alteplase 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 838.53 25.16 148 7458 1022 46677434
Angioedema 702.25 25.16 257 7349 39085 46639371
Cerebral haemorrhage 688.49 25.16 233 7373 28138 46650318
Haemorrhage intracranial 591.97 25.16 172 7434 12552 46665904
Death 237.12 25.16 281 7325 335267 46343189
Haemorrhage 188.45 25.16 115 7491 54754 46623702
Swollen tongue 125.89 25.16 71 7535 29161 46649295
Neurological decompensation 122.37 25.16 33 7573 1815 46676641
Cerebral infarction 117.84 25.16 63 7543 23303 46655153
Cerebral haematoma 107.21 25.16 34 7572 3305 46675151
No adverse event 102.91 25.16 66 7540 34165 46644291
NIH stroke scale score increased 100.40 25.16 13 7593 0 46678456
Ischaemic stroke 89.71 25.16 47 7559 16675 46661781
Brain herniation 85.68 25.16 28 7578 2995 46675461
Subarachnoid haemorrhage 85.58 25.16 40 7566 11113 46667343
Intraventricular haemorrhage 85.07 25.16 25 7581 1880 46676576
Hemiparesis 81.67 25.16 47 7559 20022 46658434
Thrombolysis 77.63 25.16 13 7593 62 46678394
Intracranial mass 77.42 25.16 21 7585 1180 46677276
Brain oedema 66.71 25.16 35 7571 12443 46666013
Reperfusion arrhythmia 60.37 25.16 10 7596 44 46678412
Haemorrhagic cerebral infarction 55.47 25.16 14 7592 592 46677864
Aphasia 55.14 25.16 42 7564 28525 46649931
Stroke in evolution 54.08 25.16 9 7597 41 46678415
Tongue oedema 52.58 25.16 21 7585 3985 46674471
Aplastic anaemia 49.80 25.16 24 7582 7129 46671327
Product quality issue 48.99 25.16 43 7563 35605 46642851
Cardiogenic shock 45.30 25.16 30 7576 16354 46662102
Ventricular extrasystoles 45.24 25.16 26 7580 11037 46667419
Cerebral hyperperfusion syndrome 44.61 25.16 7 7599 20 46678436
Brain stem haemorrhage 43.61 25.16 12 7594 711 46677745
Lip swelling 41.81 25.16 34 7572 25361 46653095
Respiratory failure 39.75 25.16 62 7544 94754 46583702
Haematoma 38.96 25.16 36 7570 31836 46646620
Hypotension 38.17 25.16 103 7503 232486 46445970
Diarrhoea 36.80 25.16 23 7583 559579 46118877
NIH stroke scale abnormal 36.26 25.16 5 7601 3 46678453
Intra-abdominal haemorrhage 33.33 25.16 13 7593 2317 46676139
Hemiplegia 32.97 25.16 18 7588 6920 46671536
Haemorrhagic infarction 32.94 25.16 8 7598 288 46678168
Cardiac tamponade 31.17 25.16 15 7591 4439 46674017
Ventricular tachycardia 30.67 25.16 24 7582 16943 46661513
Cerebrovascular accident 30.37 25.16 57 7549 100982 46577474
Chest pain 29.81 25.16 79 7527 176245 46502211
Procedural haemorrhage 29.56 25.16 12 7594 2374 46676082
Reocclusion 28.65 25.16 4 7602 3 46678453
Coma 28.50 25.16 41 7565 58308 46620148
Anaphylactic reaction 28.44 25.16 39 7567 53073 46625383
Arthralgia 28.36 25.16 12 7594 364591 46313865
Reperfusion injury 26.91 25.16 5 7601 47 46678409
Blood fibrinogen decreased 26.01 25.16 8 7598 702 46677754
Bradycardia 25.90 25.16 42 7564 66256 46612200
Macular hole 25.45 25.16 8 7598 754 46677702
Haemorrhagic stroke 25.24 25.16 14 7592 5552 46672904

