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

Stem definitionDrug idCAS RN
enzymes 5141 105857-23-6

Description:

MoleculeDescription

Synonyms:

  • alteplase
  • activase
  • alteplase (genetical recombination)
A proteolytic enzyme in the serine protease family found in many tissues which converts PLASMINOGEN to FIBRINOLYSIN. It has fibrin-binding activity and is immunologically different from UROKINASE-TYPE PLASMINOGEN ACTIVATOR. The primary sequence, composed of 527 amino acids, is identical in both the naturally occurring and synthetic proteases. Is currently clinical tested as treatment for COVID-19 patients.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
0.10 g P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 18, 1996 FDA GENENTECH

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
Haemorrhagic transformation stroke 908.35 24.72 157 8025 952 50595990
Angioedema 771.76 24.72 272 7910 37404 50559538
Cerebral haemorrhage 769.55 24.72 250 7932 26802 50570140
Haemorrhage intracranial 629.34 24.72 179 8003 12195 50584747
Death 278.68 24.72 300 7882 325079 50271863
Haemorrhage 202.49 24.72 119 8063 53322 50543620
No adverse event 162.98 24.72 88 8094 33490 50563452
Cerebral haematoma 130.06 24.72 39 8143 3172 50593770
Swollen tongue 127.75 24.72 71 8111 28559 50568383
Neurological decompensation 124.96 24.72 35 8147 2235 50594707
Subarachnoid haemorrhage 119.73 24.72 50 8132 10726 50586216
Cerebral infarction 111.46 24.72 59 8123 21545 50575397
NIH stroke scale score increased 108.23 24.72 14 8168 0 50596942
Intraventricular haemorrhage 103.69 24.72 29 8153 1841 50595101
Brain herniation 97.50 24.72 31 8151 3061 50593881
Thrombolysis 89.27 24.72 15 8167 74 50596868
Aplastic anaemia 83.07 24.72 35 8147 7668 50589274
Hemiparesis 82.04 24.72 47 8135 20001 50576941
Intracranial mass 78.97 24.72 21 8161 1102 50595840
Brain oedema 75.97 24.72 38 8144 12332 50584610
Stroke in evolution 67.34 24.72 11 8171 44 50596898
Haemorrhagic cerebral infarction 65.38 24.72 16 8166 600 50596342
NIH stroke scale abnormal 59.30 24.72 8 8174 3 50596939
Brain stem haemorrhage 57.81 24.72 15 8167 715 50596227
Aphasia 57.74 24.72 43 8139 28451 50568491
Tongue oedema 57.14 24.72 22 8160 3817 50593125
Product quality issue 56.87 24.72 44 8138 30814 50566128
Cardiogenic shock 51.88 24.72 32 8150 15567 50581375
Cerebral mass effect 51.35 24.72 14 8168 808 50596134
Haemorrhagic infarction 50.08 24.72 11 8171 254 50596688
Respiratory failure 49.35 24.72 67 8115 91114 50505828
Ventricular extrasystoles 46.65 24.72 26 8156 10490 50586452
Haematoma 46.64 24.72 39 8143 30471 50566471
Reperfusion arrhythmia 45.61 24.72 10 8172 229 50596713
Lip swelling 44.98 24.72 35 8147 24701 50572241
Cerebral hyperperfusion syndrome 44.67 24.72 7 8175 20 50596922
Ischaemic stroke 43.80 24.72 29 8153 15919 50581023
Hypotension 41.93 24.72 107 8075 235362 50361580
Diarrhoea 37.04 24.72 25 8157 588451 50008491
Coma 35.73 24.72 45 8137 56834 50540108
Hemiplegia 34.80 24.72 19 8163 7362 50589580
Intra-abdominal haemorrhage 34.03 24.72 13 8169 2207 50594735
Arthralgia 32.82 24.72 15 8167 438687 50158255
Ventricular tachycardia 32.32 24.72 24 8158 15797 50581145
Cardiac tamponade 32.01 24.72 15 8167 4217 50592725
Chest pain 31.05 24.72 80 8102 176802 50420140
Anaphylactic reaction 29.64 24.72 40 8142 54015 50542927
Procedural haemorrhage 29.62 24.72 12 8170 2378 50594564
Reocclusion 28.68 24.72 4 8178 3 50596939
Bradycardia 28.45 24.72 43 8139 64383 50532559
Haemothorax 28.31 24.72 11 8171 1955 50594987
Extravasation 28.12 24.72 11 8171 1991 50594951
Cardiac arrest 27.68 24.72 49 8133 83602 50513340
Blood fibrinogen decreased 26.76 24.72 8 8174 643 50596299
Haemorrhagic stroke 26.16 24.72 14 8168 5214 50591728
Reperfusion injury 26.15 24.72 5 8177 56 50596886
Myocardial rupture 26.07 24.72 5 8177 57 50596885
Macular hole 25.71 24.72 8 8174 735 50596207

