Tenecteplase - Drugbank

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10/30/2018 Tenecteplase - DrugBank

Tenecteplase

Targets (11) Biointeractions (1)

IDENTIFICATION

Name Tenecteplase

Accession Number DB00031 (BTD00019, BIOD00019)

Type

Biotech

Groups

Approved

Biologic Classiﬁcation Protein Based Therapies Thrombolytic agents

Description Tissue plasminogen activator (tPA). Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modiﬁcations to the complementary DNA (cDNA) for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296- 299 in the protease domain.

Protein structure

https://www.drugbank.ca/drugs/DB00031 1/23 10/30/2018 Tenecteplase - DrugBank

Protein chemical formula

C2561H3919N747O781S40

Protein average weight 58951.2 Da

Sequences

>DB00031 sequence SYQVICRDEKTQMIYQQHQSWLRPVLRSNRVEYCWCNSGRAQCHSVPVKSCSEPRCFNGG TCQQALYFSDFVCQCPEGFAGKCCEIDTRATCYEDQGISYRGNWSTAESGAECTNWQSSA LAQKPYSGRRPDAIRLGLGNHNYCRNPDRDSKPWCYVFKAGKYSSEFCSTPACSEGNSDC YFGNGSAYRGTHSLTESGASCLPWNSMILIGKVYTAQNPSAQALGLGKHNYCRNPDGDAK PWCHVLKNRRLTWEYCDVPSCSTCGLRQYSQPQFRIKGGLFADIASHPWQAAIFAAAAAS PGERFLCGGILISSCWILSAAHCFQERFPPHHLTVILGRTYRVVPGEEEQKFEVEKYIVH KEFDDDTYDNDIALLQLKSDSSRCAQESSVVRTVCLPPADLQLPDWTECELSGYGKHEAL SPFYSERLKEAHVRLYPSSRCTSQHLLNRTVTDNMLCAGDTRSGGPQANLHDACQGDSGG PLVCLNDGRMTLVGIISWGLGCGQKDVPGVYTKVTNYLDWIRDNMRP

Download FASTA Format

Synonyms

TNK-tPA

Prescription Products

MARKETING MARKETING NAME ↑↓ DOSAGE ↑↓ STRENGTH ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓

Metalyse Injection, 10000 units Intravenous Boehringer 2001-02-23 Not applicable powder, for Ingelheim solution

Metalyse Injection, 8000 units Intravenous Boehringer 2001-02-23 Not applicable powder, for Ingelheim solution

TNKase Kit 52.5 Genentech, 2000-06-02 Not applicable https://www.drugbank.ca/drugs/DB00031 2/23 10/30/2018 Tenecteplase - DrugBank

mg/50mg Inc. MARKETING MARKETING NAME ↑↓ DOSAGE ↑↓ STRENGTH ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓

TNKase Powder, for 50 mg Intravenous Hoﬀmann La 2001-10-18 Not applicable solution Roche

Showing 1 to 4 of 4 entries ‹ ›

Mixture Products

MARKETING MARKETING NAME ↑↓ INGREDIENTS DOSAGE ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓

TNKase Tenecteplase Kit Genentech, 2000-06-02 2014-06-30 (50 Inc. mg/10mL) + Isopropyl Alcohol (0.7 mL/1mL)

Showing 1 to 1 of 1 entries ‹ ›

Categories

Agents causing angioedema

Amino Acids, Peptides, and Proteins

Anticoagulants

Biological Factors

Blood and Blood Forming Organs

Blood Proteins

Cardiovascular Agents

Endopeptidases

Enzymes

Enzymes and Coenzymes

Fibrin Modulating Agents https://www.drugbank.ca/drugs/DB00031 3/23 10/30/2018 Tenecteplase - DrugBank

Fibrinolytic Agents

Hematologic Agents

Hydrolases

Peptide Hydrolases

Plasminogen Activators

Proteins

Serine Endopeptidases

Serine Proteases

UNII

WGD229O42W

CAS number

191588-94-0

PHARMACOLOGY

Indication

For treatment of myocardial infarction and lysis of intracoronary emboli

Associated Conditions

ST Elevation Myocardial Infarction (STEMI)

Pharmacodynamics

Tenecteplase is a fibrin-specific tissue-plasminogen activator. It binds to fibrin rich clots and cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.

