Desmoteplase

Identification

Name
Desmoteplase
Accession Number
DB04925
Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Description

Desmoteplase is a chemical in the saliva of vampire bats. It activates plasminogen to the serine protease, plasmin. Plasmin acts by breaking down fibrin blood clots. When a vampire bat bites its victim, it secretes an enzyme that prevents the blood from clotting. The enzyme is called DSPA (Desmodus rotundus salivary plasminogen activator) and scientists are using DSPA as stroke and heart attack medication. Desmoteplase is a recombinant form of vampire bat DSPA (Salivary plasminogen activator alpha 1).

Protein chemical formula
Not Available
Protein average weight
Not Available
Sequences
>P98119|URT1_DESRO Salivary plasminogen activator alpha 1 precursor - Desmodus rotundus
MVNTMKTKLLCVLLLCGAVFSLPRQETYRQLARGSRAYGVACKDEITQMTYRRQESWLRP
EVRSKRVEHCQCDRGQARCHTVPVNSCSEPRCFNGGTCWQAVYFSDFVCQCPAGYTGKRC
EVDTRATCYEGQGVTYRGTWSTAESRVECINWNSSLLTRRTYNGRMPDAFNLGLGNHNYC
RNPNGAPKPWCYVIKAGKFTSESCSVPVCSKATCGLRKYKEPQLHSTGGLFTDITSHPWQ
AAIFAQNRRSSGERFLCGGILISSCWVLTAAHCFQESYLPDQLKVVLGRTYRVKPGEEEQ
TFKVKKYIVHKEFDDDTYNNDIALLQLKSDSPQCAQESDSVRAICLPEANLQLPDWTECE
LSGYGKHKSSSPFYSEQLKEGHVRLYPSSRCAPKFLFNKTVTNNMLCAGDTRSGEIYPNV
HDACQGDSGGPLVCMNDNHMTLLGIISWGVGCGEKDVPGVYTKVTNYLGWIRDNMHL
Download FASTA Format
Synonyms
  • Desmodus rotundus salivary plasminogen activator
  • DSPA
Categories
UNII
T36L245S3T
CAS number
145137-38-8

Pharmacology

Indication

Investigated for use/treatment in cerebral ischemia and strokes.

Structured Indications
Not Available
Pharmacodynamics

Desmoteplase is a novel thrombolytic agent derived from vampire-bat saliva. It is genetically related to the clot buster tissue plasminogen activator (t-PA) but is more potent and demonstrates a safer toxicity profile (desmoteplase does not promote kainate- or NMDA-mediated neurotoxicity in vivo). Plasminogen activators are enzymes found in all vertebrate species investigated so far. Their physiological function is the generation of localized proteolysis in the context of tissue remodeling, wound healing and neuronal plasticity.

Mechanism of action

Desmoteplase targets and destroys fibrin, the structural scaffold of blood clots.

