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	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 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	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:

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
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:

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