alteplase 🐶 Veterinary Use | 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	908.35	24.72	157	8025	952	50595990
Angioedema	771.76	24.72	272	7910	37404	50559538
Cerebral haemorrhage	769.55	24.72	250	7932	26802	50570140
Haemorrhage intracranial	629.34	24.72	179	8003	12195	50584747
Death	278.68	24.72	300	7882	325079	50271863
Haemorrhage	202.49	24.72	119	8063	53322	50543620
No adverse event	162.98	24.72	88	8094	33490	50563452
Cerebral haematoma	130.06	24.72	39	8143	3172	50593770
Swollen tongue	127.75	24.72	71	8111	28559	50568383
Neurological decompensation	124.96	24.72	35	8147	2235	50594707
Subarachnoid haemorrhage	119.73	24.72	50	8132	10726	50586216
Cerebral infarction	111.46	24.72	59	8123	21545	50575397
NIH stroke scale score increased	108.23	24.72	14	8168	0	50596942
Intraventricular haemorrhage	103.69	24.72	29	8153	1841	50595101
Brain herniation	97.50	24.72	31	8151	3061	50593881
Thrombolysis	89.27	24.72	15	8167	74	50596868
Aplastic anaemia	83.07	24.72	35	8147	7668	50589274
Hemiparesis	82.04	24.72	47	8135	20001	50576941
Intracranial mass	78.97	24.72	21	8161	1102	50595840
Brain oedema	75.97	24.72	38	8144	12332	50584610
Stroke in evolution	67.34	24.72	11	8171	44	50596898
Haemorrhagic cerebral infarction	65.38	24.72	16	8166	600	50596342
NIH stroke scale abnormal	59.30	24.72	8	8174	3	50596939
Brain stem haemorrhage	57.81	24.72	15	8167	715	50596227
Aphasia	57.74	24.72	43	8139	28451	50568491
Tongue oedema	57.14	24.72	22	8160	3817	50593125
Product quality issue	56.87	24.72	44	8138	30814	50566128
Cardiogenic shock	51.88	24.72	32	8150	15567	50581375
Cerebral mass effect	51.35	24.72	14	8168	808	50596134
Haemorrhagic infarction	50.08	24.72	11	8171	254	50596688
Respiratory failure	49.35	24.72	67	8115	91114	50505828
Ventricular extrasystoles	46.65	24.72	26	8156	10490	50586452
Haematoma	46.64	24.72	39	8143	30471	50566471
Reperfusion arrhythmia	45.61	24.72	10	8172	229	50596713
Lip swelling	44.98	24.72	35	8147	24701	50572241
Cerebral hyperperfusion syndrome	44.67	24.72	7	8175	20	50596922
Ischaemic stroke	43.80	24.72	29	8153	15919	50581023
Hypotension	41.93	24.72	107	8075	235362	50361580
Diarrhoea	37.04	24.72	25	8157	588451	50008491
Coma	35.73	24.72	45	8137	56834	50540108
Hemiplegia	34.80	24.72	19	8163	7362	50589580
Intra-abdominal haemorrhage	34.03	24.72	13	8169	2207	50594735
Arthralgia	32.82	24.72	15	8167	438687	50158255
Ventricular tachycardia	32.32	24.72	24	8158	15797	50581145
Cardiac tamponade	32.01	24.72	15	8167	4217	50592725
Chest pain	31.05	24.72	80	8102	176802	50420140
Anaphylactic reaction	29.64	24.72	40	8142	54015	50542927
Procedural haemorrhage	29.62	24.72	12	8170	2378	50594564
Reocclusion	28.68	24.72	4	8178	3	50596939
Bradycardia	28.45	24.72	43	8139	64383	50532559
Haemothorax	28.31	24.72	11	8171	1955	50594987
Extravasation	28.12	24.72	11	8171	1991	50594951
Cardiac arrest	27.68	24.72	49	8133	83602	50513340
Blood fibrinogen decreased	26.76	24.72	8	8174	643	50596299
Haemorrhagic stroke	26.16	24.72	14	8168	5214	50591728
Reperfusion injury	26.15	24.72	5	8177	56	50596886
Myocardial rupture	26.07	24.72	5	8177	57	50596885
Macular hole	25.71	24.72	8	8174	735	50596207

