Nausea 291.55 20.33 1692 72262 955504 78714930
Pulmonary endarterectomy 274.52 20.33 59 73895 165 79670269
Diarrhoea 269.55 20.33 1559 72395 878930 78791504
Drug interaction 269.36 20.33 34 73920 415149 79255285
Neutropenia 242.40 20.33 5 73949 287705 79382729
Catheterisation cardiac 228.74 20.33 110 73844 5618 79664816
Epistaxis 208.11 20.33 372 73582 111143 79559291
Abdominal distension 207.93 20.33 387 73567 119263 79551171
Chest pain 201.18 20.33 647 73307 281657 79388777
Syncope 200.88 20.33 485 73469 178964 79491470
Pulmonary arterial pressure increased 195.72 20.33 92 73862 4463 79665971
Infusion related reaction 193.91 20.33 4 73950 230233 79440201
Cough 191.52 20.33 759 73195 366030 79304404
Dizziness postural 188.04 20.33 123 73831 11426 79659008
Infusion site pain 181.12 20.33 130 73824 14046 79656388
Catheter management 176.17 20.33 80 73874 3583 79666851
Unevaluable event 171.77 20.33 234 73720 55351 79615083
Palpitations 170.23 20.33 368 73586 126242 79544192
Oxygen therapy 170.09 20.33 72 73882 2718 79667716
Lung transplant 162.41 20.33 81 73873 4480 79665954
Haemoptysis 155.55 20.33 224 73730 55775 79614659
Catheter site erythema 154.61 20.33 82 73872 5158 79665276
Oxygen consumption increased 152.83 20.33 80 73874 4899 79665535
Drug hypersensitivity 152.59 20.33 44 73910 298872 79371562
Product dose omission issue 147.85 20.33 535 73419 247002 79423432
Flushing 145.24 20.33 279 73675 87989 79582445
Therapy change 143.43 20.33 88 73866 7311 79663123
Treatment failure 143.38 20.33 3 73951 170483 79499951
Rheumatoid arthritis 140.20 20.33 15 73939 208455 79461979
Blood pressure systolic decreased 140.19 20.33 101 73853 10975 79659459
Gastrooesophageal reflux disease 138.96 20.33 302 73652 103944 79566490
Catheter site pruritus 135.94 20.33 58 73896 2233 79668201
Thrombocytopenia 133.63 20.33 40 73914 265219 79405215
Endarterectomy 130.63 20.33 36 73918 347 79670087
Blood pressure abnormal 130.35 20.33 116 73838 17053 79653381
Feeling abnormal 130.12 20.33 383 73571 158816 79511618
Product use in unapproved indication 129.34 20.33 36 73918 250323 79420111
Drug abuse 128.99 20.33 5 73949 162686 79507748
Transplant evaluation 124.52 20.33 50 73904 1647 79668787
Acute kidney injury 123.16 20.33 182 73772 519222 79151212
Rash 122.78 20.33 218 73736 578140 79092294
Catheter site pain 122.35 20.33 71 73883 5325 79665109
Arthropathy 118.43 20.33 13 73941 177098 79493336
Stomatitis 118.11 20.33 4 73950 146753 79523681
Overdose 117.10 20.33 16 73938 184190 79486244
Hepatic enzyme increased 115.76 20.33 16 73938 182594 79487840
Malaise 114.74 20.33 812 73142 489057 79181377
Contraindicated product administered 112.14 20.33 9 73945 157529 79512905
Emergency care 112.06 20.33 41 73913 1043 79669391
Maternal exposure during pregnancy 108.91 20.33 4 73950 136534 79533900
Blood pressure diastolic decreased 102.23 20.33 133 73821 30083 79640351
Vomiting 101.08 20.33 1001 72953 664827 79005607
Catheter site discharge 92.32 20.33 45 73909 2367 79668067
Pancytopenia 91.03 20.33 21 73933 165724 79504710
Fatigue 89.96 20.33 1282 72672 928445 78741989
Pain in extremity 86.83 20.33 607 73347 363931 79306503
Hypoxia 86.81 20.33 251 73703 102992 79567442
Blood potassium decreased 86.48 20.33 155 73799 46357 79624077
Medical procedure 85.16 20.33 25 73929 308 79670126
