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 1034.27 24.70 175 8897 1060 63478890
Cerebral haemorrhage 904.67 24.70 283 8789 30446 63449504
Angioedema 845.34 24.70 300 8772 47665 63432285
Haemorrhage intracranial 677.90 24.70 188 8884 13231 63466719
Death 300.81 24.70 315 8757 374066 63105884
No adverse event 244.79 24.70 119 8953 41286 63438664
Haemorrhage 230.79 24.70 130 8942 60892 63419058
Aplastic anaemia 146.03 24.70 54 9018 9515 63470435
Cerebral haematoma 142.57 24.70 42 9030 3641 63476309
Cerebral infarction 142.08 24.70 69 9003 23824 63456126
Swollen tongue 136.49 24.70 76 8996 34724 63445226
Subarachnoid haemorrhage 135.00 24.70 57 9015 14226 63465724
Neurological decompensation 133.15 24.70 37 9035 2601 63477349
Intraventricular haemorrhage 112.83 24.70 31 9041 2089 63477861
Brain herniation 112.55 24.70 35 9037 3642 63476308
NIH stroke scale score increased 109.96 24.70 14 9058 0 63479950
Hemiparesis 88.95 24.70 50 9022 23232 63456718
Thrombolysis 85.21 24.70 15 9057 117 63479833
Brain oedema 84.37 24.70 41 9031 14154 63465796
NIH stroke scale abnormal 81.61 24.70 11 9061 6 63479944
Intracranial mass 80.04 24.70 21 9051 1186 63478764
Haemorrhagic cerebral infarction 76.91 24.70 18 9054 632 63479318
Cerebral mass effect 70.84 24.70 18 9054 895 63479055
Stroke in evolution 67.21 24.70 11 9061 52 63479898
Lip swelling 66.10 24.70 46 9026 31017 63448933
Product quality issue 62.38 24.70 47 9025 35818 63444132
Tongue oedema 59.52 24.70 23 9049 4563 63475387
Aphasia 59.07 24.70 44 9028 32956 63446994
Brain stem haemorrhage 58.93 24.70 15 9057 751 63479199
Respiratory failure 57.85 24.70 72 9000 101786 63378164
Cardiogenic shock 53.95 24.70 33 9039 17899 63462051
Haematoma 50.52 24.70 41 9031 34779 63445171
Haemorrhagic infarction 50.18 24.70 11 9061 286 63479664
Ischaemic stroke 48.85 24.70 31 9041 17926 63462024
Ventricular extrasystoles 47.08 24.70 26 9046 11661 63468289
Reperfusion arrhythmia 46.63 24.70 10 9062 234 63479716
Cerebral hyperperfusion syndrome 45.53 24.70 7 9065 20 63479930
Hypotension 44.48 24.70 111 8961 272493 63207457
Haemothorax 43.41 24.70 15 9057 2170 63477780
Diarrhoea 40.95 24.70 26 9046 715340 62764610
Intra-abdominal haemorrhage 37.90 24.70 14 9058 2455 63477495
Coma 37.32 24.70 46 9026 64318 63415632
Reocclusion 36.92 24.70 5 9067 3 63479947
Cardiac arrest 35.29 24.70 54 9018 92491 63387459
Haemorrhagic stroke 35.22 24.70 17 9055 5775 63474175
Extravasation 34.76 24.70 13 9059 2359 63477591
Procedural haemorrhage 33.18 24.70 13 9059 2675 63477275
Hemiplegia 32.84 24.70 19 9053 9304 63470646
Heparin-induced thrombocytopenia 32.64 24.70 15 9057 4567 63475383
Abdominal discomfort 32.19 24.70 4 9068 320881 63159069
Arthralgia 32.16 24.70 21 9051 569689 62910261
Ventricular tachycardia 32.13 24.70 25 9047 19954 63459996
Cardiac tamponade 32.05 24.70 15 9057 4760 63475190
Blood fibrinogen decreased 29.84 24.70 9 9063 844 63479106
Bradycardia 29.72 24.70 44 9028 73183 63406767
Chest pain 29.14 24.70 82 8990 215877 63264073
Basal ganglia haemorrhage 27.70 24.70 8 9064 646 63479304
Anaphylactic reaction 27.23 24.70 40 9032 66060 63413890
Brain death 26.94 24.70 12 9060 3398 63476552
Shock 26.62 24.70 24 9048 23439 63456511
