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Aprotinin | CAS No: 9087-70-1 | GMP-certified suppliers
A medication that reduces perioperative blood loss and transfusion needs in patients undergoing cardiopulmonary bypass during coronary artery bypass graft surgery, particularly in high-risk cases.
Therapeutic categories
Primary indications
- 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
Product Snapshot
- Aprotinin is available primarily as an injectable solution and powder for intravenous, soft tissue, and topical administration
- It is utilized for the prophylactic reduction of perioperative blood loss and the need for blood transfusion during cardiopulmonary bypass in coronary artery bypass graft surgery
- Aprotinin holds approval status in the US and Canada, with some formulations also under investigational use or withdrawn in certain markets
Clinical Overview
Pharmacodynamically, aprotinin exerts a broad-spectrum inhibitory effect on several proteases, including trypsin, chymotrypsin, plasmin, and kallikrein. By inhibiting kallikrein, aprotinin suppresses the activation of factor XIIa, thereby attenuating the intrinsic coagulation pathway and fibrinolysis. The inhibition of plasmin further contributes to decreased fibrinolytic activity. Beyond coagulation, aprotinin modulates the systemic inflammatory response that is typical of cardiopulmonary bypass surgery by reducing pro-inflammatory cytokine release and preserving platelet glycoprotein stability. This effect on the inflammatory cascade translates into lower bleeding risk and reduced demand for allogeneic blood transfusions in clinical settings where it was previously utilized.
Pharmacokinetic details of aprotinin include intravenous administration, as it is a protein with poor oral bioavailability. Clearance mechanisms and volume of distribution are not well characterized in the literature but are consistent with protease inhibitors of proteinaceous origin. Due to its nature, aprotinin is subject to enzymatic degradation.
Aprotinin was globally withdrawn from clinical use in 2008 after studies demonstrated an increased risk of serious adverse outcomes, including mortality and complications related to its antifibrinolytic action. Consequently, it remains available only under restricted conditions for research purposes.
From a safety perspective, concerns centered on thrombotic complications and hypersensitivity reactions, including anaphylaxis upon re-exposure, limit its applicability. Its use requires careful risk-benefit assessment and monitoring if considered in investigational contexts.
Current sourcing of aprotinin API demands stringent quality control measures to ensure purity and biological activity, with attention to potential immunogenicity and contamination risks inherent in protein-derived pharmaceuticals. Procurement should prioritize manufacturers complying with good manufacturing practices (GMP) specialized in protein-based active ingredients to maintain consistent quality for investigational use.
Identification & chemistry
| Generic name | Aprotinin |
|---|---|
| Molecule type | Biotech |
| CAS | 9087-70-1 |
| UNII | 04XPW8C0FL |
| DrugBank ID | DB06692 |
Pharmacology
| Summary | Aprotinin is a broad-spectrum serine protease inhibitor targeting trypsin, chymotrypsin, plasmin, and kallikrein, which results in the inhibition of the intrinsic coagulation pathway and fibrinolysis. It modulates the systemic inflammatory response associated with cardiopulmonary bypass by attenuating pro-inflammatory mediator release and preserving platelet glycoprotein function. These combined effects reduce perioperative bleeding and thrombin generation during coronary artery bypass graft surgery. |
|---|---|
| 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. |
| 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Trypsin-1 | Humans | |
| Chymotrypsinogen B | Humans | |
| Plasminogen | Humans |
ADME / PK
| Absorption | 100% (IV) |
|---|---|
| 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. |
| 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. |
Formulation & handling
- Aprotinin is a biotech peptide available in liquid and powder forms for intravenous, topical, and soft tissue administration.
- Due to its biologic nature, formulations require careful handling to maintain stability and prevent degradation.
- Storage and preparation conditions should minimize exposure to extremes of temperature and agitation to preserve activity.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has reached patent expiry in both the US and Canada, leading to a mature market environment with availability of generic formulations. Commercial activity is primarily focused on established product positioning in these regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Aprotinin is supplied by multiple originator companies, including Baxter International Inc. and Bayer Healthcare, primarily targeting the Canadian and US markets. Branded products such as Artiss, Tisseel, and Trasylol have a notable presence in these regions. The patent landscape suggests that generic competition is either current or imminent, reflecting typical post-patent market dynamics. |
|---|
Aprotinin is a type of Antifibrinolytics
Antifibrinolytics belong to a vital category of pharmaceutical active pharmaceutical ingredients (APIs) utilized in the medical field. These compounds play a crucial role in preventing excessive bleeding by inhibiting the breakdown of blood clots. By promoting clot stability, antifibrinolytics help control bleeding, particularly in situations where there is a risk of uncontrolled hemorrhage.
One well-known antifibrinolytic agent is tranexamic acid, which is widely employed in various medical procedures, including surgery, trauma management, and dental procedures. This API works by binding to plasminogen, a protein involved in the dissolution of blood clots, and preventing its conversion to plasmin, the enzyme responsible for clot degradation.
Another prominent antifibrinolytic is aminocaproic acid, which acts in a similar manner to tranexamic acid. It competitively inhibits the activation of plasminogen, thereby preserving the integrity of formed clots.
Antifibrinolytics find applications in several medical specialties, such as orthopedics, cardiovascular surgery, and gynecology. They are particularly valuable in managing bleeding disorders, such as hemophilia and menorrhagia, as well as in minimizing blood loss during major surgical procedures.
As with any pharmaceutical API, the production and use of antifibrinolytics require adherence to strict quality control standards and regulatory guidelines to ensure their safety and efficacy. Healthcare professionals should carefully assess each patient's condition and consider potential contraindications or interactions before prescribing or administering antifibrinolytic medications.
In conclusion, antifibrinolytics play a crucial role in preventing excessive bleeding by inhibiting clot breakdown. These pharmaceutical APIs, such as tranexamic acid and aminocaproic acid, are widely used in various medical procedures and provide valuable therapeutic options for managing bleeding disorders and minimizing blood loss during surgeries.
Aprotinin API manufacturers & distributors
Compare qualified Aprotinin API suppliers worldwide. We currently have 2 companies offering Aprotinin API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Bayer | Producer | Germany | Unknown | CoA, USDMF | 42 products |
| Kraeber & Co GmbH | Producer | Germany | Germany | CoA, GDP, GMP, ISO9001, MSDS | 12 products |
When sending a request, specify which Aprotinin API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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