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 1075.12 20.66 205 9678 1016 29941579
Haemorrhage intracranial 625.43 20.66 221 9662 14811 29927784
Cerebral haemorrhage 586.30 20.66 262 9621 32625 29909970
Angioedema 413.27 20.66 209 9674 34175 29908420
Ventricular extrasystoles 215.35 20.66 95 9788 11379 29931216
Haemorrhage 204.90 20.66 148 9735 45931 29896664
Haemorrhagic infarction 167.29 20.66 36 9847 351 29942244
Death 140.57 20.66 340 9543 356943 29585652
Neurological decompensation 139.04 20.66 45 9838 2283 29940312
Ischaemic stroke 136.36 20.66 78 9805 16197 29926398
Ventricular tachycardia 127.80 20.66 86 9797 23776 29918819
Cerebral infarction 124.64 20.66 88 9795 26285 29916310
No adverse event 110.94 20.66 70 9813 17349 29925246
Chest pain 110.51 20.66 163 9720 117464 29825131
Intraventricular haemorrhage 108.64 20.66 40 9843 2990 29939605
NIH stroke scale score increased 106.48 20.66 16 9867 7 29942588
Brain oedema 97.39 20.66 57 9826 12341 29930254
Haematoma 86.44 20.66 68 9815 23885 29918710
Reperfusion arrhythmia 80.56 20.66 15 9868 63 29942532
Cerebral haematoma 80.21 20.66 36 9847 4478 29938117
Hemiparesis 78.37 20.66 53 9830 14749 29927846
Subarachnoid haemorrhage 76.45 20.66 45 9838 9841 29932754
Haemorrhagic stroke 75.45 20.66 38 9845 6109 29936486
Extrasystoles 63.52 20.66 29 9854 3753 29938842
Haemorrhagic cerebral infarction 62.86 20.66 19 9864 767 29941828
Stroke in evolution 58.87 20.66 10 9873 21 29942574
Brain herniation 57.58 20.66 27 9856 3713 29938882
Aphasia 57.14 20.66 49 9834 19390 29923205
Thrombolysis 56.70 20.66 11 9872 60 29942535
Bradycardia 54.57 20.66 86 9797 65440 29877155
Swollen tongue 53.14 20.66 40 9843 13152 29929443
Cerebral hyperperfusion syndrome 48.45 20.66 10 9873 78 29942517
Ventricular fibrillation 48.28 20.66 40 9843 15098 29927497
Electrocardiogram ST segment elevation 47.41 20.66 25 9858 4417 29938178
Hypotension 46.99 20.66 159 9724 200406 29742189
Gingival bleeding 46.50 20.66 28 9855 6376 29936219
Tongue oedema 45.69 20.66 21 9862 2759 29939836
Diarrhoea 45.61 20.66 27 9856 334076 29608519
Toxicity to various agents 43.89 20.66 4 9879 177179 29765416
Cerebral artery occlusion 42.36 20.66 14 9869 758 29941837
Hemiplegia 40.46 20.66 26 9857 6635 29935960
Intentional product use issue 37.73 20.66 53 9830 36387 29906208
Cardiac arrest 35.66 20.66 88 9795 92762 29849833
Paresis 33.74 20.66 15 9868 1823 29940772
Brain stem haemorrhage 33.42 20.66 12 9871 834 29941761
Basal ganglia haemorrhage 33.18 20.66 12 9871 851 29941744
Reocclusion 32.87 20.66 6 9877 22 29942573
Intracranial pressure increased 32.65 20.66 18 9865 3472 29939123
Blood fibrinogen decreased 31.59 20.66 12 9871 977 29941618
Catheter site haemorrhage 28.34 20.66 14 9869 2158 29940437
Cardiogenic shock 27.85 20.66 31 9852 16830 29925765
Rhythm idioventricular 27.70 20.66 8 9875 275 29942320
Extravasation 27.53 20.66 13 9870 1815 29940780
Lip swelling 27.44 20.66 27 9856 12717 29929878
Fall 27.24 20.66 13 9870 181859 29760736
Tongue haemorrhage 27.11 20.66 9 9874 494 29942101
Haemothorax 27.02 20.66 16 9867 3533 29939062
Aortic dissection 26.79 20.66 14 9869 2428 29940167
Cardiac ventricular thrombosis 26.65 20.66 10 9873 787 29941808
Malaise 26.47 20.66 11 9872 166951 29775644
Parotid gland haemorrhage 26.14 20.66 5 9878 25 29942570
Reperfusion injury 25.56 20.66 6 9877 89 29942506
Cerebral ischaemia 25.41 20.66 19 9864 6181 29936414
Fatigue 24.29 20.66 43 9840 320630 29621965
Injection site oedema 24.17 20.66 6 9877 114 29942481
Arrhythmia 22.83 20.66 40 9843 33129 29909466
Mouth haemorrhage 21.96 20.66 16 9867 5001 29937594
Embolic stroke 21.66 20.66 14 9869 3608 29938987
Epistaxis 21.14 20.66 51 9832 52930 29889665
Cerebrovascular accident 21.08 20.66 68 9815 83409 29859186
Product closure issue 21.05 20.66 3 9880 0 29942595
Factor I deficiency 21.05 20.66 3 9880 0 29942595
NIH stroke scale abnormal 21.05 20.66 3 9880 0 29942595
Hemianopia 20.98 20.66 8 9875 658 29941937
Coma 20.70 20.66 43 9840 40406 29902189

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

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
D010959 MESH_DESCRIPTOR_UI
5975 INN_ID
204210 RXNORM
4155 MMSL
970 MMSL
d00521 MMSL
002074 NDDF
108997009 SNOMEDCT_US
27638005 SNOMEDCT_US
37411004 SNOMEDCT_US
387152000 SNOMEDCT_US

Pharmaceutical products:

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