Fostamatinib Disodium API is a pharmaceutical active ingredient and a phosphate prodrug of tamatinib (R406), the active metabolite responsible for its pharmacological activity. Fostamatinib acts primarily as a spleen tyrosine kinase (SYK) inhibitor. By inhibiting SYK-dependent signaling pathways, the active metabolite can interfere with immune-cell activation and platelet destruction mechanisms.
Fostamatinib is formulated as the disodium hexahydrate salt, providing a defined pharmaceutical form suitable for drug-product development. The API is characterized by the molecular formula C₂₃H₂₄FN₆Na₂O₉P·6H₂O and molecular weight 732.52 g/mol.
Fostamatinib Disodium is a phosphorylated prodrug. Following administration, it is metabolized to tamatinib (R406). Tamatinib inhibits SYK, a non-receptor tyrosine kinase involved in signaling through several immune receptors.
The API is supplied as a white to off-white powder and has limited aqueous solubility. Its physicochemical characteristics make control of hydration state, purity, residual solvents and particle-size distribution important during pharmaceutical manufacturing.
Fostamatinib itself functions as a prodrug. Its major active metabolite, tamatinib (R406), inhibits spleen tyrosine kinase. SYK participates in signaling pathways associated with Fc receptors and other immune-cell receptors. Inhibition of this pathway reduces platelet clearance mediated by immune mechanisms.
This pharmacological mechanism supports the use of fostamatinib in pharmaceutical products intended for chronic immune thrombocytopenia (ITP).
Fostamatinib Disodium is used as an API for pharmaceutical formulations containing fostamatinib. It has been developed for the treatment of adult patients with chronic immune thrombocytopenia who have had an insufficient response to previous treatment.
The API is therefore relevant to:
Quality control of Fostamatinib Disodium involves evaluation of its identity, assay, related substances, residual solvents, water content and other applicable physicochemical characteristics.
Particular attention is required for the hydrate state because the pharmaceutical substance is supplied as a hexahydrate. Water determination is consequently an important quality attribute for confirming consistency of the API.
Analytical characterization can include HPLC, FTIR, LC-MS, Karl Fischer water determination, GC residual-solvent analysis and particle-size analysis, according to the applicable approved specification.
Fostamatinib Disodium should be stored in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive moisture and unsuitable environmental exposure. Storage conditions should follow the approved manufacturer specification and stability data for the particular API batch.
Because the material is a hydrate, appropriate control of moisture and water content is particularly important to maintain consistent material quality.
For pharmaceutical manufacturers and formulation-development laboratories, Fostamatinib Disodium provides the active pharmaceutical substance used to develop fostamatinib-containing products. API qualification normally includes assessment of:
A complete Certificate of Analysis (CoA) should accompany each commercial batch and should be evaluated against the applicable approved specification.
For regulated pharmaceutical applications, documentation for Fostamatinib Disodium may include:
The exact documentation package depends on the intended pharmaceutical application and regulatory market.
Fostamatinib Disodium is also relevant to pharmaceutical research involving SYK inhibition, immune signaling and drug-development studies. Analytical-grade material can be used for method development, impurity profiling, formulation studies and comparative analytical investigations.
Fostamatinib Disodium API can be sourced for pharmaceutical research, formulation development and commercial API requirements subject to applicable regulatory and quality requirements. Buyers should verify the API form, CAS number, molecular weight, specification, assay, impurity profile, water content and batch-specific CoA before procurement.
A reliable Fostamatinib Disodium API should provide:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| Heavy Metals | NMT 10 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Solubility | Slightly soluble in water; soluble in methanol; practically insoluble in pH 1.2 aqueous buffer |