Mechanism of action Tenecteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.

https://www.drugbank.ca/drugs/DB00031 4/23 10/30/2018 Tenecteplase - DrugBank

A Plasminogen

activator

Human

A Fibrinogen alpha chain

Not Available

Human

U Urokinase plasminogen activator surface receptor

Not Available

Human

U Plasminogen activator inhibitor 1

Not Available

Human

U Plasminogen activator inhibitor 2

Not Available

Human

U Tetranectin

Not Available

Human

U Keratin, type II cytoskeletal 8

Not Available

Human

U Annexin A2

Not Available

Human

U Calreticulin

Not Available

Human

U Calnexin

Not Available

Human

U Prolow-density lipoprotein receptor-related protein 1

Not Available

Human https://www.drugbank.ca/drugs/DB00031 5/23 10/30/2018 Tenecteplase - DrugBank

Absorption Not Available

Volume of distribution Not Available

Protein binding Not Available

Metabolism Not Available

Route of elimination

Not Available

Half life

1.9 hours (mammalian reticulocytes, in vitro) >20 hours (yeast, in vivo) >10 hours (Escherichia coli, in vivo)

Clearance

99 - 119 mL/min [acute myocardial infarction patients]

Toxicity

Not Available

Aﬀected organisms

Humans and other mammals

Pathways

Tenecteplase Action Pathway

Drug action

Pharmacogenomic Eﬀects/ADRs

Not Available

INTERACTIONS https://www.drugbank.ca/drugs/DB00031 6/23 10/30/2018 Tenecteplase - DrugBank

Drug Interactions

ALL DRUGS APPROVED VET APPROVED NUTRACEUTICAL ILLICIT WITHDRAWN

INVESTIGATIONAL EXPERIMENTAL

DRUG ↑↓ INTERACTION ↑↓ (1,2,6,7-3H)Testosterone The therapeutic eﬃcacy of Tenecteplase can be increased when used in combination with (1,2,6,7-3H)Testosterone.

(R)-warfarin The risk or severity of bleeding can be increased when Tenecteplase is combined with (R)-warfarin.

(S)-Warfarin The risk or severity of bleeding can be increased when Tenecteplase is combined with (S)-Warfarin.

1-Testosterone The therapeutic eﬃcacy of Tenecteplase can be increased when used in combination with 1-Testosterone.

18-methyl-19- The therapeutic eﬃcacy of Tenecteplase can be increased when used in nortestosterone combination with 18-methyl-19-nortestosterone.

4-hydroxycoumarin The risk or severity of bleeding can be increased when Tenecteplase is combined with 4-hydroxycoumarin.

4-Hydroxytestosterone The therapeutic eﬃcacy of Tenecteplase can be increased when used in combination with 4-Hydroxytestosterone.

5beta-dihydrotestosterone The therapeutic eﬃcacy of Tenecteplase can be increased when used in combination with 5beta-dihydrotestosterone.

Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Tenecteplase.

Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Tenecteplase.

Showing 1 to 10 of 583 entries ‹ ›

Food Interactions Not Available

REFERENCES

General References https://www.drugbank.ca/drugs/DB00031 7/23 10/30/2018 Tenecteplase - DrugBank

1. Gurbel PA, Hayes K, Bliden KP, Yoho J, Tantry US: The platelet-related effects of tenecteplase versus alteplase versus reteplase. Blood Coagul Fibrinolysis. 2005 Jan;16(1):1-7. [PubMed:15650539] 2. Melzer C, Richter C, Rogalla P, Borges AC, Theres H, Baumann G, Laule M: Tenecteplase for the treatment of massive and submassive pulmonary embolism. J Thromb Thrombolysis. 2004 Aug;18(1):47-50. [PubMed:15744554] 3. Ohman EM, Van de Werf F, Antman EM, Califf RM, de Lemos JA, Gibson CM, Oliverio RL, Harrelson L, McCabe C, DiBattiste P, Braunwald E: Tenecteplase and tirofiban in ST-segment elevation acute myocardial infarction: results of a randomized trial. Am Heart J. 2005 Jul;150(1):79-88. [PubMed:16084152] 4. De Luca G, Suryapranata H, Chiariello M: Tenecteplase followed by immediate angioplasty is more effective than tenecteplase alone for people with STEMI. Commentary. Evid Based Cardiovasc Med. 2005 Dec;9(4):284- 7. Epub 2005 Nov 2. [PubMed:16380055] 5. Authors unspecified: Primary versus tenecteplase-facilitated percutaneous coronary intervention in patients with ST-segment elevation acute myocardial infarction (ASSENT-4 PCI): randomised trial. Lancet. 2006 Feb 18;367(9510):569-78. [PubMed:16488800]