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
Haemorrhagic transformation stroke 1163.06 20.00 224 10284 1082 29562937
Haemorrhage intracranial 654.45 20.00 231 10277 14311 29549708
Cerebral haemorrhage 591.67 20.00 266 10242 31160 29532859
Angioedema 463.80 20.00 226 10282 31689 29532330
Ventricular extrasystoles 215.96 20.00 95 10413 10487 29553532
Haemorrhage 204.70 20.00 151 10357 44921 29519098
Haemorrhagic infarction 177.38 20.00 39 10469 391 29563628
Death 154.09 20.00 359 10149 341725 29222294
No adverse event 146.54 20.00 86 10422 17392 29546627
Neurological decompensation 137.24 20.00 46 10462 2416 29561603
Ventricular tachycardia 131.11 20.00 88 10420 22486 29541533
NIH stroke scale score increased 119.08 20.00 18 10490 7 29564012
Chest pain 108.81 20.00 164 10344 111809 29452210
Cerebral infarction 108.11 20.00 81 10427 24594 29539425
Intraventricular haemorrhage 107.38 20.00 40 10468 2866 29561153
Brain oedema 104.69 20.00 61 10447 12159 29551860
Haematoma 92.45 20.00 72 10436 23140 29540879
Cerebral haematoma 88.98 20.00 39 10469 4257 29559762
Aplastic anaemia 87.73 20.00 46 10462 7464 29556555
Subarachnoid haemorrhage 84.65 20.00 49 10459 9643 29554376
Hemiparesis 82.94 20.00 56 10452 14430 29549589
Reperfusion arrhythmia 81.28 20.00 15 10493 54 29563965
Haemorrhagic stroke 74.53 20.00 38 10470 5818 29558201
Ischaemic stroke 68.95 20.00 52 10456 15925 29548094
Thrombolysis 66.19 20.00 13 10495 70 29563949
Swollen tongue 64.49 20.00 45 10463 12221 29551798
Extrasystoles 63.82 20.00 29 10479 3445 29560574
Cerebral mass effect 63.48 20.00 20 10488 861 29563158
Brain herniation 62.58 20.00 29 10479 3604 29560415
Haemorrhagic cerebral infarction 62.53 20.00 19 10489 724 29563295
Stroke in evolution 58.46 20.00 10 10498 20 29563999
Bradycardia 52.39 20.00 88 10420 65541 29498478
Tongue oedema 52.18 20.00 23 10485 2543 29561476
Aphasia 50.61 20.00 47 10461 19151 29544868
Hypotension 48.22 20.00 165 10343 194189 29369830
Cerebral hyperperfusion syndrome 47.83 20.00 10 10498 77 29563942
Electrocardiogram ST segment elevation 45.41 20.00 25 10483 4467 29559552
Diarrhoea 44.75 20.00 32 10476 332666 29231353
Gingival bleeding 44.39 20.00 28 10480 6425 29557594
Ventricular fibrillation 44.14 20.00 40 10468 15793 29548226
Intentional product use issue 42.20 20.00 63 10445 42435 29521584
Toxicity to various agents 41.87 20.00 6 10502 173655 29390364
Hemiplegia 41.37 20.00 27 10481 6567 29557452
Basal ganglia haemorrhage 40.92 20.00 14 10494 782 29563237
Cardiac arrest 40.44 20.00 92 10416 85499 29478520
Cerebral artery occlusion 38.73 20.00 13 10495 685 29563334
Brain stem haemorrhage 35.92 20.00 13 10495 857 29563162
Reocclusion 33.10 20.00 6 10502 19 29564000
Paresis 32.55 20.00 15 10493 1839 29562180
Aortic dissection 31.88 20.00 16 10492 2368 29561651
Blood fibrinogen decreased 31.60 20.00 12 10496 906 29563113
Intracranial pressure increased 31.43 20.00 18 10490 3467 29560552
Haemothorax 29.01 20.00 17 10491 3419 29560600
Catheter site haemorrhage 28.13 20.00 14 10494 2034 29561985
Product closure issue 27.77 20.00 4 10504 0 29564019
Malaise 27.77 20.00 11 10497 159591 29404428
Extravasation 27.72 20.00 13 10495 1659 29562360
Rhythm idioventricular 27.14 20.00 8 10500 274 29563745
Tongue haemorrhage 26.58 20.00 9 10499 487 29563532
Lip swelling 26.36 20.00 27 10481 12383 29551636
Epistaxis 25.98 20.00 57 10451 51647 29512372
Cardiogenic shock 25.89 20.00 33 10475 19157 29544862
Product quality issue 25.78 20.00 30 10478 15865 29548154
Parotid gland haemorrhage 25.77 20.00 5 10503 25 29563994
Reperfusion injury 25.71 20.00 6 10502 80 29563939
Fatigue 25.62 20.00 46 10462 316775 29247244
Cerebral ischaemia 25.57 20.00 19 10489 5684 29558335
Cardiac ventricular thrombosis 24.34 20.00 10 10498 929 29563090
Fall 23.80 20.00 17 10491 177161 29386858
Hydrocephalus 23.03 20.00 16 10492 4311 29559708
Coma 22.73 20.00 46 10462 39404 29524615
Arrhythmia 22.35 20.00 40 10468 31273 29532746
Myocardial rupture 21.65 20.00 6 10502 164 29563855
Mouth haemorrhage 21.60 20.00 16 10492 4764 29559255
Weight decreased 20.89 20.00 14 10494 150891 29413128
Injection site oedema 20.87 20.00 6 10502 188 29563831
Pericardial haemorrhage 20.87 20.00 13 10495 2918 29561101
Factor I deficiency 20.83 20.00 3 10505 0 29564019
Hyperhidrosis 20.71 20.00 60 10448 64480 29499539
Hemianopia 20.56 20.00 8 10500 645 29563374
Shock 20.19 20.00 31 10477 21373 29542646