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	1163.06	20.00	224	10284	1082	29562937
Haemorrhage intracranial	654.45	20.00	231	10277	14311	29549708
Cerebral haemorrhage	591.67	20.00	266	10242	31160	29532859
Angioedema	463.80	20.00	226	10282	31689	29532330
Ventricular extrasystoles	215.96	20.00	95	10413	10487	29553532
Haemorrhage	204.70	20.00	151	10357	44921	29519098
Haemorrhagic infarction	177.38	20.00	39	10469	391	29563628
Death	154.09	20.00	359	10149	341725	29222294
No adverse event	146.54	20.00	86	10422	17392	29546627
Neurological decompensation	137.24	20.00	46	10462	2416	29561603
Ventricular tachycardia	131.11	20.00	88	10420	22486	29541533
NIH stroke scale score increased	119.08	20.00	18	10490	7	29564012
Chest pain	108.81	20.00	164	10344	111809	29452210
Cerebral infarction	108.11	20.00	81	10427	24594	29539425
Intraventricular haemorrhage	107.38	20.00	40	10468	2866	29561153
Brain oedema	104.69	20.00	61	10447	12159	29551860
Haematoma	92.45	20.00	72	10436	23140	29540879
Cerebral haematoma	88.98	20.00	39	10469	4257	29559762
Aplastic anaemia	87.73	20.00	46	10462	7464	29556555
Subarachnoid haemorrhage	84.65	20.00	49	10459	9643	29554376
Hemiparesis	82.94	20.00	56	10452	14430	29549589
Reperfusion arrhythmia	81.28	20.00	15	10493	54	29563965
Haemorrhagic stroke	74.53	20.00	38	10470	5818	29558201
Ischaemic stroke	68.95	20.00	52	10456	15925	29548094
Thrombolysis	66.19	20.00	13	10495	70	29563949
Swollen tongue	64.49	20.00	45	10463	12221	29551798
Extrasystoles	63.82	20.00	29	10479	3445	29560574
Cerebral mass effect	63.48	20.00	20	10488	861	29563158
Brain herniation	62.58	20.00	29	10479	3604	29560415
Haemorrhagic cerebral infarction	62.53	20.00	19	10489	724	29563295
Stroke in evolution	58.46	20.00	10	10498	20	29563999
Bradycardia	52.39	20.00	88	10420	65541	29498478
Tongue oedema	52.18	20.00	23	10485	2543	29561476
Aphasia	50.61	20.00	47	10461	19151	29544868
Hypotension	48.22	20.00	165	10343	194189	29369830
Cerebral hyperperfusion syndrome	47.83	20.00	10	10498	77	29563942
Electrocardiogram ST segment elevation	45.41	20.00	25	10483	4467	29559552
Diarrhoea	44.75	20.00	32	10476	332666	29231353
Gingival bleeding	44.39	20.00	28	10480	6425	29557594
