Aprotinin

Identification

Name
Aprotinin
Accession Number
DB06692
Type
Biotech
Groups
Approved, Withdrawn
Biologic Classification
Protein Based Therapies
Other protein based therapies
Description

Aprotinin, also known as bovine pancreatic trypsin inhibitor, BPTI (Trasylol, Bayer) is a protein, that is used as medication administered by injection to reduce bleeding during complex surgery, such as heart and liver surgery. Its main effect is the slowing down of fibrinolysis, the process that leads to the breakdown of blood clots. The aim in its use is to decrease the need for blood transfusions during surgery, as well as end-organ damage due to hypotension (low blood pressure) as a result of marked blood loss. The drug was temporarily withdrawn worldwide in 2007 after studies suggested that its use increased the risk of complications or death; after this was confirmed by follow-up studies, Trasylol was entirely and permanently withdrawn in May 2008, except - at least for the time being - for very restricted research use. [Wikipedia]

Protein structure
Db06692
Protein chemical formula
C284H432N84O79S7
Protein average weight
6511.439 Da
Sequences
>Aprotinin (bovine pancreatic trypsin inhibitor)
RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA
Download FASTA Format
Synonyms
  • Aprotinin (bovine)
  • Aprotinin Biosynthetic
  • Aprotinin Bovine
  • Aprotinin Concentrated Solution
  • Bovine Aprotinin
  • Bovine Pancreatic Trypsin Inhibitor
  • BPTI
  • Fibrinolysis Inhibitor
  • Trypsin Inhibitor, Pancreatic Basic
External IDs
232-994-9 / Bayer A 128 / Bayer-A-128 / Riker-52G / RP-9921
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
TrasylolSolution10000 unitIntravenousNordic Group Bv1997-12-15Not applicableCanada
Trasylol Inj 10000 Kiu/mlLiquid100000 unitIntravenousMiles Inc. Pharmaceutical Division1981-12-311998-09-25Canada
Categories
UNII
04XPW8C0FL
CAS number
9087-70-1

Pharmacology

Indication

For prophylactic use to reduce perioperative blood loss and the need for blood transfusion in patients undergoing cardiopulmonary bypass in the course of coronary artery bypass graft surgery who are at an increased risk for blood loss and blood transfusion.

Structured Indications
Not Available
Pharmacodynamics

Aprotinin is a broad spectrum protease inhibitor which modulates the systemic inflammatory response (SIR) associated with cardiopulmonary bypass (CPB) surgery. SIR results in the interrelated activation of the hemostatic, fibrinolytic, cellular and humoral inflammatory systems. Aprotinin, through its inhibition of multiple mediators [e.g., kallikrein, plasmin] results in the attenuation of inflammatory responses, fibrinolysis, and thrombin generation. Aprotinin inhibits pro-inflammatory cytokine release and maintains glycoprotein homeostasis. In platelets, aprotinin reduces glycoprotein loss (e.g., GpIb, GpIIb/IIIa), while in granulocytes it prevents the expression of pro-inflammatory adhesive glycoproteins (e.g., CD11b). The effects of aprotinin use in CPB involves a reduction in inflammatory response which translates into a decreased need for allogeneic blood transfusions, reduced bleeding, and decreased mediastinal re-exploration for bleeding.

Mechanism of action

Aprotinin inhibits several serine proteases, specifically trypsin, chymotrypsin and plasmin at a concentration of about 125,000 IU/ml, and kallikrein at 300,000 IU/ml. Its action on kallikrein leads to the inhibition of the formation of factor XIIa. As a result, both the intrinsic pathway of coagulation and fibrinolysis are inhibited. Its action on plasmin independently slows fibrinolysis.

TargetActionsOrganism
UTrypsin-1Not AvailableHuman
UChymotrypsinogen BNot AvailableHuman
UPlasminogenNot AvailableHuman
UKallikrein-1Not AvailableHuman
Absorption

100% (IV)

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Aprotinin is slowly degraded by lysosomal enzymes.

Route of elimination

Following a single IV dose of radiolabelled aprotinin, approximately 25-40% of the radioactivity is excreted in the urine over 48 hours. After a 30 minute infusion of 1 million KIU, about 2% is excreted as unchanged drug. After a larger dose of 2 million KIU infused over 30 minutes, urinary excretion of unchanged aprotinin accounts for approximately 9% of the dose.

