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 878.14 23.59 153 7995 1045 53339873
Angioedema 738.71 23.59 267 7881 41809 53299109
Cerebral haemorrhage 738.09 23.59 245 7903 29751 53311167
Haemorrhage intracranial 603.55 23.59 174 7974 13178 53327740
Death 262.75 23.59 296 7852 356936 52983982
Haemorrhage 197.16 23.59 118 8030 57869 53283049
Cerebral haematoma 128.78 23.59 39 8109 3475 53337443
Cerebral infarction 127.55 23.59 66 8082 24378 53316540
Swollen tongue 126.09 23.59 71 8077 31009 53309909
Neurological decompensation 123.70 23.59 35 8113 2457 53338461
No adverse event 123.30 23.59 76 8072 39189 53301729
NIH stroke scale score increased 109.03 23.59 14 8134 0 53340918
Subarachnoid haemorrhage 107.85 23.59 47 8101 11846 53329072
Ischaemic stroke 100.86 23.59 51 8097 17942 53322976
Intraventricular haemorrhage 94.12 23.59 27 8121 1991 53338927
Brain herniation 92.65 23.59 30 8118 3326 53337592
Thrombolysis 87.64 23.59 15 8133 90 53340828
Hemiparesis 84.21 23.59 48 8100 21427 53319491
Intracranial mass 77.91 23.59 21 8127 1230 53339688
Aplastic anaemia 75.81 23.59 33 8115 8288 53332630
Brain oedema 74.72 23.59 38 8110 13520 53327398
Aphasia 61.45 23.59 45 8103 30733 53310185
Stroke in evolution 61.02 23.59 10 8138 44 53340874
NIH stroke scale abnormal 59.75 23.59 8 8140 3 53340915
Haemorrhagic cerebral infarction 54.77 23.59 14 8134 666 53340252
Brain stem haemorrhage 52.88 23.59 14 8134 765 53340153
Tongue oedema 52.60 23.59 21 8127 4246 53336672
Product quality issue 52.02 23.59 44 8104 36979 53303939
Cerebral mass effect 50.70 23.59 14 8134 898 53340020
Cardiogenic shock 50.20 23.59 32 8116 17450 53323468
Reperfusion arrhythmia 49.57 23.59 10 8138 160 53340758
Haemorrhagic infarction 48.71 23.59 11 8137 307 53340611
Cerebrovascular accident 46.35 23.59 68 8080 105106 53235812
Ventricular extrasystoles 45.39 23.59 26 8122 11698 53329220
Cerebral hyperperfusion syndrome 45.07 23.59 7 8141 20 53340898
Respiratory failure 44.31 23.59 65 8083 100447 53240471
Haematoma 43.04 23.59 38 8110 33806 53307112
Lip swelling 41.68 23.59 34 8114 27167 53313751
Hypotension 40.62 23.59 107 8041 253969 53086949
Diarrhoea 37.33 23.59 25 8123 625521 52715397
Hemiplegia 34.83 23.59 19 8129 7781 53333137
Intra-abdominal haemorrhage 33.60 23.59 13 8135 2419 53338499
Coma 33.25 23.59 44 8104 61739 53279179
Cardiac tamponade 31.63 23.59 15 8133 4585 53336333
Ventricular tachycardia 31.06 23.59 24 8124 17738 53323180
Chest pain 30.26 23.59 80 8068 190105 53150813
Arthralgia 29.85 23.59 15 8133 439768 52901150
Procedural haemorrhage 29.45 23.59 12 8136 2557 53338361
Reocclusion 28.91 23.59 4 8144 3 53340915
Haemothorax 28.14 23.59 11 8137 2103 53338815
Anaphylactic reaction 27.55 23.59 39 8109 58287 53282631
Bradycardia 27.12 23.59 43 8105 71013 53269905
Pulmonary embolism 26.78 23.59 56 8092 114386 53226532
Blood fibrinogen decreased 25.94 23.59 8 8140 756 53340162
Reperfusion injury 25.90 23.59 5 8143 63 53340855
Heparin-induced thrombocytopenia 25.78 23.59 13 8135 4536 53336382
Cardiac arrest 25.71 23.59 49 8099 93618 53247300
Macular hole 25.67 23.59 8 8140 783 53340135
Haemorrhagic stroke 25.64 23.59 14 8134 5744 53335174
Cerebral artery embolism 24.96 23.59 8 8140 857 53340061
Myocardial rupture 24.96 23.59 5 8143 77 53340841
Brain death 24.40 23.59 11 8137 2997 53337921
Extravasation 23.87 23.59 10 8138 2284 53338634

