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Tirofiban | CAS No: 144494-65-5 | GMP-certified suppliers
A medication that, combined with heparin, treats acute coronary syndrome by preventing thrombotic complications in medically managed patients and those undergoing coronary interventions.
Therapeutic categories
Primary indications
- For treatment, in combination with heparin, of acute coronary syndrome, including patients who are to be managed medically and those undergoing PTCA or atherectomy
Product Snapshot
- Tirofiban is a parenteral injectable small molecule formulation
- It is primarily indicated for the treatment of acute coronary syndrome in combination with heparin
- The product is approved for use in key regulatory markets including the US and Canada
Clinical Overview
Pharmacologically, tirofiban acts as a reversible, non-peptide antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, which is the principal receptor mediating platelet aggregation via fibrinogen binding. By inhibiting fibrinogen binding to GP IIb/IIIa, tirofiban effectively reduces platelet aggregation in a dose-dependent manner. Intravenous administration leads to rapid and substantial inhibition, exceeding 90% platelet aggregation blockade by the end of a 30-minute infusion. Clinical evidence demonstrates that tirofiban reduces ischemic events within 48 hours in patients with unstable angina when compared with standard heparin therapy.
Tirofiban belongs chemically to the class of phenylalanine derivatives, specifically amino acid-related compounds with aromatic and cyclic structural features. The drug is primarily eliminated via renal excretion, necessitating dosage adjustments in patients with impaired kidney function.
Safety considerations include monitoring for bleeding, the most significant adverse effect associated with GP IIb/IIIa antagonists. Reversibility of platelet inhibition post-infusion allows for some flexibility in management; however, caution is warranted during concurrent use with other anticoagulants or antiplatelet therapies to mitigate hemorrhagic risk. No peptide component reduces immunogenic concerns compared to peptide-derived agents.
Notable marketed formulations of tirofiban are administered as intravenous solutions designed for rapid onset in acute cardiovascular settings.
From an API sourcing perspective, tirofiban requires stringent quality control due to its critical role in acute care and narrow therapeutic index. Purity, stereochemistry, and compliance with pharmacopeial standards are essential. Suppliers should adhere to Good Manufacturing Practices (GMP) and provide comprehensive documentation including certificates of analysis and impurity profiles to ensure consistent performance in finished pharmaceutical products.
Identification & chemistry
| Generic name | Tirofiban |
|---|---|
| Molecule type | Small molecule |
| CAS | 144494-65-5 |
| UNII | GGX234SI5H |
| DrugBank ID | DB00775 |
Pharmacology
| Summary | Tirofiban is a reversible antagonist of the platelet glycoprotein IIb/IIIa receptor (integrin alpha-IIb/beta-3), inhibiting fibrinogen binding and platelet aggregation. It acts intravenously to reduce clot formation during acute coronary syndrome and interventional cardiac procedures. Its platelet aggregation inhibition is dose-dependent and reversible upon treatment cessation. |
|---|---|
| Mechanism of action | Tirofiban is a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation. Platelet aggregation inhibition is reversible following cessation of the infusion of tirofiban. |
| Pharmacodynamics | Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation. When administered intravenously, tirofiban inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner. When given according to the recommended regimen, >90% inhibition is attained by the end of the 30-minute infusion. Tirofiban has been recently shown in patients with unstable angina to reduce ischemic events at 48 hours following infusion when compared to standard heparin therapy. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Integrin alpha-IIb | Humans | antagonist |
| Integrin beta-3 | Humans | antagonist |
ADME / PK
| Half-life | 2 hours |
|---|---|
| Protein binding | 65% |
| Metabolism | Metabolism appears to be limited. |
| Route of elimination | It is cleared from the plasma largely by renal excretion, with about 65% of an administered dose appearing in urine and about 25% in feces, both largely as unchanged tirofiban. |
| Volume of distribution | * 22 to 42 L |
| Clearance | * 213 - 314 mL/min [Healthy subjects] * 152 - 267 mL/min [patients with coronary artery disease] |
Formulation & handling
- Tirofiban is a small molecule API primarily formulated for intravenous injection and parenteral administration.
- It exhibits low water solubility, necessitating suitable solvent systems for stable injectable formulations.
- There is no indication of peptide or biologic characteristics, reducing concerns related to enzymatic degradation.