Half life

Following this distribution phase, a plasma half-life of about 150 minutes is observed. At later time points, (i.e., beyond 5 hours after dosing) there is a terminal elimination phase with a half-life of about 10 hours.

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Aprotinin Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Aprotinin.Approved, Investigational
AbciximabThe therapeutic efficacy of Abciximab can be decreased when used in combination with Aprotinin.Approved
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be decreased when used in combination with Aprotinin.Approved
Acetylsalicylic acidThe therapeutic efficacy of Acetylsalicylic acid can be decreased when used in combination with Aprotinin.Approved, Vet Approved
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Aprotinin.Approved, Investigational
AloxiprinThe therapeutic efficacy of Aloxiprin can be decreased when used in combination with Aprotinin.Experimental
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Aprotinin.Approved, Illicit, Investigational
AlteplaseThe therapeutic efficacy of Alteplase can be decreased when used in combination with Aprotinin.Approved
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Aprotinin.Experimental, Investigational
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Aprotinin.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Aprotinin.Approved
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Aprotinin.Approved
AmoxapineThe serum concentration of Amoxapine can be increased when it is combined with Aprotinin.Approved
AnagrelideThe therapeutic efficacy of Anagrelide can be decreased when used in combination with Aprotinin.Approved
AncrodThe therapeutic efficacy of Ancrod can be decreased when used in combination with Aprotinin.Investigational
AnistreplaseThe therapeutic efficacy of Anistreplase can be decreased when used in combination with Aprotinin.Approved
Antithrombin III humanThe therapeutic efficacy of Antithrombin III human can be decreased when used in combination with Aprotinin.Approved
ApixabanThe therapeutic efficacy of Apixaban can be decreased when used in combination with Aprotinin.Approved
ArdeparinThe therapeutic efficacy of Ardeparin can be decreased when used in combination with Aprotinin.Approved, Investigational, Withdrawn
ArgatrobanThe therapeutic efficacy of Argatroban can be decreased when used in combination with Aprotinin.Approved, Investigational
AstaxanthinThe therapeutic efficacy of Astaxanthin can be decreased when used in combination with Aprotinin.Investigational
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Aprotinin.Approved
BatroxobinThe therapeutic efficacy of Batroxobin can be decreased when used in combination with Aprotinin.Experimental
BemiparinThe therapeutic efficacy of Bemiparin can be decreased when used in combination with Aprotinin.Approved, Investigational
BenazeprilAprotinin may decrease the antihypertensive activities of Benazepril.Approved, Investigational
BeraprostThe therapeutic efficacy of Beraprost can be decreased when used in combination with Aprotinin.Investigational
BivalirudinThe therapeutic efficacy of Bivalirudin can be decreased when used in combination with Aprotinin.Approved, Investigational
BoceprevirThe serum concentration of Aprotinin can be decreased when it is combined with Boceprevir.Approved, Withdrawn
BrinaseThe therapeutic efficacy of Brinase can be decreased when used in combination with Aprotinin.Experimental
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Aprotinin.Approved, Investigational
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Aprotinin.Approved
CandoxatrilAprotinin may decrease the antihypertensive activities of Candoxatril.Experimental
CangrelorThe therapeutic efficacy of Cangrelor can be decreased when used in combination with Aprotinin.Approved
CaplacizumabThe therapeutic efficacy of Caplacizumab can be decreased when used in combination with Aprotinin.Investigational
CaptoprilAprotinin may decrease the antihypertensive activities of Captopril.Approved
CarbamazepineThe metabolism of Aprotinin can be increased when combined with Carbamazepine.Approved, Investigational
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Aprotinin.Investigational, Withdrawn
CilazaprilAprotinin may decrease the antihypertensive activities of Cilazapril.Approved
CilostazolThe therapeutic efficacy of Cilostazol can be decreased when used in combination with Aprotinin.Approved
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Aprotinin.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Aprotinin.Approved, Vet Approved
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Aprotinin.Approved
CloricromenThe therapeutic efficacy of Cloricromen can be decreased when used in combination with Aprotinin.Experimental
ClorindioneThe therapeutic efficacy of Clorindione can be decreased when used in combination with Aprotinin.Experimental
Conjugated estrogensThe serum concentration of Conjugated estrogens can be decreased when it is combined with Aprotinin.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Aprotinin.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Aprotinin is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Aprotinin.Approved, Investigational, Vet Approved
Dabigatran etexilateThe therapeutic efficacy of Dabigatran etexilate can be decreased when used in combination with Aprotinin.Approved
DalteparinThe therapeutic efficacy of Dalteparin can be decreased when used in combination with Aprotinin.Approved
DanaparoidThe therapeutic efficacy of Danaparoid can be decreased when used in combination with Aprotinin.Approved, Withdrawn
DefibrotideThe therapeutic efficacy of Defibrotide can be decreased when used in combination with Aprotinin.Approved, Investigational
DelaprilAprotinin may decrease the antihypertensive activities of Delapril.Experimental
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Aprotinin.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Aprotinin.Approved