Ventricular fibrillation	44.14	20.00	40	10468	15793	29548226
Intentional product use issue	42.20	20.00	63	10445	42435	29521584
Toxicity to various agents	41.87	20.00	6	10502	173655	29390364
Hemiplegia	41.37	20.00	27	10481	6567	29557452
Basal ganglia haemorrhage	40.92	20.00	14	10494	782	29563237
Cardiac arrest	40.44	20.00	92	10416	85499	29478520
Cerebral artery occlusion	38.73	20.00	13	10495	685	29563334
Brain stem haemorrhage	35.92	20.00	13	10495	857	29563162
Reocclusion	33.10	20.00	6	10502	19	29564000
Paresis	32.55	20.00	15	10493	1839	29562180
Aortic dissection	31.88	20.00	16	10492	2368	29561651
Blood fibrinogen decreased	31.60	20.00	12	10496	906	29563113
Intracranial pressure increased	31.43	20.00	18	10490	3467	29560552
Haemothorax	29.01	20.00	17	10491	3419	29560600
Catheter site haemorrhage	28.13	20.00	14	10494	2034	29561985
Product closure issue	27.77	20.00	4	10504	0	29564019
Malaise	27.77	20.00	11	10497	159591	29404428
Extravasation	27.72	20.00	13	10495	1659	29562360
Rhythm idioventricular	27.14	20.00	8	10500	274	29563745
Tongue haemorrhage	26.58	20.00	9	10499	487	29563532
Lip swelling	26.36	20.00	27	10481	12383	29551636
Epistaxis	25.98	20.00	57	10451	51647	29512372
Cardiogenic shock	25.89	20.00	33	10475	19157	29544862
Product quality issue	25.78	20.00	30	10478	15865	29548154
Parotid gland haemorrhage	25.77	20.00	5	10503	25	29563994
Reperfusion injury	25.71	20.00	6	10502	80	29563939
Fatigue	25.62	20.00	46	10462	316775	29247244
Cerebral ischaemia	25.57	20.00	19	10489	5684	29558335
Cardiac ventricular thrombosis	24.34	20.00	10	10498	929	29563090
Fall	23.80	20.00	17	10491	177161	29386858
Hydrocephalus	23.03	20.00	16	10492	4311	29559708
Coma	22.73	20.00	46	10462	39404	29524615
Arrhythmia	22.35	20.00	40	10468	31273	29532746
Myocardial rupture	21.65	20.00	6	10502	164	29563855
Mouth haemorrhage	21.60	20.00	16	10492	4764	29559255
Weight decreased	20.89	20.00	14	10494	150891	29413128
Injection site oedema	20.87	20.00	6	10502	188	29563831
Pericardial haemorrhage	20.87	20.00	13	10495	2918	29561101
Factor I deficiency	20.83	20.00	3	10505	0	29564019
Hyperhidrosis	20.71	20.00	60	10448	64480	29499539
Hemianopia	20.56	20.00	8	10500	645	29563374
Shock	20.19	20.00	31	10477	21373	29542646