External Links UniProt P00750

Genbank L00153

KEGG Drug D06070

PubChem Substance 46508657

ChEMBL CHEMBL2108791

Therapeutic Targets Database DAP000204

PharmGKB PA164776757

RxList RxList Drug Page

Drugs.com Drugs.com Drug Page

Wikipedia

Tenecteplase https://www.drugbank.ca/drugs/DB00031 8/23 10/30/2018 p Tenecteplase - DrugBank

ATC Codes B01AD11 — Tenecteplase B01AD — Enzymes B01A — ANTITHROMBOTIC AGENTS B01 — ANTITHROMBOTIC AGENTS B — BLOOD AND BLOOD FORMING ORGANS

AHFS Codes

20:12.20 — Thrombolytic Agents

CLINICAL TRIALS

Clinical Trials

PHASE ↑↓ STATUS ↑↓ PURPOSE ↑↓ CONDITIONS ↑↓ COUNT ↑↓ 1 Withdrawn Treatment Acute Respiratory Distress Syndrome (ARDS) 1

1, 2 Terminated Treatment Acute Myelogenous Leukaemia (AML) / 1 Myelodysplastic Syndrome

2 Active Not Treatment Stroke, Ischemic 1 Recruiting

2 Completed Treatment Acute Myocardial Infarction (AMI) 1

2 Completed Treatment Cerebral Infarctions / Ischemia, Brain / Strokes 1

2 Completed Treatment Stroke, Ischemic 1

2 Completed Treatment Strokes 1

2 Recruiting Treatment Stroke, Ischemic 1

2 Terminated Treatment Leukemias 1

2 Terminated Treatment Pulmonary Embolism (PE) 1

Showing 1 to 10 of 34 entries ‹ ›

PHARMACOECONOMICS

Manufacturers

Not Available https://www.drugbank.ca/drugs/DB00031 9/23 10/30/2018 Tenecteplase - DrugBank

Packagers

F Hoﬀmann-La Roche Ltd.

Genentech Inc.

Dosage forms

FORM ↑↓ ROUTE ↑↓ STRENGTH ↑↓ Injection, powder, for solution Intravenous 10000 units

Injection, powder, for solution Intravenous 8000 units

Kit

Kit 52.5 mg/50mg

Powder, for solution Intravenous 50 mg

Showing 1 to 5 of 5 entries ‹ ›

Prices

UNIT DESCRIPTION ↑↓ COST ↑↓ UNIT ↑↓ Tnkase 50 mg kit 3238.76USD kit

Showing 1 to 1 of 1 entries ‹ ›

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

PATENT NUMBER ↑↓ PEDIATRIC EXTENSION ↑↓ APPROVED ↑↓ EXPIRES (ESTIMATED) ↑↓ ↑↓

CA2129660 No 2005-06-28 2013-05-28

CA1341432 No 2003-06-17 2020-06-17

https://www.drugbank.ca/drugs/DB00031 10/23 10/30/2018 Tenecteplase - DrugBank Showing 1 to 2 of 2 entries ‹ ›

PROPERTIES

State

Liquid

Experimental Properties

PROPERTY VALUE SOURCE

melting point (°C) 60 °C Novokhatny, V.V. et al., J. Biol. Chem. 266:12994-123002 (1991)

hydrophobicity -0.528 Not Available

isoelectric point 7.61 Not Available

TAXONOMY

Description Not Available

Kingdom Organic Compounds

Super Class Organic Acids

Class Carboxylic Acids and Derivatives

Sub Class

Amino Acids, Peptides, and Analogues

Direct Parent

Peptides

Alternative Parents

Not Available

https://www.drugbank.ca/drugs/DB00031 11/23 10/30/2018 Tenecteplase - DrugBank Substituents

Not Available

Molecular Framework Not Available

External Descriptors Not Available

TARGETS

1. Plasminogen

Kind Protein

Organism Human

Pharmacological action

Yes

Actions

Activator General Function Serine-type peptidase activity

Specific Function Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In...

Gene Name PLG

Uniprot ID P00747

Uniprot Name Plasminogen https://www.drugbank.ca/drugs/DB00031 12/23 10/30/2018 Tenecteplase - DrugBank Molecular Weight 90568.415 Da

References

1. Longstaﬀ C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. [PubMed:18673235] 2. Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. [PubMed:19436656] 3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST- segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464] 4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

2. Fibrinogen alpha chain

Kind

Protein

Organism

Human

Pharmacological action

Yes General Function Structural molecule activity

Specific Function Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function ...