Productive cough 84.39 20.33 225 73729 88106 79582328
Dyspnoea at rest 84.31 20.33 63 73891 7239 79663195
Infusion site erythema 84.18 20.33 70 73884 9390 79661044
Pulmonary thrombosis 84.09 20.33 78 73876 12093 79658341
Therapeutic product effect incomplete 83.90 20.33 15 73939 141630 79528804
Pericarditis 83.31 20.33 3 73951 104233 79566201
Presyncope 83.06 20.33 142 73812 40912 79629522
Glossodynia 82.50 20.33 3 73951 103334 79567100
Hyponatraemia 82.24 20.33 31 73923 177817 79492617
Weight increased 82.07 20.33 488 73466 276898 79393536
Central venous catheterisation 81.88 20.33 46 73908 3243 79667191
Heart rate increased 81.58 20.33 272 73682 120452 79549982
Rehabilitation therapy 80.92 20.33 38 73916 1839 79668595
Confusional state 80.69 20.33 106 73848 317891 79352543
Walking distance test abnormal 80.34 20.33 29 73925 709 79669725
Hypertension 80.29 20.33 114 73840 330878 79339556
Alopecia 79.55 20.33 59 73895 231296 79439138
Vascular device infection 79.14 20.33 70 73884 10206 79660228
Catheter site haemorrhage 77.25 20.33 52 73902 5065 79665369
Musculoskeletal stiffness 76.85 20.33 33 73921 174975 79495459
C-reactive protein increased 75.70 20.33 14 73940 129013 79541421
Abdominal pain upper 75.57 20.33 408 73546 223411 79447023
Device related infection 75.23 20.33 123 73831 34171 79636263
Angioplasty 75.06 20.33 36 73918 1827 79668607
Exposure during pregnancy 74.18 20.33 5 73949 101127 79569307
Ascites 71.70 20.33 192 73762 75370 79595064
Device alarm issue 71.15 20.33 36 73918 2053 79668381
Electrocardiogram QT prolonged 70.88 20.33 3 73951 90383 79580051
Catheter site swelling 69.09 20.33 34 73920 1826 79668608
Dialysis 68.35 20.33 85 73869 18377 79652057
Hypersensitivity 67.97 20.33 86 73868 262153 79408281
White blood cell count decreased 67.37 20.33 46 73908 188242 79482192
Pyrexia 66.56 20.33 364 73590 678345 78992089
Cardiac failure congestive 66.45 20.33 285 73669 142117 79528317
Urticaria 65.26 20.33 46 73908 185155 79485279
Pericardial effusion 65.08 20.33 137 73817 46100 79624334
Blood cholesterol increased 64.92 20.33 3 73951 83717 79586717
Constipation 64.82 20.33 467 73487 282583 79387851
Suicide attempt 64.22 20.33 3 73951 82929 79587505
Lung disorder 64.03 20.33 192 73762 80365 79590069
Brain natriuretic peptide increased 63.36 20.33 58 73896 8842 79661592
Seizure 62.56 20.33 50 73904 188784 79481650
Chest discomfort 59.64 20.33 270 73684 137774 79532660
Psoriasis 58.80 20.33 7 73947 89580 79580854
Infusion site infection 58.64 20.33 30 73924 1751 79668683
Catheter site rash 58.17 20.33 25 73929 980 79669454
General physical health deterioration 58.03 20.33 104 73850 275134 79395300
Pneumonia 57.97 20.33 896 73058 659350 79011084
Depressed level of consciousness 57.75 20.33 10 73944 96642 79573792
Paracentesis 57.27 20.33 27 73927 1318 79669116
Localised oedema 56.96 20.33 52 73902 7900 79662534
Diastolic hypotension 56.83 20.33 16 73938 168 79670266
Mineral supplementation 55.64 20.33 23 73931 817 79669617
Abdominal discomfort 54.71 20.33 409 73545 250318 79420116
Delirium 54.60 20.33 7 73947 84620 79585814
Device occlusion 54.49 20.33 61 73893 11805 79658629
Hyperkalaemia 54.47 20.33 19 73935 114379 79556055
Pruritus 54.32 20.33 186 73768 394462 79275972
Bradycardia 54.24 20.33 29 73925 135528 79534906
Catheter placement 54.17 20.33 34 73920 2940 79667494