TargetActionsOrganism
UPlasminogenNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabDesmoteplase may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolDesmoteplase may increase the anticoagulant activities of Acenocoumarol.Approved, Investigational
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Desmoteplase.Approved, Vet Approved
AloxiprinThe risk or severity of adverse effects can be increased when Aloxiprin is combined with Desmoteplase.Experimental
AlprostadilAlprostadil may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Desmoteplase.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Desmoteplase.Approved
AncrodDesmoteplase may increase the anticoagulant activities of Ancrod.Approved, Investigational
AndrographolideAndrographolide may increase the anticoagulant activities of Desmoteplase.Investigational
Antithrombin III humanDesmoteplase may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanDesmoteplase may increase the anticoagulant activities of Apixaban.Approved
AprotininThe therapeutic efficacy of Desmoteplase can be decreased when used in combination with Aprotinin.Approved, Investigational, Withdrawn
ArdeparinDesmoteplase may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanDesmoteplase may increase the anticoagulant activities of Argatroban.Approved, Investigational
AzelastineAzelastine may increase the anticoagulant activities of Desmoteplase.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Desmoteplase.Approved, Investigational
BecaplerminDesmoteplase may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BeraprostBeraprost may increase the anticoagulant activities of Desmoteplase.Investigational
BivalirudinDesmoteplase may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BuflomedilBuflomedil may increase the anticoagulant activities of Desmoteplase.Experimental
ButylphthalideButylphthalide may increase the anticoagulant activities of Desmoteplase.Investigational
CangrelorCangrelor may increase the anticoagulant activities of Desmoteplase.Approved
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Desmoteplase.Experimental, Investigational
CertoparinDesmoteplase may increase the anticoagulant activities of Certoparin.Approved, Investigational
CilostazolCilostazol may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
Citric AcidDesmoteplase may increase the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Desmoteplase.Approved
CloricromenCloricromen may increase the anticoagulant activities of Desmoteplase.Experimental
Dabigatran etexilateDesmoteplase may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinDesmoteplase may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidDesmoteplase may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanDesmoteplase may increase the anticoagulant activities of Darexaban.Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
DersalazineThe risk or severity of adverse effects can be increased when Dersalazine is combined with Desmoteplase.Investigational
DesirudinDesmoteplase may increase the anticoagulant activities of Desirudin.Approved
DextranDesmoteplase may increase the anticoagulant activities of Dextran.Approved, Investigational, Vet Approved
Dextran 40Desmoteplase may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Desmoteplase may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Desmoteplase may increase the anticoagulant activities of Dextran 75.Approved
DicoumarolDesmoteplase may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Desmoteplase.Approved, Investigational
DipyridamoleDipyridamole may increase the anticoagulant activities of Desmoteplase.Approved
Edetic AcidDesmoteplase may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanDesmoteplase may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinDesmoteplase may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
EplivanserinEplivanserin may increase the anticoagulant activities of Desmoteplase.Investigational
eplivanserineeplivanserine may increase the anticoagulant activities of Desmoteplase.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Desmoteplase.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
Ethyl biscoumacetateDesmoteplase may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ferulic acidDesmoteplase may increase the anticoagulant activities of Ferulic acid.Experimental
FluindioneDesmoteplase may increase the anticoagulant activities of Fluindione.Approved, Investigational
FondaparinuxDesmoteplase may increase the anticoagulant activities of Fondaparinux.Approved, Investigational
Fondaparinux sodiumDesmoteplase may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateDesmoteplase may increase the anticoagulant activities of Gabexate.Investigational
GuacetisalThe risk or severity of adverse effects can be increased when Guacetisal is combined with Desmoteplase.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Desmoteplase.Experimental
HeparinDesmoteplase may increase the anticoagulant activities of Heparin.Approved, Investigational
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Desmoteplase.Investigational
IbudilastIbudilast may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Desmoteplase.Approved, Investigational, Nutraceutical
IdraparinuxDesmoteplase may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Desmoteplase.Approved, Investigational, Withdrawn
IfetrobanIfetroban may increase the anticoagulant activities of Desmoteplase.Investigational
IloprostIloprost may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
IndobufenIndobufen may increase the anticoagulant activities of Desmoteplase.Investigational
KetanserinKetanserin may increase the anticoagulant activities of Desmoteplase.Investigational
LepirudinDesmoteplase may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanDesmoteplase may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Desmoteplase.Approved, Investigational
LinsidomineLinsidomine may increase the anticoagulant activities of Desmoteplase.Experimental
MelagatranDesmoteplase may increase the anticoagulant activities of Melagatran.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Desmoteplase.Approved
Methyl salicylateThe risk or severity of adverse effects can be increased when Methyl salicylate is combined with Desmoteplase.Approved, Vet Approved
MilrinoneMilrinone may increase the anticoagulant activities of Desmoteplase.Approved
NadroparinDesmoteplase may increase the anticoagulant activities of Nadroparin.Approved, Investigational
NafamostatDesmoteplase may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Desmoteplase.Investigational
NimesulideNimesulide may increase the anticoagulant activities of Desmoteplase.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Desmoteplase.Investigational
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Desmoteplase.Approved
OtamixabanDesmoteplase may increase the anticoagulant activities of Otamixaban.Investigational
Pentaerythritol TetranitrateDesmoteplase may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
Pentosan PolysulfateDesmoteplase may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
PhenindioneDesmoteplase may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonDesmoteplase may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PicotamidePicotamide may increase the anticoagulant activities of Desmoteplase.Experimental
PrasugrelPrasugrel may increase the anticoagulant activities of Desmoteplase.Approved
Protein CDesmoteplase may increase the anticoagulant activities of Protein C.Approved
Protein S humanDesmoteplase may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeDesmoteplase may increase the anticoagulant activities of Protocatechualdehyde.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Desmoteplase.Investigational
RelcovaptanRelcovaptan may increase the anticoagulant activities of Desmoteplase.Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Desmoteplase.Approved, Experimental, Investigational
ReviparinDesmoteplase may increase the anticoagulant activities of Reviparin.Approved, Investigational
RidogrelRidogrel may increase the anticoagulant activities of Desmoteplase.Approved
RivaroxabanDesmoteplase may increase the anticoagulant activities of Rivaroxaban.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Desmoteplase.Approved, Investigational, Vet Approved
SarpogrelateSarpogrelate may increase the anticoagulant activities of Desmoteplase.Investigational
SevofluraneSevoflurane may increase the anticoagulant activities of Desmoteplase.Approved, Vet Approved
SRT501SRT501 may increase the anticoagulant activities of Desmoteplase.Investigational
SulodexideDesmoteplase may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TesmilifeneTesmilifene may increase the anticoagulant activities of Desmoteplase.Investigational
TicagrelorTicagrelor may increase the anticoagulant activities of Desmoteplase.Approved
TiclopidineTiclopidine may increase the anticoagulant activities of Desmoteplase.Approved
TirofibanTirofiban may increase the anticoagulant activities of Desmoteplase.Approved
TranilastTranilast may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Desmoteplase.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Desmoteplase is combined with Treprostinil.Approved, Investigational
TriflusalTriflusal may increase the anticoagulant activities of Desmoteplase.Approved, Investigational
Trolamine salicylateThe risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Desmoteplase.Approved
TroxerutinDesmoteplase may increase the anticoagulant activities of Troxerutin.Investigational
VorapaxarVorapaxar may increase the anticoagulant activities of Desmoteplase.Approved
WarfarinDesmoteplase may increase the anticoagulant activities of Warfarin.Approved
XimelagatranDesmoteplase may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Food Interactions
Not Available