Myocardial rupture 26.23 24.70 5 9067 63 63479887
Reperfusion injury 26.01 24.70 5 9067 66 63479884
Nasopharyngitis 25.91 24.70 3 9069 254254 63225696
Retroperitoneal haemorrhage 25.87 24.70 11 9061 2786 63477164
Macular hole 25.76 24.70 8 9064 828 63479122
Product temperature excursion issue 25.60 24.70 6 9066 212 63479738
Hydrocephalus 24.72 24.70 13 9059 5287 63474663

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 1298.69 20.72 249 11317 1274 34944091
Haemorrhage intracranial 699.26 20.72 244 11322 15702 34929663
Cerebral haemorrhage 695.36 20.72 301 11265 34636 34910729
Angioedema 522.52 20.72 252 11314 37122 34908243
Haemorrhage 218.89 20.72 161 11405 51209 34894156
Ventricular extrasystoles 214.08 20.72 96 11470 11912 34933453
No adverse event 205.73 20.72 115 11451 22812 34922553
Haemorrhagic infarction 192.76 20.72 42 11524 435 34944930
Death 150.64 20.72 374 11192 397675 34547690
Neurological decompensation 135.92 20.72 47 11519 2919 34942446
NIH stroke scale score increased 131.54 20.72 20 11546 11 34945354
Cerebral infarction 125.77 20.72 90 11476 27365 34918000
Ventricular tachycardia 123.75 20.72 88 11478 26491 34918874
Brain oedema 120.30 20.72 68 11498 13753 34931612
Intraventricular haemorrhage 116.91 20.72 44 11522 3487 34941878
Cerebral haematoma 115.68 20.72 47 11519 4568 34940797
Aplastic anaemia 104.51 20.72 55 11511 9661 34935704
Chest pain 103.60 20.72 165 11401 126597 34818768
Hemiparesis 94.31 20.72 61 11505 15717 34929648
Subarachnoid haemorrhage 93.61 20.72 56 11510 12579 34932786
Haematoma 92.87 20.72 73 11493 25532 34919833
Haemorrhagic cerebral infarction 82.45 20.72 24 11542 847 34944518
Reperfusion arrhythmia 81.71 20.72 15 11551 57 34945308
Brain herniation 80.93 20.72 35 11531 3973 34941392
Gingival bleeding 76.34 20.72 40 11526 6960 34938405
Haemorrhagic stroke 76.00 20.72 39 11527 6500 34938865
Ischaemic stroke 74.87 20.72 56 11510 18194 34927171
Swollen tongue 71.76 20.72 50 11516 14555 34930810
Cerebral mass effect 66.87 20.72 21 11545 962 34944403
Thrombolysis 64.96 20.72 13 11553 85 34945280
Extrasystoles 63.14 20.72 29 11537 3794 34941571
Stroke in evolution 61.43 20.72 11 11555 35 34945330
Aphasia 60.74 20.72 53 11513 21401 34923964
Tongue oedema 59.95 20.72 26 11540 2971 34942394
Cerebral artery occlusion 59.14 20.72 18 11548 742 34944623
Hemiplegia 54.50 20.72 32 11534 6940 34938425
Bradycardia 50.59 20.72 90 11476 75328 34870037
Diarrhoea 50.06 20.72 34 11532 389878 34555487
Cardiac arrest 50.04 20.72 103 11463 96056 34849309
Brain stem haemorrhage 47.50 20.72 16 11550 916 34944449
Cerebral hyperperfusion syndrome 47.45 20.72 10 11556 87 34945278
Hypotension 46.67 20.72 170 11396 221479 34723886
Toxicity to various agents 43.71 20.72 7 11559 200355 34745010
Electrocardiogram ST segment elevation 43.48 20.72 25 11541 5213 34940152
Basal ganglia haemorrhage 39.82 20.72 14 11552 912 34944453
Intracranial pressure increased 38.61 20.72 21 11545 3934 34941431
Product closure issue 37.93 20.72 6 11560 6 34945359
Ventricular fibrillation 34.10 20.72 40 11526 22914 34922451
Aortic dissection 33.59 20.72 17 11549 2751 34942614
Tongue haemorrhage 33.55 20.72 11 11555 579 34944786
