Futibatinib API is a synthetic, orally active fibroblast growth factor receptor (FGFR) kinase inhibitor developed for targeted anticancer therapy. It is also known by the development code TAS-120. Futibatinib inhibits FGFR1, FGFR2, FGFR3 and FGFR4, with particularly important activity against aberrant FGFR2 signaling.
Futibatinib is used in pharmaceutical formulations for the treatment of previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma with FGFR2 gene fusions or other rearrangements. It is marketed in the United States under the brand name LYTGOBI.
The API has the molecular formula C₂₂H₂₂N₆O₃, molecular weight 418.45 g/mol, and CAS Registry Number 1448169-71-8. FDA and PubChem confirm these chemical identity parameters.
Futibatinib is described as a white crystalline powder. It has pH-dependent solubility, is insoluble in water, and is practically insoluble at approximately pH 3 and above.
| Property | Value |
|---|---|
| API Name | Futibatinib |
| Development Code | TAS-120 |
| CAS Number | 1448169-71-8 |
| Molecular Formula | C₂₂H₂₂N₆O₃ |
| Molecular Weight | 418.45 g/mol |
| Chemical Class | Pyrazolopyrimidine derivative |
| Pharmacological Class | FGFR Kinase Inhibitor |
| Primary Targets | FGFR1, FGFR2, FGFR3, FGFR4 |
| Appearance | White crystalline powder |
| Water Solubility | Insoluble in water |
FDA's current labeling confirms that futibatinib is a small-molecule inhibitor of FGFR1–4, with IC₅₀ values below 4 nM.
Futibatinib is an irreversible FGFR inhibitor that targets the kinase activity of FGFR family receptors. FGFR signaling is involved in cellular proliferation, differentiation, migration and survival.
By inhibiting FGFR signaling, futibatinib interferes with abnormal signaling pathways that can promote tumor growth and survival. Its activity against FGFR2 alterations, particularly FGFR2 fusions or rearrangements, forms the basis for its use in selected patients with intrahepatic cholangiocarcinoma.
Futibatinib demonstrates potent inhibition of FGFR1, FGFR2, FGFR3 and FGFR4, with reported biochemical IC₅₀ values below 4 nM.
Futibatinib is used as an active ingredient in pharmaceutical products intended for targeted oncology treatment.
The FDA-approved product LYTGOBI is supplied as oral tablets in 4 mg and 16 mg strengths.
The API is relevant to:
FGFR2 gene fusions and rearrangements can result in abnormal FGFR signaling and contribute to tumor development. Futibatinib is specifically designed to inhibit this signaling pathway.
The approved indication focuses on adults with previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma harboring FGFR2 fusions or other rearrangements.
Futibatinib is a white crystalline powder. Its solubility is strongly dependent on pH. According to current FDA labeling, futibatinib is insoluble in water and poorly soluble in common solvents, with solubility decreasing as pH increases.
This physicochemical property is important during:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 98.0% by HPLC |
| Loss on Drying | NMT 1.0% |
| Heavy Metals | NMT 20 ppm |
| pH (1% Solution) | 5.0 – 7.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 2.0% |
| Melting Point | 150°C – 154°C |