Gene Name FGA

Uniprot ID P02671

Uniprot Name Fibrinogen alpha chain https://www.drugbank.ca/drugs/DB00031 13/23 10/30/2018 Tenecteplase - DrugBank

Molecular Weight

94972.455 Da

References

1. Melandri G, Vagnarelli F, Calabrese D, Semprini F, Nanni S, Branzi A: Review of tenecteplase (TNKase) in the treatment of acute myocardial infarction. Vasc Health Risk Manag. 2009;5(1):249-56. Epub 2009 Apr 8. [PubMed:19436656] 2. Longstaﬀ C, Williams S, Thelwell C: Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23. [PubMed:18673235] 3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST- segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464]

3. Urokinase plasminogen activator surface receptor

Kind Protein

Organism Human

Pharmacological action

Unknown General Function

Urokinase plasminogen activator receptor activity

Speciﬁc Function Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation eﬀects of U-...

Gene Name

PLAUR

Uniprot ID Q03405

Uniprot Name Urokinase plasminogen activator surface receptor

Molecular Weight https://www.drugbank.ca/drugs/DB00031 14/23 10/30/2018 Tenecteplase - DrugBank 36977.62 Da

References

1. Maupas-Schwalm F, Auge N, Robinet C, Cambus JP, Parsons SJ, Salvayre R, Negre-Salvayre A: The sphingomyelin/ceramide pathway is involved in ERK1/2 phosphorylation, cell proliferation, and uPAR overexpression induced by tissue-type plasminogen activator. FASEB J. 2004 Sep;18(12):1398- 400. Epub 2004 Jul 1. [PubMed:15231724] 2. Bankl HC, Samorapoompichit P, Pikula B, Latinovic L, Bankl H, Lechner K, Valent P: Characterization of human prostate mast cells and their increase in periprostatic vein thrombosis. Am J Clin Pathol. 2001 Jul;116(1):97-106. [PubMed:11447759] 3. Ferrier CM, Van Geloof WL, Straatman H, Van De Molengra FJ, Van Muijen GN, Ruiter DJ: Spitz naevi may express components of the plasminogen activation system. J Pathol. 2002 Sep;198(1):92-9. [PubMed:12210068]

4. Plasminogen activator inhibitor 1

Kind Protein

Organism Human

Pharmacological action

Unknown General Function Serine-type endopeptidase inhibitor activity

Speciﬁc Function Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major con...

Gene Name SERPINE1

Uniprot ID P05121

Uniprot Name Plasminogen activator inhibitor 1

Molecular Weight https://www.drugbank.ca/drugs/DB00031 15/23 10/30/2018 Tenecteplase - DrugBank 45059.695 Da

References

1. Lindberg P, Kinnby B, Lecander I, Lang NP, Matsson L: Increasing expression of tissue plasminogen activator and plasminogen activator inhibitor type 2 in dog gingival tissues with progressive inﬂammation. Arch Oral Biol. 2001 Jan;46(1):23-31. [PubMed:11163592] 2. Hattori M, Azami Y: Searching for preventive measures of cardiovascular events in aged Japanese taxi drivers--the daily rhythm of cardiovascular risk factors during a night duty day. J Hum Ergol (Tokyo). 2001 Dec;30(1-2):321-6. [PubMed:14564902] 3. Hilleman DE, Tsikouris JP, Seals AA, Marmur JD: Fibrinolytic agents for the management of ST- segment elevation myocardial infarction. Pharmacotherapy. 2007 Nov;27(11):1558-70. [PubMed:17963464]

5. Plasminogen activator inhibitor 2

Kind Protein

Organism

Human

Pharmacological action

Unknown General Function

Serine-type endopeptidase inhibitor activity

Speciﬁc Function Inhibits urokinase-type plasminogen activator. The monocyte derived PAI-2 is distinct from the endothelial cell-derived PAI-1.