DesirudinThe therapeutic efficacy of Desirudin can be decreased when used in combination with Aprotinin.Approved
DesmoteplaseThe therapeutic efficacy of Desmoteplase can be decreased when used in combination with Aprotinin.Investigational
DibenzepinThe serum concentration of Dibenzepin can be increased when it is combined with Aprotinin.Experimental
DicoumarolThe therapeutic efficacy of Dicoumarol can be decreased when used in combination with Aprotinin.Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Aprotinin.Approved, Investigational
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Aprotinin.Approved, Investigational
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Aprotinin.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Aprotinin.Approved
DiphenadioneThe therapeutic efficacy of Diphenadione can be decreased when used in combination with Aprotinin.Experimental
DipyridamoleThe therapeutic efficacy of Dipyridamole can be decreased when used in combination with Aprotinin.Approved
DitazoleThe therapeutic efficacy of Ditazole can be decreased when used in combination with Aprotinin.Approved, Withdrawn
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Aprotinin.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Aprotinin.Approved
Drotrecogin alfaThe therapeutic efficacy of Drotrecogin alfa can be decreased when used in combination with Aprotinin.Approved, Investigational, Withdrawn
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Aprotinin.Approved
EnalaprilAprotinin may decrease the antihypertensive activities of Enalapril.Approved, Vet Approved
EnalaprilatAprotinin may decrease the antihypertensive activities of Enalaprilat.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Aprotinin.Approved, Investigational
EnoxaparinThe therapeutic efficacy of Enoxaparin can be decreased when used in combination with Aprotinin.Approved
EplivanserinThe therapeutic efficacy of Eplivanserin can be decreased when used in combination with Aprotinin.Investigational
eplivanserineThe therapeutic efficacy of eplivanserine can be decreased when used in combination with Aprotinin.Investigational
EpoprostenolThe therapeutic efficacy of Epoprostenol can be decreased when used in combination with Aprotinin.Approved
EptifibatideThe therapeutic efficacy of Eptifibatide can be decreased when used in combination with Aprotinin.Approved, Investigational
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Aprotinin.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Aprotinin.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Aprotinin.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Aprotinin.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Aprotinin.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Aprotinin.Approved
Ethyl biscoumacetateThe therapeutic efficacy of Ethyl biscoumacetate can be decreased when used in combination with Aprotinin.Withdrawn
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Aprotinin.Approved
Fibrinogen HumanThe risk or severity of adverse effects can be increased when Aprotinin is combined with Fibrinogen Human.Approved
FibrinolysinThe therapeutic efficacy of Fibrinolysin can be decreased when used in combination with Aprotinin.Investigational
FluindioneThe therapeutic efficacy of Fluindione can be decreased when used in combination with Aprotinin.Investigational
FondaparinuxThe therapeutic efficacy of Fondaparinux can be decreased when used in combination with Aprotinin.Investigational
FosinoprilAprotinin may decrease the antihypertensive activities of Fosinopril.Approved
GarlicThe serum concentration of Aprotinin can be decreased when it is combined with Garlic.Approved
HeparinThe therapeutic efficacy of Heparin can be decreased when used in combination with Aprotinin.Approved, Investigational
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Aprotinin.Withdrawn
HigenamineThe therapeutic efficacy of Higenamine can be decreased when used in combination with Aprotinin.Investigational
IloprostThe therapeutic efficacy of Iloprost can be decreased when used in combination with Aprotinin.Approved, Investigational
ImidaprilAprotinin may decrease the antihypertensive activities of Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Aprotinin.Approved
IndobufenThe therapeutic efficacy of Indobufen can be decreased when used in combination with Aprotinin.Investigational
IprindoleThe serum concentration of Iprindole can be increased when it is combined with Aprotinin.Experimental
LepirudinThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Aprotinin.Approved
LisinoprilAprotinin may decrease the antihypertensive activities of Lisinopril.Approved, Investigational
LofepramineThe serum concentration of Lofepramine can be increased when it is combined with Aprotinin.Experimental
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Aprotinin.Approved, Investigational
MelagatranThe therapeutic efficacy of Melagatran can be decreased when used in combination with Aprotinin.Experimental
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Aprotinin.Approved
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Aprotinin.Experimental
MethylergometrineThe serum concentration of Methylergometrine can be increased when it is combined with Aprotinin.Approved
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Aprotinin.Approved, Illicit
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Aprotinin.Approved
MoexiprilAprotinin may decrease the antihypertensive activities of Moexipril.Approved
NadroparinThe therapeutic efficacy of Nadroparin can be decreased when used in combination with Aprotinin.Approved
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Aprotinin.Approved, Withdrawn
NitroaspirinThe therapeutic efficacy of Nitroaspirin can be decreased when used in combination with Aprotinin.Investigational
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Aprotinin.Approved