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
Haemorrhagic transformation stroke 1915.48 21.22 353 15273 2036 64481070
Cerebral haemorrhage 1243.82 21.22 466 15160 50624 64432482
Haemorrhage intracranial 1083.10 21.22 347 15279 23537 64459569
Angioedema 1061.31 21.22 438 15188 61383 64421723
Haemorrhage 295.79 21.22 203 15423 79148 64403958
Cerebral haematoma 275.01 21.22 92 15534 7093 64476013
Neurological decompensation 257.47 21.22 78 15548 4358 64478748
Death 236.92 21.22 420 15206 482285 64000821
No adverse event 229.71 21.22 120 15506 28441 64454665
Cerebral infarction 227.57 21.22 135 15491 40909 64442197
NIH stroke scale score increased 225.76 21.22 32 15594 10 64483096
Subarachnoid haemorrhage 203.23 21.22 96 15530 18342 64464764
Intraventricular haemorrhage 178.26 21.22 58 15568 4095 64479011
Brain oedema 178.19 21.22 93 15533 21982 64461124
Aplastic anaemia 167.42 21.22 77 15549 13843 64469263
Brain herniation 163.45 21.22 61 15565 6472 64476634
Haemorrhagic cerebral infarction 163.43 21.22 42 15584 1272 64481834
Swollen tongue 158.10 21.22 101 15525 34853 64448253
Hemiparesis 152.07 21.22 93 15533 29734 64453372
Thrombolysis 152.01 21.22 28 15598 159 64482947
Haemorrhagic infarction 135.66 21.22 32 15594 673 64482433
Cerebral mass effect 134.26 21.22 38 15588 1668 64481438
Haematoma 123.80 21.22 97 15529 46153 64436953
Stroke in evolution 115.38 21.22 20 15606 75 64483031
Aphasia 105.62 21.22 84 15542 40822 64442284
Ventricular extrasystoles 100.60 21.22 59 15567 17470 64465636
Intracranial mass 93.66 21.22 30 15596 2013 64481093
Haemorrhagic stroke 92.11 21.22 46 15580 9905 64473201
Cerebral hyperperfusion syndrome 91.63 21.22 17 15609 101 64483005
Ventricular tachycardia 87.67 21.22 70 15556 34195 64448911
Tongue oedema 87.57 21.22 38 15588 5952 64477154
Brain stem haemorrhage 84.56 21.22 26 15600 1525 64481581
NIH stroke scale abnormal 75.80 21.22 11 15615 6 64483100
Product quality issue 74.36 21.22 60 15566 29739 64453367
Ischaemic stroke 73.60 21.22 59 15567 28976 64454130
Hemiplegia 70.70 21.22 42 15584 12726 64470380
Diarrhoea 69.50 21.22 45 15581 722659 63760447
Reperfusion arrhythmia 65.43 21.22 15 15611 277 64482829
Aortic dissection 64.22 21.22 26 15600 3426 64479680
Cardiogenic shock 63.89 21.22 57 15569 32370 64450736
Toxicity to various agents 63.55 21.22 7 15619 363506 64119600
Cardiac arrest 62.44 21.22 124 15502 153940 64329166
Lip swelling 60.72 21.22 55 15571 31852 64451254
Haemothorax 58.87 21.22 27 15599 4815 64478291
Basal ganglia haemorrhage 57.76 21.22 19 15607 1387 64481719
Fatigue 55.49 21.22 60 15566 748670 63734436
Respiratory failure 55.11 21.22 121 15505 161062 64322044
Arthralgia 50.55 21.22 22 15604 442238 64040868
Hydrocephalus 50.10 21.22 28 15598 7563 64475543
Reperfusion injury 49.23 21.22 11 15615 180 64482926
Intentional product use issue 48.95 21.22 85 15541 95279 64387827
Cerebral artery occlusion 47.56 21.22 17 15609 1594 64481512
Hypotension 47.33 21.22 200 15426 380774 64102332
Intracranial pressure increased 46.73 21.22 26 15600 6963 64476143
Coma 46.16 21.22 79 15547 87536 64395570
Cardiac tamponade 45.57 21.22 27 15599 8137 64474969
Intra-abdominal haemorrhage 44.42 21.22 21 15605 4010 64479096
Malaise 43.26 21.22 21 15605 396226 64086880
Blood fibrinogen decreased 41.59 21.22 15 15611 1443 64481663
Product closure issue 40.89 21.22 6 15620 4 64483102
Fall 39.89 21.22 26 15600 416800 64066306
Anaphylactic reaction 38.94 21.22 64 15562 68600 64414506