Gene Name SERPINB2

Uniprot ID P05120

Uniprot Name Plasminogen activator inhibitor 2

Molecular Weight 46595.84 Da

https://www.drugbank.ca/drugs/DB00031 16/23 10/30/2018 Tenecteplase - DrugBank References

1. Verkleij-Hagoort AC, Ursem NT, Hop WC, Geurts-Moespot A, Steegers EA, Sweep FC, Steegers- Theunissen RP: Complex congenital malformations and the impact of the plasminogen activator system and beta-hCG in amniotic fluid. Eur J Obstet Gynecol Reprod Biol. 2007 Nov;135(1):47-52. Epub 2006 Dec 1. [PubMed:17141398] 2. Bremer HA, Brommer EJ, Wallenburg HC: Effects of labor and delivery on fibrinolysis. Eur J Obstet Gynecol Reprod Biol. 1994 Jun 30;55(3):163-8. [PubMed:7958159] 3. Stump DC, Thienpont M, Collen D: Purification and characterization of a novel inhibitor of urokinase from human urine. Quantitation and preliminary characterization in plasma. J Biol Chem. 1986 Sep 25;261(27):12759-66. [PubMed:3091604]

6. Tetranectin

Kind Protein

Organism Human

Pharmacological action

Unknown General Function Kringle domain binding

Speciﬁc Function Tetranectin binds to plasminogen and to isolated kringle 4. May be involved in the packaging of molecules destined for exocytosis.

Gene Name CLEC3B

Uniprot ID P05452

Uniprot Name Tetranectin

Molecular Weight 22536.665 Da

References

https://www.drugbank.ca/drugs/DB00031 17/23 10/30/2018 Tenecteplase - DrugBank

1. Westergaard UB, Andersen MH, Heegaard CW, Fedosov SN, Petersen TE: Tetranectin binds hepatocyte growth factor and tissue-type plasminogen activator. Eur J Biochem. 2003 Apr;270(8):1850-4. [PubMed:12694198] 2. Kamper EF, Kopeikina LT, Koutsoukos V, Stavridis J: Plasma tetranectin levels and disease activity in patients with rheumatoid arthritis. J Rheumatol. 1997 Feb;24(2):262-8. [PubMed:9034981] 3. Vuckovic B, Deric M: [Lipoprotein(a): a link between thrombogenesis and atherogenesis]. Med Pregl. 2007 Jan-Feb;60(1-2):37-41. [PubMed:17853709]

7. Keratin, type II cytoskeletal 8

Kind

Protein

Organism Human

Pharmacological action

Unknown General Function Structural molecule activity

Speciﬁc Function Together with KRT19, helps to link the contractile apparatus to dystrophin at the costameres of striated muscle.

Gene Name KRT8

Uniprot ID P05787

Uniprot Name

Keratin, type II cytoskeletal 8

Molecular Weight

53703.76 Da

References

1. Kralovich KR, Li L, Hembrough TA, Webb DJ, Karns LR, Gonias SL: Characterization of the binding sites for plasminogen and tissue-type plasminogen activator in cytokeratin 8 and cytokeratin 18. J Protein Chem. 1998 Nov;17(8):845-54. [PubMed:9988531] https://www.drugbank.ca/drugs/DB00031 18/23 10/30/2018 Tenecteplase - DrugBank 2. Hembrough TA, Kralovich KR, Li L, Gonias SL: Cytokeratin 8 released by breast carcinoma cells in vitro binds plasminogen and tissue-type plasminogen activator and promotes plasminogen activation. Biochem J. 1996 Aug 1;317 ( Pt 3):763-9. [PubMed:8760360] 3. Hembrough TA, Li L, Gonias SL: Cell-surface cytokeratin 8 is the major plasminogen receptor on breast cancer cells and is required for the accelerated activation of cell-associated plasminogen by tissue-type plasminogen activator. J Biol Chem. 1996 Oct 11;271(41):25684-91. [PubMed:8810346]

8. Annexin A2

Kind Protein

Organism Human

Pharmacological action

Unknown General Function S100 protein binding

Speciﬁc Function

Calcium-regulated membrane-binding protein whose aﬃnity for calcium is greatly enhanced by anionic phospholipids. It binds two calcium ions with high aﬃnity. May be involved in heat- stress resp...

Gene Name ANXA2

Uniprot ID P07355

Uniprot Name Annexin A2

Molecular Weight 38603.63 Da

References

1. Diaz VM, Hurtado M, Thomson TM, Reventos J, Paciucci R: Speciﬁc interaction of tissue-type plasminogen activator (t-PA) with annexin II on the membrane of pancreatic cancer cells activates plasminogen and promotes invasion in vitro. Gut. 2004 Jul;53(7):993-1000. [PubMed:15194650]

https://www.drugbank.ca/drugs/DB00031 19/23 10/30/2018 Tenecteplase - DrugBank 2. Kang HM, Choi KS, Kassam G, Fitzpatrick SL, Kwon M, Waisman DM: Role of annexin II tetramer in plasminogen activation. Trends Cardiovasc Med. 1999 Apr-May;9(3-4):92-102. [PubMed:10578524] 3. MacLeod TJ, Kwon M, Filipenko NR, Waisman DM: Phospholipid-associated annexin A2-S100A10 heterotetramer and its subunits: characterization of the interaction with tissue plasminogen activator, plasminogen, and plasmin. J Biol Chem. 2003 Jul 11;278(28):25577-84. Epub 2003 Apr 30. [PubMed:12730231]