Coma 52.82 20.33 14 73940 100635 79569799
Lower respiratory tract infection 52.66 20.33 27 73927 129193 79541241
Suicidal ideation 52.57 20.33 5 73949 76335 79594099
Pulmonary artery therapeutic procedure 52.51 20.33 11 73943 26 79670408
Myocardial infarction 52.41 20.33 56 73898 184073 79486361
Decreased appetite 52.32 20.33 516 73438 341902 79328532
Catheter site infection 51.75 20.33 46 73908 6749 79663685
Flatulence 51.53 20.33 119 73835 42605 79627829
Lung operation 51.30 20.33 16 73938 245 79670189
Cardiac failure 50.70 20.33 280 73674 154562 79515872
Myalgia 50.67 20.33 320 73634 185321 79485113
Internal haemorrhage 50.47 20.33 51 73903 8782 79661652
Impaired healing 50.37 20.33 10 73944 87645 79582789
Alanine aminotransferase increased 50.23 20.33 46 73908 162524 79507910
Lactic acidosis 50.11 20.33 4 73950 70355 79600079
Metabolic acidosis 48.30 20.33 9 73945 82520 79587914
Blood pressure increased 48.10 20.33 76 73878 211284 79459150
Infusion site discharge 48.04 20.33 19 73935 601 79669833
Concomitant disease aggravated 47.75 20.33 60 73894 13107 79657327
Mobility decreased 47.63 20.33 27 73927 122148 79548286
Scleroderma 47.43 20.33 40 73914 5470 79664964
Deep vein thrombosis 46.74 20.33 27 73927 120892 79549542
Cardiac operation 46.50 20.33 38 73916 4974 79665460
Incorrect product administration duration 45.55 20.33 56 73898 11966 79658468
Pulmonary oedema 45.36 20.33 182 73772 88072 79582362
Terminal state 45.22 20.33 37 73917 4852 79665582
Cognitive disorder 44.59 20.33 6 73948 69920 79600514
Retching 44.34 20.33 67 73887 17400 79653034
Blister 44.33 20.33 28 73926 119448 79550986
Renal disorder 44.05 20.33 111 73843 41994 79628440
Drug intolerance 43.11 20.33 115 73839 264004 79406430
Gout 42.86 20.33 80 73874 24669 79645765
Catheter site related reaction 41.44 20.33 21 73933 1201 79669233
Type 2 diabetes mellitus 41.38 20.33 3 73951 57119 79613315
Product supply issue 41.34 20.33 25 73929 2023 79668411
Wound 40.72 20.33 29 73925 116150 79554284
Thrombectomy 40.60 20.33 14 73940 298 79670136
Hospice care 40.59 20.33 49 73905 10275 79660159
Loss of consciousness 40.09 20.33 280 73674 167663 79502771
Helicobacter infection 39.95 20.33 8 73946 69696 79600738
Acute myocardial infarction 39.89 20.33 11 73943 77025 79593409
Multiple organ dysfunction syndrome 39.61 20.33 32 73922 120214 79550220
Drug titration error 39.50 20.33 20 73934 1142 79669292
Catheter site vesicles 39.46 20.33 14 73940 325 79670109
Injection site reaction 39.33 20.33 3 73951 54782 79615652
Angioedema 39.10 20.33 11 73943 76024 79594410
Dizziness exertional 38.98 20.33 16 73938 558 79669876
Device dislocation 38.95 20.33 79 73875 25891 79644543
Agitation 38.92 20.33 22 73932 99693 79570741
Exercise tolerance decreased 38.89 20.33 45 73909 9026 79661408
Catheter site irritation 38.48 20.33 16 73938 577 79669857
Hyperglycaemia 38.42 20.33 9 73945 70326 79600108
Intentional product use issue 38.23 20.33 51 73903 152061 79518373
Hepatitis 37.46 20.33 4 73950 55723 79614711
Gastric disorder 37.41 20.33 97 73857 37336 79633098
Cardiac arrest 37.18 20.33 64 73890 172032 79498402
Drug-induced liver injury 37.04 20.33 8 73946 66109 79604325
Cholestasis 37.00 20.33 3 73951 52106 79618328
Nasal dryness 36.98 20.33 32 73922 4531 79665903
Coronary artery disease 36.52 20.33 8 73946 65466 79604968