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 1151.64 21.71 220 10235 1138 32501933
Haemorrhage intracranial 641.73 21.71 227 10228 15660 32487411
Cerebral haemorrhage 597.92 21.71 268 10187 34479 32468592
Angioedema 439.83 21.71 220 10235 36069 32467002
Ventricular extrasystoles 213.40 21.71 95 10360 11931 32491140
Haemorrhage 203.41 21.71 150 10305 49298 32453773
Haemorrhagic infarction 180.18 21.71 39 10416 403 32502668
Ischaemic stroke 159.57 21.71 88 10367 17488 32485583
Death 147.98 21.71 356 10099 382161 32120910
Cerebral infarction 139.40 21.71 95 10360 27519 32475552
Neurological decompensation 137.62 21.71 46 10409 2652 32500419
Ventricular tachycardia 129.18 21.71 88 10367 25468 32477603
NIH stroke scale score increased 120.87 21.71 18 10437 7 32503064
No adverse event 113.25 21.71 74 10381 19979 32483092
Intraventricular haemorrhage 111.57 21.71 41 10414 3129 32499942
Chest pain 109.83 21.71 165 10290 123972 32379099
Brain oedema 104.34 21.71 60 10395 12900 32490171
Cerebral haematoma 88.48 21.71 39 10416 4772 32498299
Subarachnoid haemorrhage 85.94 21.71 49 10406 10362 32492709
Haematoma 85.91 21.71 69 10386 25615 32477456
Hemiparesis 84.23 21.71 56 10399 15551 32487520
Reperfusion arrhythmia 80.94 21.71 15 10440 63 32503008
Haemorrhagic stroke 74.49 21.71 38 10417 6440 32496631
Thrombolysis 66.87 21.71 13 10442 74 32502997
Cerebral mass effect 65.20 21.71 20 10435 872 32502199
Swollen tongue 64.24 21.71 45 10410 13594 32489477
Extrasystoles 63.12 21.71 29 10426 3908 32499163
Haemorrhagic cerebral infarction 62.44 21.71 19 10436 806 32502265
Brain herniation 60.45 21.71 28 10427 3843 32499228
Stroke in evolution 59.12 21.71 10 10445 21 32503050
Aphasia 55.30 21.71 49 10406 20779 32482292
Bradycardia 53.25 21.71 88 10367 71474 32431597
Aplastic anaemia 51.10 21.71 31 10424 7342 32495729
Tongue oedema 48.52 21.71 22 10433 2874 32500197
Cerebral hyperperfusion syndrome 48.05 21.71 10 10445 84 32502987
Hypotension 47.61 21.71 165 10290 215945 32287126
Cerebral artery occlusion 46.09 21.71 15 10440 794 32502277
Electrocardiogram ST segment elevation 45.71 21.71 25 10430 4875 32498196
Diarrhoea 45.41 21.71 31 10424 364771 32138300
Gingival bleeding 44.94 21.71 28 10427 6953 32496118
Ventricular fibrillation 44.51 21.71 40 10415 17270 32485801
Hemiplegia 42.12 21.71 27 10428 7041 32496030
Toxicity to various agents 40.19 21.71 5 10450 178036 32325035
Cardiac arrest 40.12 21.71 93 10362 96683 32406388
Intentional product use issue 34.22 21.71 54 10401 42157 32460914
Basal ganglia haemorrhage 33.34 21.71 12 10443 862 32502209
Paresis 32.63 21.71 15 10440 2022 32501049
Reocclusion 32.41 21.71 6 10449 25 32503046
Brain stem haemorrhage 32.12 21.71 12 10443 958 32502113
Intracranial pressure increased 31.60 21.71 18 10437 3795 32499276
Blood fibrinogen decreased 31.04 21.71 12 10443 1052 32502019
Cardiac ventricular thrombosis 29.31 21.71 11 10444 889 32502182
Haemothorax 28.94 21.71 17 10438 3795 32499276
Product closure issue 28.17 21.71 4 10451 0 32503071
Catheter site haemorrhage 28.06 21.71 14 10441 2261 32500810
Malaise 27.97 21.71 11 10444 177127 32325944
Extravasation 27.35 21.71 13 10442 1890 32501181
Rhythm idioventricular 26.91 21.71 8 10447 313 32502758
Fall 26.65 21.71 15 10440 196186 32306885
Tongue haemorrhage 26.64 21.71 9 10446 535 32502536
Cardiogenic shock 26.57 21.71 33 10422 20629 32482442
Aortic dissection 26.35 21.71 14 10441 2576 32500495
Lip swelling 26.27 21.71 27 10428 13738 32489333
Parotid gland haemorrhage 26.26 21.71 5 10450 25 32503046
Fatigue 25.74 21.71 46 10409 350655 32152416
Reperfusion injury 25.71 21.71 6 10449 89 32502982
Epistaxis 25.71 21.71 56 10399 55799 32447272
Cerebral ischaemia 25.39 21.71 19 10436 6348 32496723
Embolic stroke 23.94 21.71 15 10440 3759 32499312
Cerebrovascular accident 23.53 21.71 71 10384 86249 32416822
Hydrocephalus 23.38 21.71 16 10439 4649 32498422
Injection site oedema 22.80 21.71 6 10449 149 32502922
Coma 22.26 21.71 45 10410 42567 32460504
Product quality issue 22.02 21.71 29 10426 19204 32483867
Arrhythmia 21.77 21.71 40 10415 35263 32467808

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
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
D010959 MESH_DESCRIPTOR_UI

Pharmaceutical products:

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