Gilteritinib API is an orally active, small-molecule tyrosine kinase inhibitor (TKI) developed under the code ASP2215. It primarily inhibits FMS-like tyrosine kinase 3 (FLT3) and AXL receptor tyrosine kinases. Gilteritinib inhibits FLT3 signaling, including signaling associated with FLT3-ITD and selected FLT3-TKD mutations, thereby suppressing proliferation and promoting apoptosis in FLT3-driven leukemic cells.
Gilteritinib has the CAS Registry Number 1254053-43-4, molecular formula C₂₉H₄₄N₈O₃, and molecular weight 552.7 g/mol for the free base.
The pharmaceutical product XOSPATA contains gilteritinib fumarate. Gilteritinib fumarate is a 2:1 salt of gilteritinib and fumaric acid, with molecular formula (C₂₉H₄₄N₈O₃)₂·C₄H₄O₄ and molecular weight 1221.50 g/mol. Each 40 mg tablet contains 40 mg of gilteritinib free base, equivalent to approximately 44.2 mg of gilteritinib fumarate.
Gilteritinib is approved for adult patients with relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation, as detected by an FDA-approved test.
| Property | Value |
|---|---|
| API Name | Gilteritinib |
| CAS Number | 1254053-43-4 |
| Development Code | ASP2215 / ASP-2215 |
| Chemical Class | Pyrazine Carboxamide Derivative |
| Pharmacological Class | Tyrosine Kinase Inhibitor |
| Primary Targets | FLT3 and AXL |
| Molecular Formula | C₂₉H₄₄N₈O₃ |
| Molecular Weight | 552.7 g/mol |
| Salt Form | Gilteritinib Fumarate |
| Fumarate CAS Number | 1254053-84-3 |
| Fumarate Molecular Formula | (C₂₉H₄₄N₈O₃)₂·C₄H₄O₄ |
| Fumarate Molecular Weight | 1221.50 g/mol |
| Brand | XOSPATA |
| Dosage Form | Film-coated tablet |
The FDA and EMA documentation confirms that the drug substance specification includes identification, assay, related substances, residual solvents, water content and sulfate/sulphated-ash testing appropriate to gilteritinib fumarate.
Gilteritinib inhibits multiple receptor tyrosine kinases, with clinically important activity against FLT3 and AXL.
It inhibits FLT3 signaling in cells expressing:
Inhibition of FLT3 signaling reduces leukemic-cell proliferation and can induce apoptosis.
Gilteritinib is primarily associated with the treatment of FLT3-mutated acute myeloid leukemia (AML).
The API is relevant to:
| 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 0.5% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 2.0% |