Reocclusion 33.30 20.72 6 11560 20 34945345
NIH stroke scale abnormal 32.72 20.72 5 11561 3 34945362
Intentional product use issue 32.18 20.72 65 11501 59751 34885614
Paresis 31.21 20.72 15 11551 2171 34943194
Catheter site haemorrhage 30.97 20.72 15 11551 2209 34943156
Coma 29.94 20.72 54 11512 45624 34899741
Blood fibrinogen decreased 29.02 20.72 12 11554 1218 34944147
Fatigue 28.92 20.72 49 11517 370604 34574761
Malaise 28.39 20.72 13 11553 185812 34759553
Haemothorax 28.33 20.72 17 11549 3835 34941530
Product quality issue 27.51 20.72 31 11535 17004 34928361
Epistaxis 27.48 20.72 60 11506 58191 34887174
Cerebral ischaemia 27.26 20.72 20 11546 6302 34939063
Extravasation 27.08 20.72 13 11553 1877 34943488
Fall 26.89 20.72 17 11549 202868 34742497
Rhythm idioventricular 26.61 20.72 8 11558 316 34945049
Myocardial rupture 26.39 20.72 7 11559 174 34945191
Cardiac ventricular thrombosis 26.30 20.72 11 11555 1149 34944216
Reperfusion injury 26.14 20.72 6 11560 80 34945285
Hydrocephalus 25.89 20.72 18 11548 5214 34940151
Mouth haemorrhage 25.62 20.72 18 11548 5301 34940064
Parotid gland haemorrhage 25.35 20.72 5 11561 30 34945335
Hemianopia 24.25 20.72 9 11557 685 34944680
Lip swelling 23.84 20.72 28 11538 16052 34929313
Shock 23.23 20.72 34 11532 24145 34921220
Hyperhidrosis 23.07 20.72 66 11500 75626 34869739
Weight decreased 23.04 20.72 15 11551 176286 34769079
Neutropenia 22.38 20.72 12 11554 156766 34788599
Product dose omission issue 22.33 20.72 6 11560 119705 34825660
Respiratory failure 21.69 20.72 82 11484 108490 34836875
Paralysis 21.30 20.72 17 11549 6065 34939300
NIH stroke scale score decreased 21.04 20.72 3 11563 0 34945365
Factor I deficiency 21.04 20.72 3 11563 0 34945365
Pericardial haemorrhage 20.83 20.72 13 11553 3145 34942220

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 2147.75 21.41 390 17078 2302 79724618
Cerebral haemorrhage 1474.51 21.41 531 16937 57142 79669778
Angioedema 1190.15 21.41 490 16978 75545 79651375
Haemorrhage intracranial 1172.79 21.41 368 17100 25825 79701095
Haemorrhage 336.35 21.41 223 17245 90895 79636025
Cerebral haematoma 319.38 21.41 103 17365 7839 79719081
No adverse event 319.26 21.41 158 17310 37034 79689886
Cerebral infarction 277.61 21.41 154 17314 45522 79681398
Neurological decompensation 264.92 21.41 81 17387 5172 79721748
Death 249.07 21.41 444 17024 566070 79160850
Aplastic anaemia 244.39 21.41 105 17363 17800 79709120
NIH stroke scale score increased 238.75 21.41 34 17434 17 79726903
Subarachnoid haemorrhage 225.04 21.41 109 17359 24356 79702564
Brain herniation 202.31 21.41 72 17396 7391 79719529
Brain oedema 201.04 21.41 102 17366 25161 79701759
Intraventricular haemorrhage 198.99 21.41 64 17404 4823 79722097
Haemorrhagic cerebral infarction 197.32 21.41 49 17419 1430 79725490
Swollen tongue 176.04 21.41 112 17356 42458 79684462
Hemiparesis 170.77 21.41 101 17367 33632 79693288
Cerebral mass effect 161.41 21.41 44 17424 1862 79725058
Thrombolysis 145.62 21.41 28 17440 232 79726688
Haemorrhagic infarction 141.15 21.41 33 17435 741 79726179
Haematoma 128.52 21.41 100 17368 52095 79674825
Stroke in evolution 121.99 21.41 21 17447 85 79726835
Aphasia 118.25 21.41 91 17377 46641 79680279