Rales 36.34 20.33 66 73888 19935 79650499
Device infusion issue 35.98 20.33 24 73930 2302 79668132
Infection 35.94 20.33 110 73844 241602 79428832
Osteoarthritis 35.93 20.33 18 73936 87291 79583143
Liver function test abnormal 35.72 20.33 8 73946 64467 79605967
Acute respiratory failure 35.72 20.33 129 73825 59412 79611022
Infusion site swelling 35.54 20.33 40 73914 7786 79662648
Head injury 35.48 20.33 95 73859 37274 79633160
Aspartate aminotransferase increased 35.34 20.33 46 73908 138595 79531839
Cerebrovascular accident 35.17 20.33 56 73898 155236 79515198
Disease complication 34.80 20.33 32 73922 4905 79665529
Hallucination 34.80 20.33 18 73936 85727 79584707
Product availability issue 34.69 20.33 29 73925 3918 79666516
Muscle injury 33.92 20.33 3 73951 48558 79621876
Therapeutic response decreased 33.77 20.33 10 73944 66843 79603591
Diuretic therapy 33.62 20.33 11 73943 198 79670236
Seasonal allergy 33.51 20.33 57 73897 16349 79654085
Hypoglycaemia 33.50 20.33 27 73927 101567 79568867
Injury 33.39 20.33 15 73939 77481 79592953
Medication error 33.37 20.33 11 73943 68631 79601803
Abnormal weight gain 33.20 20.33 24 73930 2620 79667814
Surgery 32.84 20.33 85 73869 32681 79637753
Lymphocyte count decreased 32.82 20.33 3 73951 47286 79623148
Device leakage 32.46 20.33 45 73909 10811 79659623
Asthma 32.25 20.33 47 73907 135048 79535386
Cardio-respiratory arrest 32 20.33 32 73922 108478 79561956
Liver injury 31.41 20.33 7 73947 56607 79613827
Agranulocytosis 30.87 20.33 3 73951 45027 79625407
Jaundice 30.83 20.33 6 73948 53343 79617091
Product use issue 30.83 20.33 96 73858 209726 79460708
Multiple allergies 30.74 20.33 43 73911 10417 79660017
Discomfort 30.68 20.33 43 73911 125574 79544860
Hepatocellular injury 30.54 20.33 4 73950 47589 79622845
Interstitial lung disease 30.12 20.33 36 73918 112564 79557870
Disease recurrence 30.08 20.33 3 73951 44106 79626328
Systemic lupus erythematosus 30.06 20.33 41 73913 121108 79549326
Sinus disorder 29.81 20.33 65 73889 22399 79648035
Complication associated with device 29.61 20.33 56 73898 17440 79652994
Diabetes mellitus 29.59 20.33 18 73936 78372 79592062
Cardiac disorder 29.42 20.33 130 73824 65627 79604807
Blood iron decreased 29.41 20.33 52 73902 15382 79655052
Infusion site abscess 28.95 20.33 10 73944 214 79670220
Weight decreased 28.78 20.33 476 73478 354722 79315712
Choking 28.72 20.33 45 73909 12056 79658378
Sickle cell anaemia with crisis 28.57 20.33 36 73918 7886 79662548
Fibromyalgia 28.44 20.33 12 73942 64328 79606106
Intestinal obstruction 28.21 20.33 96 73858 42924 79627510
Product prescribing issue 28.09 20.33 26 73928 4019 79666415
Nasopharyngitis 27.99 20.33 359 73595 253522 79416912
Infusion site haemorrhage 27.97 20.33 25 73929 3695 79666739
Pulmonary veno-occlusive disease 27.92 20.33 18 73936 1630 79668804
Right ventricular dilatation 27.71 20.33 19 73935 1907 79668527
Asthenia 27.69 20.33 645 73309 511044 79159390
Transaminases increased 27.52 20.33 7 73947 51736 79618698
Drug eruption 27.47 20.33 4 73950 43931 79626503
Sickle cell anaemia 27.26 20.33 13 73941 651 79669783
Drug dependence 27.22 20.33 3 73951 40766 79629668
Paraesthesia 27.10 20.33 79 73875 176244 79494190
Device connection issue 27.02 20.33 15 73939 1033 79669401
COVID-19 26.98 20.33 67 73887 157607 79512827
