Eltrombopag API Manufacturers & Suppliers
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Eltrombopag | CAS No: 496775-61-2 | GMP-certified suppliers
A medication that stimulates platelet production to treat thrombocytopenia in chronic immune thrombocytopenia and hepatitis C-associated thrombocytopenia for hematology and hepatology applications.
Therapeutic categories
Primary indications
- Thrombopoietin receptor agonists are pharmaceutical agents that stimulate platelet production in the bone marrow
- In this, they differ from the previously discussed agents that act by attempting to curtail platelet destruction
Product Snapshot
- Eltrombopag is an oral small molecule available primarily in film-coated tablet and powder for suspension formulations
- It functions as a thrombopoietin receptor agonist to stimulate platelet production in the bone marrow
- Eltrombopag is approved for use in key regulatory markets including the US, Canada, and the European Union
Clinical Overview
Pharmacologically, eltrombopag belongs to the biphenyl class of organic compounds and functions by selectively stimulating the thrombopoietin (TPO) receptor located on hematopoietic stem and progenitor cells. This interaction occurs at the transmembrane domain of the human TPO receptor, triggering intracellular signaling cascades primarily involving STAT and JAK phosphorylation. Eltrombopag’s mechanism of action differs from endogenous thrombopoietin and peptibody TPO mimetics in that it does not activate the AKT pathway. Clinical data in aplastic anemia suggest it may also promote multilineage hematopoietic effects beyond platelet production, though the precise mechanisms remain to be fully elucidated.
Key absorption, distribution, metabolism, and excretion (ADME) characteristics include oral bioavailability with metabolism mediated by cytochrome P450 enzymes, including CYP1A2, and interactions with various UDP-glucuronosyltransferase isoforms such as UGT1A1 and UGT1A3. Eltrombopag is also known to inhibit certain transport proteins including OATP1B1 and BCRP/ABCG2, which may impact concurrent drug pharmacokinetics.
Safety considerations include monitoring for thromboembolic events, hepatotoxicity, and bone marrow fibrosis during therapy. Dose adjustments may be necessary in hepatic impairment. No carcinogenicity or mutagenicity has been conclusively demonstrated.
Eltrombopag is marketed under several brand names worldwide and is utilized primarily within hematology and hepatology treatment settings.
For API sourcing, strict adherence to pharmacopeial quality standards and regulatory guidelines is essential due to eltrombopag’s complex synthetic route and its sensitive physicochemical properties. Suppliers should provide robust documentation on purity, polymorphic form, and stability to ensure consistent clinical performance.
Identification & chemistry
| Generic name | Eltrombopag |
|---|---|
| Molecule type | Small molecule |
| CAS | 496775-61-2 |
| UNII | S56D65XJ9G |
| DrugBank ID | DB06210 |
Pharmacology
| Summary | Eltrombopag is an oral small-molecule agonist of the thrombopoietin (TPO) receptor that binds to its transmembrane domain, promoting platelet production. It activates downstream signaling pathways involving STAT and JAK phosphorylation without engaging the AKT pathway. The drug’s pharmacodynamic effects include stimulation of megakaryocyte proliferation and differentiation, potentially influencing multiple hematopoietic lineages in certain conditions. |
|---|---|
| Mechanism of action | Eltrombopag is an orally bioavailable, small-molecule TPO-receptor agonist that interacts with the transmembrane domain of the human TPO-receptor. Eltrombopag is a stimulator of STAT and JAK phosphorylation. Unlike recombinant TPO or romiplostim, Eltrombopag does not activate the AKT pathway in any way. It should be noted that when given to patients with aplastic anemia, other lineages besides platelet count were increased, suggesting that either eltrombopag enhanced the effect of TPO in vivo; or there is a yet uncovered mechanism of action at work. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Thrombopoietin receptor | Humans | agonist |
ADME / PK
| Absorption | Peak absorption of Eltrombopag occurs around 2-6 hours following oral administration, and the total oral absorption of drug-related material following a 75 mg dose was estimated to be at least 52%. |
|---|---|
| Half-life | About 21-32 hours in healthy patients. About 26-35 hours in patients with idiopathic thrombocytopenic purpura. |
| Protein binding | Eltrombopag is highly protein bound (>99%). |
| Metabolism | Eltrombopag is predominantly through pathways including cleavage, oxidation, and conjugation with glucuronic acid, glutathione, or cysteine. In vitro studies suggest that CYP1A2 and CYP2C8 are responsible for the oxidative metabolism of eltrombopag. UGT1A1 and UGT1A3 are responsible for the glucuronidation of eltrombopag. |
| Route of elimination | Eltrombopag is eliminated primarily via the feces (59%), along with 31% being renally excreted. |
| Volume of distribution | Based on a radiolabel study, the concentration of eltrombopag in blood cells is approximately 50% to 79% of plasma concentrations. |
Formulation & handling
- Eltrombopag is a small molecule oral API formulated primarily as film-coated tablets and oral suspensions.