FDA Adverse Event Reporting System (Geriatric)

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	1915.48	21.22	353	15273	2036	64481070
Cerebral haemorrhage	1243.82	21.22	466	15160	50624	64432482
Haemorrhage intracranial	1083.10	21.22	347	15279	23537	64459569
Angioedema	1061.31	21.22	438	15188	61383	64421723
Haemorrhage	295.79	21.22	203	15423	79148	64403958
Cerebral haematoma	275.01	21.22	92	15534	7093	64476013
Neurological decompensation	257.47	21.22	78	15548	4358	64478748
Death	236.92	21.22	420	15206	482285	64000821
No adverse event	229.71	21.22	120	15506	28441	64454665
Cerebral infarction	227.57	21.22	135	15491	40909	64442197
NIH stroke scale score increased	225.76	21.22	32	15594	10	64483096
Subarachnoid haemorrhage	203.23	21.22	96	15530	18342	64464764
Intraventricular haemorrhage	178.26	21.22	58	15568	4095	64479011
Brain oedema	178.19	21.22	93	15533	21982	64461124
Aplastic anaemia	167.42	21.22	77	15549	13843	64469263
Brain herniation	163.45	21.22	61	15565	6472	64476634
Haemorrhagic cerebral infarction	163.43	21.22	42	15584	1272	64481834
Swollen tongue	158.10	21.22	101	15525	34853	64448253
Hemiparesis	152.07	21.22	93	15533	29734	64453372
Thrombolysis	152.01	21.22	28	15598	159	64482947
Haemorrhagic infarction	135.66	21.22	32	15594	673	64482433
Cerebral mass effect	134.26	21.22	38	15588	1668	64481438
Haematoma	123.80	21.22	97	15529	46153	64436953
Stroke in evolution	115.38	21.22	20	15606	75	64483031
Aphasia	105.62	21.22	84	15542	40822	64442284
Ventricular extrasystoles	100.60	21.22	59	15567	17470	64465636
Intracranial mass	93.66	21.22	30	15596	2013	64481093
Haemorrhagic stroke	92.11	21.22	46	15580	9905	64473201
Cerebral hyperperfusion syndrome	91.63	21.22	17	15609	101	64483005
Ventricular tachycardia	87.67	21.22	70	15556	34195	64448911
Tongue oedema	87.57	21.22	38	15588	5952	64477154
Brain stem haemorrhage	84.56	21.22	26	15600	1525	64481581
NIH stroke scale abnormal	75.80	21.22	11	15615	6	64483100
Product quality issue	74.36	21.22	60	15566	29739	64453367
Ischaemic stroke	73.60	21.22	59	15567	28976	64454130
Hemiplegia	70.70	21.22	42	15584	12726	64470380
Diarrhoea	69.50	21.22	45	15581	722659	63760447
Reperfusion arrhythmia	65.43	21.22	15	15611	277	64482829
Aortic dissection	64.22	21.22	26	15600	3426	64479680
Cardiogenic shock	63.89	21.22	57	15569	32370	64450736
Toxicity to various agents	63.55	21.22	7	15619	363506	64119600
Cardiac arrest	62.44	21.22	124	15502	153940	64329166
Lip swelling	60.72	21.22	55	15571	31852	64451254
Haemothorax	58.87	21.22	27	15599	4815	64478291
Basal ganglia haemorrhage	57.76	21.22	19	15607	1387	64481719
Fatigue	55.49	21.22	60	15566	748670	63734436
Respiratory failure	55.11	21.22	121	15505	161062	64322044
Arthralgia	50.55	21.22	22	15604	442238	64040868
Hydrocephalus	50.10	21.22	28	15598	7563	64475543
Reperfusion injury	49.23	21.22	11	15615	180	64482926
Intentional product use issue	48.95	21.22	85	15541	95279	64387827
Cerebral artery occlusion	47.56	21.22	17	15609	1594	64481512
Hypotension	47.33	21.22	200	15426	380774	64102332
Intracranial pressure increased	46.73	21.22	26	15600	6963	64476143
Coma	46.16	21.22	79	15547	87536	64395570
Cardiac tamponade	45.57	21.22	27	15599	8137	64474969
Intra-abdominal haemorrhage	44.42	21.22	21	15605	4010	64479096
Malaise	43.26	21.22	21	15605	396226	64086880
Blood fibrinogen decreased	41.59	21.22	15	15611	1443	64481663
Product closure issue	40.89	21.22	6	15620	4	64483102
Fall	39.89	21.22	26	15600	416800	64066306
Anaphylactic reaction	38.94	21.22	64	15562	68600	64414506
Epistaxis	38.54	21.22	78	15548	98053	64385053
Pericardial haemorrhage	37.92	21.22	19	15607	4117	64478989
Pulseless electrical activity	36.85	21.22	28	15598	12711	64470395
Tongue haemorrhage	36.81	21.22	12	15614	851	64482255
Myocardial rupture	36.48	21.22	9	15617	230	64482876