9. Calreticulin

Kind Protein

Organism Human

Pharmacological action

Unknown General Function Zinc ion binding

Speciﬁc Function

Calcium-binding chaperone that promotes folding, oligomeric assembly and quality control in the endoplasmic reticulum (ER) via the calreticulin/calnexin cycle. This lectin interacts transiently wit...

Gene Name CALR

Uniprot ID

P27797

Uniprot Name Calreticulin

Molecular Weight 48141.2 Da

References

1. Allen S, Bulleid NJ: Calnexin and calreticulin bind to enzymically active tissue-type plasminogen activator during biosynthesis and are not required for folding to the native conformation. Biochem J. 1997 Nov 15;328 ( Pt 1):113-9. [PubMed:9359841]

https://www.drugbank.ca/drugs/DB00031 20/23 10/30/2018 Tenecteplase - DrugBank

10. Calnexin

Kind Protein

Organism Human

Pharmacological action

Unknown General Function Poly(a) rna binding

Speciﬁc Function

Calcium-binding protein that interacts with newly synthesized glycoproteins in the endoplasmic reticulum. It may act in assisting protein assembly and/or in the retention within the ER of unassembl...

Gene Name

CANX

Uniprot ID

P27824

Uniprot Name Calnexin

Molecular Weight 67567.695 Da

References

11. Prolow-density lipoprotein receptor-related protein 1

Kind

https://www.drugbank.ca/drugs/DB00031 21/23 10/30/2018 Tenecteplase - DrugBank Protein

Organism Human

Pharmacological action

Unknown General Function Receptor activity

Speciﬁc Function

Endocytic receptor involved in endocytosis and in phagocytosis of apoptotic cells. Required for early embryonic development. Involved in cellular lipid homeostasis. Involved in the plasma clearance...

Gene Name LRP1

Uniprot ID Q07954

Uniprot Name Prolow-density lipoprotein receptor-related protein 1

Molecular Weight 504601.695 Da

References

1. Moestrup SK, Nielsen S, Andreasen P, Jorgensen KE, Nykjaer A, Roigaard H, Gliemann J, Christensen EI: Epithelial glycoprotein-330 mediates endocytosis of plasminogen activator-plasminogen activator inhibitor type-1 complexes. J Biol Chem. 1993 Aug 5;268(22):16564-70. [PubMed:8344937] 2. Nykjaer A, Petersen CM, Moller B, Jensen PH, Moestrup SK, Holtet TL, Etzerodt M, Thogersen HC, Munch M, Andreasen PA, et al.: Puriﬁed alpha 2-macroglobulin receptor/LDL receptor-related protein binds urokinase.plasminogen activator inhibitor type-1 complex. Evidence that the alpha 2- macroglobulin receptor mediates cellular degradation of urokinase receptor-bound complexes. J Biol Chem. 1992 Jul 25;267(21):14543-6. [PubMed:1378833] 3. Hu K, Yang J, Tanaka S, Gonias SL, Mars WM, Liu Y: Tissue-type plasminogen activator acts as a cytokine that triggers intracellular signal transduction and induces matrix metalloproteinase-9 gene expression. J Biol Chem. 2006 Jan 27;281(4):2120-7. Epub 2005 Nov 22. [PubMed:16303771]

Drug created on June 13, 2005 07:24 / Updated on October 28, 2018 07:22 https://www.drugbank.ca/drugs/DB00031 22/23 10/30/2018 Tenecteplase - DrugBank

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This project is supported by the Canadian Institutes of Health Research (award #111062), Alberta Innovates - Health Solutions, and by The Metabolomics Innovation Centre (TMIC), a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by Genome Alberta, Genome British Columbia, and Genome Canada, a not-for-proﬁt organization that is leading Canada's national genomics strategy with funding from the federal government. Maintenance, support, and commercial licensing is provided by OMx Personal Health Analytics, Inc. Designed by Educe Design & Innovation Inc.

https://www.drugbank.ca/drugs/DB00031 23/23