Regulatory status
| Lifecycle | The API is currently in a mature market phase in both the US and Canada, with key patents expiring between 2010 and 2016, and a more recent patent active until 2023 in the US. This patent landscape suggests a shift toward increased generic competition in these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Tirofiban is primarily manufactured by Medicure International Inc. and packaged by multiple companies including Baxter International Inc. and Merck & Co., indicating a multi-entity supply network. Its branded products, notably Aggrastat, are distributed mainly in the US and Canadian markets. Patent expiry dates, with the latest in the US occurring in 2023, suggest that generic competition is either currently present or likely imminent within these regions. |
|---|
Tirofiban is a type of Glycoprotein IIb/IIIa receptor antagonists
Glycoprotein IIb/IIIa receptor antagonists belong to a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the field of medicine. These antagonists specifically target and inhibit the activity of the glycoprotein IIb/IIIa receptors found on platelets.
The glycoprotein IIb/IIIa receptors play a crucial role in platelet aggregation, which is an essential step in the formation of blood clots. By blocking these receptors, glycoprotein IIb/IIIa receptor antagonists prevent platelets from binding to each other and forming clots, thereby inhibiting thrombus formation.
These pharmaceutical compounds have shown great potential in the treatment and prevention of conditions related to unwanted blood clotting, such as acute coronary syndromes and percutaneous coronary interventions. They are commonly used during angioplasty and stent placement procedures to reduce the risk of clot formation and subsequent complications.
Glycoprotein IIb/IIIa receptor antagonists are typically administered intravenously and have a relatively short duration of action. Common examples include abciximab, eptifibatide, and tirofiban. These agents are carefully monitored and controlled due to their potent antiplatelet effects.
It is important to note that the use of glycoprotein IIb/IIIa receptor antagonists requires close medical supervision, as they can increase the risk of bleeding. Therefore, healthcare professionals must carefully weigh the benefits and risks when considering the administration of these pharmaceutical APIs.
Tirofiban (Glycoprotein IIb/IIIa receptor antagonists), classified under Anticoagulants
Anticoagulants are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used to prevent and treat blood clotting disorders. These medications play a crucial role in various medical conditions, including deep vein thrombosis (DVT), pulmonary embolism (PE), and atrial fibrillation (AF). Anticoagulants work by inhibiting the formation of blood clots or by preventing existing clots from getting larger.
There are different types of anticoagulants available, including direct thrombin inhibitors, vitamin K antagonists, and factor Xa inhibitors. Direct thrombin inhibitors, such as dabigatran, directly target the enzyme thrombin to hinder clot formation. Vitamin K antagonists, like warfarin, interfere with the production of clotting factors that rely on vitamin K. Factor Xa inhibitors, such as rivaroxaban and apixaban, inhibit the activity of factor Xa, a crucial component in the clotting cascade.
Anticoagulants are commonly prescribed to patients at risk of developing blood clots or those with existing clotting disorders. They are often used during surgeries, such as hip or knee replacements, to minimize the risk of post-operative clot formation. Patients with AF, a condition characterized by irregular heart rhythm, may also be prescribed anticoagulants to prevent stroke caused by blood clots.
While anticoagulants offer significant benefits in preventing and treating clot-related conditions, they also carry potential risks, including bleeding complications. Patients taking anticoagulants require careful monitoring to ensure the right dosage is administered, as excessive anticoagulation can lead to hemorrhage. Regular blood tests and close medical supervision are essential to manage the delicate balance between preventing clots and avoiding excessive bleeding.
In conclusion, anticoagulants are a crucial category of pharmaceutical APIs used to prevent and treat blood clotting disorders. They function by inhibiting clot formation or preventing existing clots from enlarging. While highly beneficial, their use requires careful monitoring to minimize the risk of bleeding complications.
Tirofiban API manufacturers & distributors
Compare qualified Tirofiban API suppliers worldwide. We currently have 4 companies offering Tirofiban 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 |
|---|---|---|---|---|---|
| Edmond Pharma (Recipharm) | Producer | Italy | Italy | CoA, GMP | 20 products |
| Farmabios | Producer | Italy | Italy | CoA, ISO9001, USDMF | 58 products |
| Wisdom Pharma | Producer | China | China | CoA, USDMF | 12 products |
| Xi’an Wanlong pharmaceuti... | Producer | China | China | CoA, GMP, USDMF | 2 products |
When sending a request, specify which Tirofiban 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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