Pulmonary arterial wedge pressure increased 26.94 20.33 12 73942 513 79669921
Myelosuppression 26.81 20.33 3 73951 40293 79630141
Emotional distress 26.53 20.33 3 73951 39966 79630468
Product prescribing error 25.98 20.33 5 73949 44808 79625626
Blood lactate dehydrogenase increased 25.85 20.33 3 73951 39167 79631267
Osteoporosis 25.73 20.33 9 73945 54103 79616331
Blood glucose increased 25.53 20.33 42 73912 114933 79555501
Atrial septal defect 25.41 20.33 18 73936 1904 79668530
Infusion site irritation 25.39 20.33 13 73941 760 79669674
Depression 25.38 20.33 109 73845 216681 79453753
Generalised oedema 25.32 20.33 63 73891 23646 79646788
Influenza 25.23 20.33 206 73748 129400 79541034
Mouth ulceration 25.19 20.33 3 73951 38391 79632043
Cardiac pacemaker insertion 25.15 20.33 29 73925 5793 79664641
Swelling 24.97 20.33 309 73645 216402 79454032
Sickle cell disease 24.71 20.33 8 73946 139 79670295
Cerebral infarction 24.64 20.33 6 73948 45670 79624764
Hepatic steatosis 24.64 20.33 3 73951 37735 79632699
Vascular device occlusion 24.55 20.33 10 73944 342 79670092
Abdominal cavity drainage 24.52 20.33 13 73941 817 79669617
Vascular resistance pulmonary decreased 24.32 20.33 7 73947 80 79670354
No adverse event 24.17 20.33 3 73951 37189 79633245
Pulmonary pain 24.06 20.33 25 73929 4448 79665986
Irritable bowel syndrome 23.90 20.33 14 73940 62227 79608207
Hypomagnesaemia 23.73 20.33 7 73947 46904 79623530
Nocturnal dyspnoea 23.30 20.33 16 73938 1610 79668824
Psychotic disorder 23.21 20.33 5 73949 41397 79629037
Choking sensation 23.14 20.33 23 73931 3883 79666551
Disseminated intravascular coagulation 23.03 20.33 3 73951 35839 79634595
Epilepsy 22.77 20.33 5 73949 40855 79629579
Cor pulmonale 22.75 20.33 18 73936 2250 79668184
Wrong dose 22.71 20.33 16 73938 1678 79668756
Hypokalaemia 22.52 20.33 64 73890 143976 79526458
Haemoglobin decreased 22.37 20.33 309 73645 221810 79448624
Encephalopathy 22.11 20.33 18 73936 67379 79603055
Dermatitis contact 22.10 20.33 38 73916 10995 79659439
Drug withdrawal syndrome 22.08 20.33 3 73951 34715 79635719
Drug dose titration not performed 22.00 20.33 12 73942 798 79669636
Catheter site extravasation 21.99 20.33 10 73944 449 79669985
Traumatic fracture 21.97 20.33 13 73941 1011 79669423
Ejection fraction decreased 21.96 20.33 3 73951 34574 79635860
Hernia repair 21.94 20.33 17 73937 2061 79668373
Ear discomfort 21.89 20.33 33 73921 8550 79661884
Cardioversion 21.80 20.33 17 73937 2081 79668353
Cardiac failure high output 21.74 20.33 9 73945 321 79670113
Skin exfoliation 21.72 20.33 12 73942 55088 79615346
Platelet count decreased 21.50 20.33 100 73854 194564 79475870
Gamma-glutamyltransferase increased 21.43 20.33 12 73942 54668 79615766
Intensive care 21.36 20.33 13 73941 1064 79669370
Intra-abdominal fluid collection 21.28 20.33 20 73934 3152 79667282
Hypoaesthesia 21.09 20.33 90 73864 179262 79491172
Dysarthria 21.04 20.33 19 73935 67603 79602831
Injection site infection 21.00 20.33 17 73937 2195 79668239
Prostate cancer 20.87 20.33 3 73951 33265 79637169
Infusion site induration 20.73 20.33 13 73941 1122 79669312
Haematuria 20.64 20.33 20 73934 68816 79601618
Prescribed overdose 20.39 20.33 5 73949 37878 79632556
Infusion site rash 20.35 20.33 15 73939 1687 79668747
Sinus congestion 20.34 20.33 52 73902 19844 79650590