- It exhibits low water solubility and high lipophilicity, which may influence formulation strategies for bioavailability enhancement.
- Administration requires careful timing relative to meals to avoid chelation with polyvalent cations and ensure optimal absorption.
Regulatory status
| Lifecycle | The API is marketed in the US, Canada, and EU, with key US patents expiring between April 2019 and February 2028, indicating a transition from protected to increasingly generic market phases in the coming years. |
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| Markets | US, Canada, EU |
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Supply Chain
| Supply chain summary | Eltrombopag is supplied by multiple originator companies with branded products primarily distributed in the US, Canada, and EU markets. Several patents protect the drug in the United States, with the most recent expiring in February 2028. The expiration timeline indicates existing generic competition in some cases, particularly after 2019 and 2021 patents, while further generic entry may increase following the 2028 patent expiry. |
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Safety
| Toxicity | Eltrombopag may cause hepatotoxicity, especially if administered in combination with interferon and ribavirin in patients with chronic hepatitis C (may increase the risk of hepatic decompensation). |
|---|
- Eltrombopag has been associated with hepatotoxicity
- Monitor hepatic function during handling and processing
- Combined exposure with interferon and ribavirin may elevate risk of hepatic adverse effects
Eltrombopag is a type of Other antithrombin
The Other Antithrombin subcategory in pharmaceutical active pharmaceutical ingredients (APIs) refers to a class of compounds that exhibit antithrombin activity but do not fall under the traditional anticoagulant or antiplatelet categories. These APIs play a crucial role in preventing blood clot formation and reducing the risk of thrombotic events.
One notable API in this subcategory is [Name of the API], which demonstrates potent antithrombin properties by inhibiting specific clotting factors in the blood. By targeting these factors, [Name of the API] helps regulate the coagulation cascade, a complex process involved in blood clot formation.
The unique mechanism of action of [Name of the API] distinguishes it from other antithrombin APIs, making it a valuable option for treating thrombotic disorders. This API exhibits high selectivity, effectively inhibiting clotting factors without significantly impacting other blood components or processes.
[Name of the API] is carefully developed and rigorously tested to ensure its safety, efficacy, and reliability. It undergoes stringent quality control measures to meet regulatory standards and ensure consistency in its performance.
Pharmaceutical companies incorporate [Name of the API] into various formulations, such as oral tablets, injections, or topical preparations, enabling healthcare providers to administer it in the most suitable form for patients.
The Other Antithrombin subcategory in pharmaceutical APIs, with [Name of the API] as a prominent member, provides an innovative therapeutic approach to managing thrombotic disorders and contributes to enhancing patient care and outcomes in the field of hematology.
Eltrombopag (Other antithrombin), 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.
Eltrombopag API manufacturers & distributors
Compare qualified Eltrombopag API suppliers worldwide. We currently have 7 companies offering Eltrombopag API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| ACE Japan | Producer | Japan | Japan | CoA | 76 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, USDMF, WC | 98 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Raks Pharma | Producer | India | India | CoA, USDMF | 58 products |
| Saneca Pharma | Producer | Slovakia | Slovakia | CoA, GMP | 25 products |
| Shilpa Medicare Ltd | Producer | India | India | CoA, FDA, GMP, ISO9001 | 54 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC | 762 products |
When sending a request, specify which Eltrombopag 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.).
Use the list above to find high-quality Eltrombopag API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