Epistaxis 38.54 21.22 78 15548 98053 64385053
Pericardial haemorrhage 37.92 21.22 19 15607 4117 64478989
Pulseless electrical activity 36.85 21.22 28 15598 12711 64470395
Tongue haemorrhage 36.81 21.22 12 15614 851 64482255
Myocardial rupture 36.48 21.22 9 15617 230 64482876
Extravasation 36.38 21.22 17 15609 3163 64479943
Nasopharyngitis 36.28 21.22 3 15623 196070 64287036
Mouth haemorrhage 36.20 21.22 25 15601 9794 64473312
Catheter site haemorrhage 36.05 21.22 19 15607 4572 64478534
Gingival bleeding 35.14 21.22 29 15597 14825 64468281
Hemianopia 33.55 21.22 13 15613 1526 64481580
Weight decreased 32.95 21.22 14 15612 285725 64197381
Cerebral artery embolism 32.95 21.22 13 15613 1601 64481505
Shock 32.31 21.22 43 15583 38197 64444909
Heparin-induced thrombocytopenia 32.23 21.22 22 15604 8457 64474649
Bradycardia 31.94 21.22 81 15545 118138 64364968
Paresis 31.72 21.22 16 15610 3516 64479590
Procedural haemorrhage 31.70 21.22 17 15609 4235 64478871
Embolism 31.29 21.22 25 15601 12210 64470896
Vitreous haemorrhage 30.74 21.22 15 15611 3070 64480036
Macular hole 30.48 21.22 10 15616 724 64482382
Brain death 29.57 21.22 17 15609 4844 64478262
Drug intolerance 29.55 21.22 5 15621 187987 64295119
Embolic stroke 29.35 21.22 19 15607 6692 64476414
Completed suicide 29.25 21.22 9 15617 224405 64258701
Cytokine release syndrome 28.54 21.22 30 15596 20799 64462307
Hypofibrinogenaemia 28.36 21.22 12 15614 1766 64481340
Myalgia 27.82 21.22 3 15623 158614 64324492
Parotid gland haemorrhage 27.51 21.22 5 15621 26 64483080
Coagulopathy 27.13 21.22 36 15590 31884 64451222
Chest pain 27.02 21.22 121 15505 235859 64247247
Carotid artery occlusion 27.01 21.22 15 15611 4002 64479104
Cerebral artery thrombosis 26.89 21.22 10 15616 1049 64482057
Cerebellar haemorrhage 26.81 21.22 13 15613 2624 64480482
Lip oedema 25.96 21.22 16 15610 5173 64477933
Electrocardiogram ST segment elevation 25.63 21.22 18 15608 7241 64475865
Monoparesis 25.50 21.22 13 15613 2921 64480185
Intracardiac thrombus 25.10 21.22 14 15612 3767 64479339
Retroperitoneal haematoma 24.79 21.22 15 15611 4696 64478410
Extrasystoles 24.66 21.22 17 15609 6641 64476465
Depression 24.52 21.22 7 15619 183284 64299822
Pruritus 24.21 21.22 24 15602 312376 64170730
Cardiac ventricular thrombosis 24.04 21.22 10 15616 1410 64481696
Reocclusion 23.76 21.22 4 15622 12 64483094
Facial paralysis 23.67 21.22 26 15600 18940 64464166
Pain 23.67 21.22 63 15563 553448 63929658
Compartment syndrome 23.63 21.22 14 15612 4218 64478888
Cerebral artery stenosis 23.48 21.22 8 15618 651 64482455
Product dose omission issue 23.32 21.22 9 15617 194738 64288368
Peripheral artery occlusion 23.14 21.22 11 15615 2127 64480979
Rash 22.94 21.22 48 15578 458501 64024605
Cerebral ischaemia 22.63 21.22 19 15607 9943 64473163
Thyroid haemorrhage 22.60 21.22 5 15621 78 64483028
Abdominal discomfort 22.54 21.22 8 15618 182314 64300792
Quadriplegia 22.33 21.22 12 15614 3001 64480105
Insomnia 22.30 21.22 10 15616 197826 64285280
Weight increased 22.21 21.22 12 15614 213336 64269770
Paralysis 22.08 21.22 20 15606 11575 64471531
Endotracheal intubation 22.05 21.22 13 15613 3882 64479224
Factor I deficiency 21.98 21.22 3 15623 0 64483106
Ventricular fibrillation 21.97 21.22 28 15598 23832 64459274
Dysarthria 21.87 21.22 46 15580 59360 64423746
Cerebral reperfusion injury 21.82 21.22 4 15622 22 64483084
Stridor 21.81 21.22 14 15612 4860 64478246
Decreased appetite 21.34 21.22 22 15604 281267 64201839
Asthenia 21.24 21.22 45 15581 427999 64055107