NIH stroke scale abnormal 111.69 21.41 16 17452 9 79726911
Haemorrhagic stroke 103.91 21.41 50 17418 10996 79715924
Ventricular extrasystoles 102.32 21.41 60 17408 19644 79707276
Brain stem haemorrhage 98.55 21.41 29 17439 1621 79725299
Tongue oedema 97.94 21.41 42 17426 7075 79719845
Intracranial mass 93.66 21.41 30 17438 2229 79724691
Cerebral hyperperfusion syndrome 91.44 21.41 17 17451 115 79726805
Ventricular tachycardia 83.49 21.41 71 17397 41864 79685056
Cardiac arrest 83.01 21.41 141 17327 171955 79554965
Hemiplegia 81.57 21.41 47 17421 14892 79712028
Ischaemic stroke 80.50 21.41 63 17405 33068 79693852
Product quality issue 79.15 21.41 63 17405 33877 79693043
Diarrhoea 78.72 21.41 48 17420 880441 78846479
Cerebral artery occlusion 71.93 21.41 23 17445 1699 79725221
Haemothorax 71.03 21.41 31 17437 5447 79721473
Lip swelling 70.87 21.41 64 17404 40847 79686073
Gingival bleeding 67.68 21.41 43 17425 16233 79710687
Reperfusion arrhythmia 66.53 21.41 15 17453 285 79726635
Aortic dissection 65.33 21.41 27 17441 4148 79722772
Fatigue 64.98 21.41 65 17403 929662 78797258
Toxicity to various agents 64.98 21.41 8 17460 421532 79305388
Respiratory failure 61.93 21.41 128 17340 180783 79546137
Basal ganglia haemorrhage 60.39 21.41 20 17448 1651 79725269
Cardiogenic shock 58.16 21.41 58 17410 41856 79685064
Coma 54.60 21.41 87 17381 100562 79626358
Product closure issue 54.39 21.41 8 17460 7 79726913
Arthralgia 54.09 21.41 29 17439 571774 79155146
Hydrocephalus 53.98 21.41 30 17438 8870 79718050
Intracranial pressure increased 53.08 21.41 29 17439 8293 79718627
Intra-abdominal haemorrhage 50.25 21.41 23 17445 4517 79722403
Reperfusion injury 49.78 21.41 11 17457 190 79726730
Hypotension 48.66 21.41 208 17260 440109 79286811
Tongue haemorrhage 48.49 21.41 15 17453 994 79725926
Malaise 47.56 21.41 24 17444 489845 79237075
Cardiac tamponade 47.50 21.41 28 17440 9248 79717672
Mouth haemorrhage 45.82 21.41 29 17439 10870 79716050
Cytokine release syndrome 44.83 21.41 47 17421 35951 79690969
Nasopharyngitis 43.93 21.41 3 17465 253878 79473042
Heparin-induced thrombocytopenia 43.83 21.41 27 17441 9655 79717265
Epistaxis 43.05 21.41 83 17385 111432 79615488
Fall 42.87 21.41 27 17441 487602 79239318
Shock 42.42 21.41 50 17418 43498 79683422
Blood fibrinogen decreased 42.18 21.41 16 17452 1963 79724957
Myocardial rupture 41.93 21.41 10 17458 245 79726675
Catheter site haemorrhage 41.67 21.41 21 17447 5096 79721824
Anaphylactic reaction 40.83 21.41 69 17399 83674 79643246
Hemianopia 40.58 21.41 15 17453 1713 79725207
Treatment delayed 40.34 21.41 8 17460 79 79726841
Pulseless electrical activity 38.95 21.41 29 17439 14131 79712789
Pericardial haemorrhage 38.23 21.41 19 17449 4476 79722444
Brain death 36.81 21.41 20 17448 5657 79721263
Drug intolerance 36.15 21.41 7 17461 264112 79462808
Embolic stroke 35.87 21.41 22 17446 7804 79719116
Cerebral artery embolism 35.71 21.41 14 17454 1877 79725043
Extravasation 35.34 21.41 17 17451 3733 79723187
Weight decreased 35.06 21.41 17 17451 355181 79371739
Procedural haemorrhage 34.52 21.41 18 17450 4688 79722232
Coagulopathy 34.50 21.41 41 17427 35965 79690955
Pain 33.26 21.41 65 17403 703737 79023183
Bradycardia 33.13 21.41 84 17384 135473 79591447