References

General References
  1. Grandjean C, McMullen PC, Newschwander G: Vampire bats yield potent clot buster for ischemic stroke. J Cardiovasc Nurs. 2004 Nov-Dec;19(6):417-20. [PubMed:15529064]
  2. Hacke W, Albers G, Al-Rawi Y, Bogousslavsky J, Davalos A, Eliasziw M, Fischer M, Furlan A, Kaste M, Lees KR, Soehngen M, Warach S: The Desmoteplase in Acute Ischemic Stroke Trial (DIAS): a phase II MRI-based 9-hour window acute stroke thrombolysis trial with intravenous desmoteplase. Stroke. 2005 Jan;36(1):66-73. Epub 2004 Nov 29. [PubMed:15569863]
  3. Schleuning WD: Vampire bat plasminogen activator DSPA-alpha-1 (desmoteplase): a thrombolytic drug optimized by natural selection. Haemostasis. 2001 May-Dec;31(3-6):118-22. [PubMed:11910176]
  4. Liberatore GT, Samson A, Bladin C, Schleuning WD, Medcalf RL: Vampire bat salivary plasminogen activator (desmoteplase): a unique fibrinolytic enzyme that does not promote neurodegeneration. Stroke. 2003 Feb;34(2):537-43. [PubMed:12574572]
  5. Reddrop C, Moldrich RX, Beart PM, Farso M, Liberatore GT, Howells DW, Petersen KU, Schleuning WD, Medcalf RL: Vampire bat salivary plasminogen activator (desmoteplase) inhibits tissue-type plasminogen activator-induced potentiation of excitotoxic injury. Stroke. 2005 Jun;36(6):1241-6. Epub 2005 May 5. [PubMed:15879331]
  6. Hoffmann JJ, Kops O: Inhibition of desmoteplase-induced fibrinolytic activity in vitro. J Thromb Thrombolysis. 2005 Aug;20(1):23-6. [PubMed:16133891]
  7. Furlan AJ, Eyding D, Albers GW, Al-Rawi Y, Lees KR, Rowley HA, Sachara C, Soehngen M, Warach S, Hacke W: Dose Escalation of Desmoteplase for Acute Ischemic Stroke (DEDAS): evidence of safety and efficacy 3 to 9 hours after stroke onset. Stroke. 2006 May;37(5):1227-31. Epub 2006 Mar 30. [PubMed:16574922]
External Links
UniProt
P98119
PubChem Substance
347909849
Wikipedia
Desmoteplase

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1, 2CompletedTreatmentStrokes1
2CompletedTreatmentAcute Ischemic Stroke (AIS)1
2CompletedTreatmentStrokes1
3CompletedTreatmentStroke, Acute1
3CompletedTreatmentStrokes1
3TerminatedTreatmentStrokes1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
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
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
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
Molecular Weight
90568.415 Da
References
  1. Dafer RM, Biller J: Desmoteplase in the treatment of acute ischemic stroke. Expert Rev Neurother. 2007 Apr;7(4):333-7. [PubMed:17425487]

Drug created on October 21, 2007 16:23 / Updated on February 03, 2018 13:57