Explore a selection of our essential drug information below, or:
Identification
- Summary
Aprotinin is a serine protease inhibitor used to reduce the risk for perioperative blood loss and the need for blood transfusion in high-risk patients during cardiopulmonary bypass for coronary artery bypass graft surgery.
- Brand Names
- Artiss, Tisseel, Trasylol
- Generic Name
- Aprotinin
- DrugBank Accession Number
- DB06692
- Background
Aprotinin is a protein-based drug that is also known as bovine pancreatic trypsin inhibitor (BPTI). Since it demonstrates the capacity to slow fibrinolysis, it has been employed to reduce bleeding during complex surgery such as heart and liver surgery. For this use, it is typically administered by injection. The goal of using of aprotinin was subsequently to minimize end-organ damage resulting from hypotension due to blood loss in surgery and to reduce the necessity for blood transfusions during surgery. Nevertheless, the drug was formally withdrawn worldwide in May of 2008 after studies confirmed that its use enhanced the risk of complications or death. The substance is consequently made available only for very restricted research use.
- Type
- Biotech
- Groups
- Approved, Investigational, Withdrawn
- Biologic Classification
- Protein Based Therapies
Other protein based therapies - Protein Structure
- Protein Chemical Formula
- C284H432N84O79S7
- Protein Average Weight
- 6511.439 Da
- Sequences
>Aprotinin (bovine pancreatic trypsin inhibitor) RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA
Download FASTA Format- Synonyms
- Aprotinin
- Aprotinin (bovine)
- Aprotinin biosynthetic
- Aprotinin bovine
- Aprotinin concentrated solution
- Aprotinina
- Aprotinine
- Aprotininum
- Bovine aprotinin
- Bovine pancreatic trypsin inhibitor
- BPTI
- Fibrinolysis inhibitor
- Trypsin inhibitor, pancreatic basic
- External IDs
- 232-994-9
- Bayer A 128
- Bayer-A-128
- BAYERA-128
- RIKER 52G
- Riker-52G
- RP 9921
- RP-9921
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.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Therapies
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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 serine proteases including trypsin, chymotrypsin and plasmin at a concentration of about 125,000 IU/mL, and kallikrein at 300,000 IU/mL. The inhibition of kallikrein inhibits formation of factor XIIa. This inhibits the intrinsic pathway of coagulation and fibrinolysis. Inhibition of plasmin also slows fibrinolysis.
Target Actions Organism USerine protease 1 Not Available Humans UChymotrypsinogen B Not Available Humans UPlasminogen Not Available Humans UKallikrein-1 Not Available Humans - 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
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
Pathway Category Aprotinin Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol Aprotinin may increase the bradycardic activities of Acebutolol. Acetylcholine The risk or severity of adverse effects can be increased when Aprotinin is combined with Acetylcholine. Aclidinium Aprotinin may increase the neuromuscular blocking activities of Aclidinium. Albutrepenonacog alfa Aprotinin may increase the thrombogenic activities of Albutrepenonacog alfa. Alpha-1-proteinase inhibitor Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Aprotinin. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Trasylol Solution 2000000 1/200mL Intravenous Bayer Pharmaceuticals Corporation 1993-12-29 2008-05-22 US 
Trasylol Solution 10000 unit / mL Intravenous Nordic Group Bv 1997-12-15 Not applicable Canada 
Trasylol Solution 1000000 1/100mL Intravenous Bayer Pharmaceuticals Corporation 1993-12-29 2008-05-22 US Trasylol Inj 10000 Kiu/ml Liquid 100000 unit / amp Intravenous Miles Canada Inc. Pharmaceutical Division 1981-12-31 1998-09-25 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Artiss Aprotinin (3000 kiu / mL) + Calcium chloride (40 mcmol / mL) + Fibrinogen human (125 mg / mL) + Human thrombin (4 unit / mL) Solution Topical Baxter Laboratories 2011-12-18 Not applicable Canada ARTISS - Lösungen für einen Gewebekleber Aprotinin (1500 KIE/ml) + Calcium chloride (20 μmol/ml) + Fibrinogen human (45.5 mg/ml) + Thrombin (2 IU/ml) Solution Topical Baxter Medical Products Gmb H 2009-03-19 Not applicable Austria 
ARTISS 10 ML ÇÖZELTİ İÇEREN KULLANIMA HAZIR ENJEKTOR, 1 ADET Aprotinin (3000 KIU/ml) + Calcium chloride dihydrate (40 mcmol/ml) + Fibrinogen human (91 mg/ml) + Thrombin (4 IU/ml) Solution Topical BAXTER TURKEY RENAL HİZMETLER A.Ş. 2020-08-14 Not applicable Turkey 