OmapatrilatAprotinin may decrease the antihypertensive activities of Omapatrilat.Investigational
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Aprotinin.Investigational
OzagrelThe therapeutic efficacy of Ozagrel can be decreased when used in combination with Aprotinin.Investigational
ParnaparinThe therapeutic efficacy of Parnaparin can be decreased when used in combination with Aprotinin.Approved, Investigational
Pentaerythritol TetranitrateThe therapeutic efficacy of Pentaerythritol Tetranitrate can be decreased when used in combination with Aprotinin.Approved
PerindoprilAprotinin may decrease the antihypertensive activities of Perindopril.Approved
PethidineThe risk or severity of adverse effects can be increased when Aprotinin is combined with Pethidine.Approved
PhenindioneThe therapeutic efficacy of Phenindione can be decreased when used in combination with Aprotinin.Approved, Investigational
PhenprocoumonThe therapeutic efficacy of Phenprocoumon can be decreased when used in combination with Aprotinin.Approved, Investigational
PicotamideThe therapeutic efficacy of Picotamide can be decreased when used in combination with Aprotinin.Experimental
PrasugrelThe therapeutic efficacy of Prasugrel can be decreased when used in combination with Aprotinin.Approved
Protein CThe therapeutic efficacy of Protein C can be decreased when used in combination with Aprotinin.Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Aprotinin.Approved
QuinaprilAprotinin may decrease the antihypertensive activities of Quinapril.Approved, Investigational
RamiprilAprotinin may decrease the antihypertensive activities of Ramipril.Approved
RescinnamineAprotinin may decrease the antihypertensive activities of Rescinnamine.Approved
ReteplaseThe therapeutic efficacy of Reteplase can be decreased when used in combination with Aprotinin.Approved
ReviparinThe therapeutic efficacy of Reviparin can be decreased when used in combination with Aprotinin.Approved, Investigational
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Aprotinin.Approved
RivaroxabanThe therapeutic efficacy of Rivaroxaban can be decreased when used in combination with Aprotinin.Approved
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Aprotinin.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Aprotinin.Approved
SarpogrelateThe therapeutic efficacy of Sarpogrelate can be decreased when used in combination with Aprotinin.Investigational
SaruplaseThe therapeutic efficacy of Saruplase can be decreased when used in combination with Aprotinin.Experimental
SelexipagThe therapeutic efficacy of Selexipag can be decreased when used in combination with Aprotinin.Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Aprotinin.Approved, Investigational
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Aprotinin.Approved
SpiraprilAprotinin may decrease the antihypertensive activities of Spirapril.Approved
St. John's WortThe metabolism of Aprotinin can be increased when combined with St. John's Wort.Investigational, Nutraceutical
StreptokinaseThe therapeutic efficacy of Streptokinase can be decreased when used in combination with Aprotinin.Approved, Investigational
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Aprotinin.Approved, Investigational
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Aprotinin.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Aprotinin.Approved, Investigational
TemocaprilAprotinin may decrease the antihypertensive activities of Temocapril.Experimental, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Aprotinin is combined with Temsirolimus.Approved
TenecteplaseThe therapeutic efficacy of Tenecteplase can be decreased when used in combination with Aprotinin.Approved
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Aprotinin.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Aprotinin.Approved, Investigational
TicagrelorThe therapeutic efficacy of Ticagrelor can be decreased when used in combination with Aprotinin.Approved
TiclopidineThe therapeutic efficacy of Ticlopidine can be decreased when used in combination with Aprotinin.Approved
TinzaparinThe therapeutic efficacy of Tinzaparin can be decreased when used in combination with Aprotinin.Approved
TioclomarolThe therapeutic efficacy of Tioclomarol can be decreased when used in combination with Aprotinin.Experimental
TipranavirThe serum concentration of Aprotinin can be decreased when it is combined with Tipranavir.Approved, Investigational
TirofibanThe therapeutic efficacy of Tirofiban can be decreased when used in combination with Aprotinin.Approved
TrandolaprilAprotinin may decrease the antihypertensive activities of Trandolapril.Approved
TreprostinilThe therapeutic efficacy of Treprostinil can be decreased when used in combination with Aprotinin.Approved, Investigational
TretinoinTretinoin may increase the thrombogenic activities of Aprotinin.Approved, Investigational, Nutraceutical
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Aprotinin.Approved
TriflusalThe therapeutic efficacy of Triflusal can be decreased when used in combination with Aprotinin.Approved, Investigational
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Aprotinin.Approved
UrokinaseThe therapeutic efficacy of Urokinase can be decreased when used in combination with Aprotinin.Approved, Investigational, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Aprotinin.Approved, Investigational
VerapamilThe metabolism of Verapamil can be decreased when combined with Aprotinin.Approved
VorapaxarThe therapeutic efficacy of Vorapaxar can be decreased when used in combination with Aprotinin.Approved
WarfarinThe therapeutic efficacy of Warfarin can be decreased when used in combination with Aprotinin.Approved
XimelagatranThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Aprotinin.Approved, Investigational, Withdrawn
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Aprotinin.Approved
ZofenoprilAprotinin may decrease the antihypertensive activities of Zofenopril.Experimental
Food Interactions
Not Available