Extravasation	36.38	21.22	17	15609	3163	64479943
Nasopharyngitis	36.28	21.22	3	15623	196070	64287036
Mouth haemorrhage	36.20	21.22	25	15601	9794	64473312
Catheter site haemorrhage	36.05	21.22	19	15607	4572	64478534
Gingival bleeding	35.14	21.22	29	15597	14825	64468281
Hemianopia	33.55	21.22	13	15613	1526	64481580
Weight decreased	32.95	21.22	14	15612	285725	64197381
Cerebral artery embolism	32.95	21.22	13	15613	1601	64481505
Shock	32.31	21.22	43	15583	38197	64444909
Heparin-induced thrombocytopenia	32.23	21.22	22	15604	8457	64474649
Bradycardia	31.94	21.22	81	15545	118138	64364968
Paresis	31.72	21.22	16	15610	3516	64479590
Procedural haemorrhage	31.70	21.22	17	15609	4235	64478871
Embolism	31.29	21.22	25	15601	12210	64470896
Vitreous haemorrhage	30.74	21.22	15	15611	3070	64480036
Macular hole	30.48	21.22	10	15616	724	64482382
Brain death	29.57	21.22	17	15609	4844	64478262
Drug intolerance	29.55	21.22	5	15621	187987	64295119
Embolic stroke	29.35	21.22	19	15607	6692	64476414
Completed suicide	29.25	21.22	9	15617	224405	64258701
Cytokine release syndrome	28.54	21.22	30	15596	20799	64462307
Hypofibrinogenaemia	28.36	21.22	12	15614	1766	64481340
Myalgia	27.82	21.22	3	15623	158614	64324492
Parotid gland haemorrhage	27.51	21.22	5	15621	26	64483080
Coagulopathy	27.13	21.22	36	15590	31884	64451222
Chest pain	27.02	21.22	121	15505	235859	64247247
Carotid artery occlusion	27.01	21.22	15	15611	4002	64479104
Cerebral artery thrombosis	26.89	21.22	10	15616	1049	64482057
Cerebellar haemorrhage	26.81	21.22	13	15613	2624	64480482
Lip oedema	25.96	21.22	16	15610	5173	64477933
Electrocardiogram ST segment elevation	25.63	21.22	18	15608	7241	64475865
Monoparesis	25.50	21.22	13	15613	2921	64480185
Intracardiac thrombus	25.10	21.22	14	15612	3767	64479339
Retroperitoneal haematoma	24.79	21.22	15	15611	4696	64478410
Extrasystoles	24.66	21.22	17	15609	6641	64476465
Depression	24.52	21.22	7	15619	183284	64299822
Pruritus	24.21	21.22	24	15602	312376	64170730
Cardiac ventricular thrombosis	24.04	21.22	10	15616	1410	64481696
Reocclusion	23.76	21.22	4	15622	12	64483094
Facial paralysis	23.67	21.22	26	15600	18940	64464166
Pain	23.67	21.22	63	15563	553448	63929658
Compartment syndrome	23.63	21.22	14	15612	4218	64478888
Cerebral artery stenosis	23.48	21.22	8	15618	651	64482455
Product dose omission issue	23.32	21.22	9	15617	194738	64288368
Peripheral artery occlusion	23.14	21.22	11	15615	2127	64480979
Rash	22.94	21.22	48	15578	458501	64024605
Cerebral ischaemia	22.63	21.22	19	15607	9943	64473163
Thyroid haemorrhage	22.60	21.22	5	15621	78	64483028
Abdominal discomfort	22.54	21.22	8	15618	182314	64300792
Quadriplegia	22.33	21.22	12	15614	3001	64480105
Insomnia	22.30	21.22	10	15616	197826	64285280
Weight increased	22.21	21.22	12	15614	213336	64269770
Paralysis	22.08	21.22	20	15606	11575	64471531
Endotracheal intubation	22.05	21.22	13	15613	3882	64479224
Factor I deficiency	21.98	21.22	3	15623	0	64483106
Ventricular fibrillation	21.97	21.22	28	15598	23832	64459274
Dysarthria	21.87	21.22	46	15580	59360	64423746
Cerebral reperfusion injury	21.82	21.22	4	15622	22	64483084
Stridor	21.81	21.22	14	15612	4860	64478246
Decreased appetite	21.34	21.22	22	15604	281267	64201839
Asthenia	21.24	21.22	45	15581	427999	64055107

FDA Adverse Event Reporting System (Pediatric)

None

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 | Suggest Off label Use Form| |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

🐶 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:

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
108997009	SNOMEDCT_US
27638005	SNOMEDCT_US
37411004	SNOMEDCT_US
387152000	SNOMEDCT_US
D010959	MESH_DESCRIPTOR_UI
002074	NDDF

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