ARTISS 2 ML ÇÖZELTİ İÇEREN KULLANIMA HAZIR ENJEKTOR, 1 ADET Aprotinin (3000 KIU/ml) + Calcium chloride dihydrate (40 mcmol/ml) + Fibrinogen human (91 mg/ml) + Thrombin (4 IU/ml) Solution Topical BAXTER TURKEY RENAL HİZMETLER A.Ş. 2020-08-14 Not applicable Turkey ARTISS 4 ML ÇÖZELTİ İÇEREN KULLANIMA HAZIR ENJEKTOR, 1 ADET Aprotinin (3000 KIU/ml) + Calcium chloride dihydrate (40 mcmol/ml) + Fibrinogen human (91 mg/ml) + Thrombin (4 IU/ml) Solution Topical BAXTER TURKEY RENAL HİZMETLER A.Ş. 2020-08-14 Not applicable Turkey
Categories
- ATC Codes
- B02AB01 — Aprotinin
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- 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
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 04XPW8C0FL
- CAS number
- 9087-70-1
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
- Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [Article]
- External Links
- KEGG Drug
- D02971
- PubChem Substance
- 347910361
- 353110
- ChEMBL
- CHEMBL1201619
- Therapeutic Targets Database
- DAP000185
- PharmGKB
- PA448472
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Aprotinin
- FDA label
- Download (108 KB)
- MSDS
- Download (19.5 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Surgery, Cardiac 1 somestatus stop reason just information to hide Not Available Completed Treatment Angina Pectoris / Ischemic Heart Disease 1 somestatus stop reason just information to hide Not Available No Longer Available Not Available Postoperative Hemorrhages 1 somestatus stop reason just information to hide Not Available Unknown Status Not Available Surgery, Cardiac 1 somestatus stop reason just information to hide Not Available Unknown Status Treatment Coronavirus Disease 2019 (COVID‑19) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Baxter International Inc.
- Bayer Healthcare
- Dosage Forms
Form Route Strength Solution Topical Solution Topical 360 - Solution Powder, for solution Topical Kit Topical Powder Topical Kit; solution Solution Topical 3000 KIU/ml Powder Soft tissue Solution Intravenous 10000 unit / mL Solution Intravenous 1000000 1/100mL Solution Intravenous 2000000 1/200mL Solution Intravenous 10000 KIE/ml Liquid Intravenous 100000 unit / amp Injection Intravenous 500000 kiu/50ml - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) >100 °C Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General 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 against all of these substrates
- Specific Function
- metal ion binding
- Gene Name
- PRSS1
- Uniprot ID
- P07477
- Uniprot Name
- Serine protease 1
- Molecular Weight
- 26557.88 Da
References
- Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Not Available
- Specific Function
- serine-type endopeptidase activity
- Gene Name
- CTRB1
- Uniprot ID
- P17538
- Uniprot Name
- Chymotrypsinogen B
- Molecular Weight
- 27712.52 Da
References
- Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General 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 ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin and laminin leads to cell detachment and apoptosis. Also cleaves fibrin, thrombospondin and von Willebrand factor. Its role in tissue remodeling and tumor invasion may be modulated by CSPG4. Binds to cells
- Specific Function
- apolipoprotein binding
- Gene Name
- PLG
- Uniprot ID
- P00747
- Uniprot Name
- Plasminogen
- Molecular Weight
- 90568.415 Da
References
- Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Glandular kallikreins cleave Met-Lys and Arg-Ser bonds in kininogen to release Lys-bradykinin
- Specific Function
- serine-type endopeptidase activity
- Gene Name
- KLK1
- Uniprot ID
- P06870
- Uniprot Name
- Kallikrein-1
- Molecular Weight
- 28889.425 Da
References
- Mahdy AM, Webster NR: Perioperative systemic haemostatic agents. Br J Anaesth. 2004 Dec;93(6):842-58. Epub 2004 Jul 26. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters
- Specific Function
- acetylcholinesterase activity
- Gene Name
- BCHE
- Uniprot ID
- P06276
- Uniprot Name
- Cholinesterase
- Molecular Weight
- 68417.575 Da
References
- Aronson JK (2016). Meyler's Side Effects of Drugs: The International Encyclopedia of Adverse Drug Reactions and Interactions (16th ed.). Amsterdam : Elsevier Science. [ISBN:9780444537164]
Drug created at February 12, 2009 16:44 / Updated at October 03, 2024 04:54