References

Synthesis Reference

Marion Steinbuch, Jacques Chabbat, Olivier Taby, "Process for preparation of activated protein C by immobilized aprotinin chromatography." U.S. Patent US5198534, issued February, 1985.

US5198534
General References
  1. Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [PubMed:15277296]
External Links
KEGG Drug
D02971
PubChem Substance
347910361
ChEMBL
CHEMBL1201619
Therapeutic Targets Database
DAP000185
PharmGKB
PA448472
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Aprotinin
ATC Codes
B02AB01 — Aprotinin
AHFS Codes
  • 20:28.16 — Hemostatics
FDA label
Download (108 KB)
MSDS
Download (19.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedPreventionPancreatitis1
1TerminatedTreatmentMetastatic Breast Cancer (MBC)1
2RecruitingTreatmentBile Leak / Common Bile Duct Gall Stones / Infection NOS1
3CompletedPreventionBlood Loss,Surgical1
3CompletedPreventionBlood Loss,Surgical / Postoperative Hemorrhages1
3TerminatedTreatmentBlood Loss,Surgical1
3TerminatedTreatmentBlood Loss,Surgical / Postoperative Hemorrhages1
4CompletedTreatmentControl of Local Bleeding in Patients Undergoing Prostatectomy1
Not AvailableCompletedNot AvailableSurgery, Cardiac1
Not AvailableCompletedTreatmentAngina Pectoris / Ischaemic Heart Diseases1
Not AvailableNo Longer AvailableNot AvailablePostoperative Hemorrhages1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
SolutionIntravenous10000 unit
LiquidIntravenous100000 unit
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)>100 °CNot 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 endopeptidase activity
Specific Function
Has activity against the synthetic substrates Boc-Phe-Ser-Arg-Mec, Boc-Leu-Thr-Arg-Mec, Boc-Gln-Ala-Arg-Mec and Boc-Val-Pro-Arg-Mec. The single-chain form is more active than the two-chain form aga...
Gene Name
PRSS1
Uniprot ID
P07477
Uniprot Name
Trypsin-1
Molecular Weight
26557.88 Da
References
  1. Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [PubMed:15277296]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
Not Available
Gene Name
CTRB1
Uniprot ID
P17538
Uniprot Name
Chymotrypsinogen B
Molecular Weight
27869.74 Da
References
  1. Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [PubMed:15277296]
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. Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [PubMed:15277296]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
Glandular kallikreins cleave Met-Lys and Arg-Ser bonds in kininogen to release Lys-bradykinin.
Gene Name
KLK1
Uniprot ID
P06870
Uniprot Name
Kallikrein-1
Molecular Weight
28889.425 Da
References
  1. Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [PubMed:15277296]

Drug created on February 12, 2009 09:44 / Updated on January 14, 2018 10:04