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AD02 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Enzymes
ATC S01XA13 SENSORY ORGANS
OPHTHALMOLOGICALS
OTHER OPHTHALMOLOGICALS
Other ophthalmologicals
MeSH PA D002317 Cardiovascular Agents
MeSH PA D005343 Fibrinolytic Agents
MeSH PA D006401 Hematologic Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acute myocardial infarction indication 57054005 DOID:9408
Pulmonary embolism indication 59282003 DOID:9477
Ischemic stroke indication 422504002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Plasminogen Enzyme ACTIVATOR DRUG LABEL DRUG LABEL

External reference:

IDSource
1RXS4UE564 UNII
4019319 VANDF
4019599 VANDF
C0032143 UMLSCUI
CHEMBL1201593 ChEMBL_ID
D02837 KEGG_DRUG
DB00009 DRUGBANK_ID
5975 INN_ID
204210 RXNORM
4155 MMSL
970 MMSL
d00521 MMSL
108997009 SNOMEDCT_US
27638005 SNOMEDCT_US
37411004 SNOMEDCT_US
387152000 SNOMEDCT_US
D010959 MESH_DESCRIPTOR_UI
002074 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cathflo Activase HUMAN PRESCRIPTION DRUG LABEL 1 50242-041 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2.20 mg INTRAVENOUS BLA 21 sections