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

Stem definition	Drug id	CAS RN
enzymes	5141	105857-23-6

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.10	g	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
June 18, 1996	FDA	GENENTECH

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Plasminogen	Enzyme	P00747	PLMN_HUMAN	ACTIVATOR				DRUG LABEL	DRUG LABEL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cathflo Activase	HUMAN PRESCRIPTION DRUG LABEL	1	50242-041	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	2.20 mg	INTRAVENOUS	BLA	21 sections