Vitreous haemorrhage 32.49 21.41 16 17452 3697 79723223
Abdominal discomfort 31.57 21.41 8 17460 250719 79476201
Facial paralysis 30.79 21.41 30 17438 21042 79705878
Reocclusion 30.73 21.41 5 17463 13 79726907
Embolism 30.57 21.41 25 17443 13957 79712963
Paresis 30.41 21.41 16 17452 4245 79722675
Macular hole 30.37 21.41 10 17458 811 79726109
Intentional product use issue 29.90 21.41 87 17381 152025 79574895
Alopecia 29.88 21.41 7 17461 231348 79495572
Cerebellar haemorrhage 29.85 21.41 14 17454 2906 79724014
Weight increased 29.37 21.41 12 17456 277374 79449546
Product dose omission issue 29.12 21.41 9 17459 247528 79479392
Hypofibrinogenaemia 28.15 21.41 12 17456 1990 79724930
Dysarthria 28.15 21.41 52 17416 67570 79659350
Pruritus 28.13 21.41 27 17441 394621 79332299
Musculoskeletal stiffness 27.73 21.41 3 17465 175005 79551915
Myalgia 27.43 21.41 4 17464 185637 79541283
Cerebral artery thrombosis 27.40 21.41 10 17458 1101 79725819
Parotid gland haemorrhage 27.27 21.41 5 17463 31 79726889
Completed suicide 27.06 21.41 10 17458 245757 79481163
Retroperitoneal haemorrhage 26.67 21.41 16 17452 5454 79721466
Carotid artery occlusion 26.42 21.41 18 17450 7629 79719291
Cardiac ventricular thrombosis 26.17 21.41 11 17457 1762 79725158
Rash 25.95 21.41 55 17413 578303 79148617
Respiratory distress 25.73 21.41 46 17422 58293 79668627
Peripheral artery occlusion 25.34 21.41 12 17456 2545 79724375
Insomnia 25.32 21.41 11 17457 245159 79481761
Depression 25.28 21.41 8 17460 216782 79510138
Peripheral ischaemia 25.19 21.41 19 17449 9438 79717482
Electrocardiogram ST segment elevation 24.90 21.41 18 17450 8379 79718541
Decreased appetite 24.90 21.41 23 17445 342395 79384525
Intracardiac thrombus 24.75 21.41 14 17454 4279 79722641
Lip oedema 24.56 21.41 16 17452 6300 79720620
Retroperitoneal haematoma 24.56 21.41 15 17453 5282 79721638
Extrasystoles 24.54 21.41 17 17451 7402 79719518
Monoparesis 24.53 21.41 13 17455 3498 79723422
Cerebral ischaemia 24.44 21.41 20 17448 11175 79715745
Paralysis 23.57 21.41 21 17447 13156 79713764
Chest pain 23.53 21.41 123 17345 282181 79444739
Hypoxia 23.19 21.41 62 17406 103181 79623739
Cerebral artery stenosis 23.10 21.41 8 17460 757 79726163
Asthenia 22.66 21.41 49 17419 511640 79215280
Compartment syndrome 22.56 21.41 14 17454 5068 79721852
Factor I deficiency 22.28 21.41 3 17465 0 79726920
NIH stroke scale score decreased 22.28 21.41 3 17465 0 79726920
Quadriplegia 22.24 21.41 12 17456 3348 79723572
Haemoperitoneum 21.95 21.41 13 17455 4330 79722590
Multiple organ dysfunction syndrome 21.94 21.41 67 17401 120179 79606741
Thyroid haemorrhage 21.79 21.41 5 17463 103 79726817
Stridor 21.66 21.41 14 17454 5439 79721481
Cerebrovascular accident 21.64 21.41 79 17389 155213 79571707
Haematuria 21.54 21.41 47 17421 68789 79658131
Sinusitis 21.44 21.41 8 17460 195493 79531427

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 | Suggest Off label Use Form| |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
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
Cathflo Activase HUMAN PRESCRIPTION DRUG LABEL 1 50242-041 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 2.20 mg INTRAVENOUS BLA 21 sections