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C02KX05 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
OTHER ANTIHYPERTENSIVES
Antihypertensives for pulmonary arterial hypertension
MeSH PA D020536 Enzyme Activators
FDA MoA N0000190484 Guanylate Cyclase Stimulators
FDA EPC N0000190485 Soluble Guanylate Cyclase Stimulator
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:76022 soluble guanylyl cyclase activators

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

DiseaseRelationSNOMED_IDDOID
Pulmonary arterial hypertension indication 11399002
Chronic thromboembolic pulmonary hypertension indication 233947005
Pregnancy, function contraindication 289908002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.68 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
0.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
1MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2.5MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 10662188 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PERSISTENT/RECURRENT CHRONIC THROMBOEMBOLIC PULMONARY HYPERTENSION (CTEPH), (WHO GROUP 4) AFTER SURGICAL TREATMENT, OR INOPERABLE CTEPH, TO IMPROVE EXERCISE CAPACITY AND WHO FUNCTIONAL CLASS
2MG ADEMPAS BAYER HLTHCARE N204819 Oct. 8, 2013 RX TABLET ORAL 11203593 Feb. 18, 2034 TREATMENT OF ADULTS WITH PULMONARY HYPERTENSION (PAH), (WHO GROUP 1), TO IMPROVE EXERCISE CAPACITY, WHO FUNCTIONAL CLASS AND TO DELAY CLINICAL WORSENING

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Guanylate cyclase soluble subunit beta-1 Enzyme POSITIVE ALLOSTERIC MODULATOR MEC 7.52 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
cAMP-specific 3',5'-cyclic phosphodiesterase 7B Enzyme IC50 5.54 SCIENTIFIC LITERATURE

External reference:

IDSource
D09572 KEGG_DRUG
4032785 VANDF
CHEBI:76018 CHEBI
CHEMBL2107834 ChEMBL_ID
C542595 MESH_SUPPLEMENTAL_RECORD_UI
5257 IUPHAR_LIGAND_ID
8857 INN_ID
DB08931 DRUGBANK_ID
RU3FE2Y4XI UNII
1439816 RXNORM
207043 MMSL
29792 MMSL
d08140 MMSL
015236 NDDF
713333001 SNOMEDCT_US
715490004 SNOMEDCT_US
C2717561 UMLSCUI
GZO PDB_CHEM_ID
11304743 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-250 TABLET, FILM COATED 0.50 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-250 TABLET, FILM COATED 0.50 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-250 TABLET, FILM COATED 0.50 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-251 TABLET, FILM COATED 1 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-251 TABLET, FILM COATED 1 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-251 TABLET, FILM COATED 1 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-252 TABLET, FILM COATED 1.50 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-252 TABLET, FILM COATED 1.50 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-252 TABLET, FILM COATED 1.50 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-253 TABLET, FILM COATED 2 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-253 TABLET, FILM COATED 2 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-253 TABLET, FILM COATED 2 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-254 TABLET, FILM COATED 2.50 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-254 TABLET, FILM COATED 2.50 mg ORAL NDA 29 sections
Adempas HUMAN PRESCRIPTION DRUG LABEL 1 50419-254 TABLET, FILM COATED 2.50 mg ORAL NDA 29 sections