Fruquintinib API is a synthetic, orally active, highly selective vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor. It primarily inhibits VEGFR-1, VEGFR-2 and VEGFR-3, which are important regulators of tumor angiogenesis. Fruquintinib is used in pharmaceutical formulations for the treatment of metastatic colorectal cancer in appropriate patients.
Fruquintinib is also known by the development code HMPL-013. It belongs to the quinazoline class of kinase inhibitors and contains a substituted benzofuran carboxamide structure. Its chemical name is 6-[(6,7-dimethoxyquinazolin-4-yl)oxy]-N,2-dimethyl-1-benzofuran-3-carboxamide.
The API has the molecular formula C₂₁H₁₉N₃O₅, molecular weight 393.39 g/mol, and CAS Registry Number 1194506-26-7. PubChem and commercial reference-standard suppliers confirm these identity parameters.
Fruquintinib is supplied as a white to off-white powder. FDA reports a pKa of 2.78 and pH-dependent aqueous solubility, with approximately 0.9 μg/mL at pH 6.8 and 129.9 μg/mL at pH 1.
| Property | Value |
|---|---|
| API Name | Fruquintinib |
| CAS Number | 1194506-26-7 |
| Molecular Formula | C₂₁H₁₉N₃O₅ |
| Molecular Weight | 393.39 g/mol |
| Development Code | HMPL-013 |
| Chemical Class | Quinazoline kinase inhibitor |
| Pharmacological Class | VEGFR inhibitor |
| Primary Targets | VEGFR-1, VEGFR-2, VEGFR-3 |
| Appearance | White to off-white powder |
| pKa | 2.78 |
Fruquintinib is a selective inhibitor of VEGFR-1, VEGFR-2 and VEGFR-3. These receptors participate in vascular endothelial growth factor signaling and angiogenesis.
By inhibiting VEGFR signaling, fruquintinib suppresses processes involved in the formation and maintenance of tumor-associated blood vessels. This anti-angiogenic activity can restrict the vascular support required for tumor growth and progression.
Reported biochemical activity demonstrates strong inhibition of VEGFR signaling, with PubChem listing IC₅₀ values of approximately 33 nM for VEGFR-1, 0.35 nM for VEGFR-2 and 35 nM for VEGFR-3.
Fruquintinib is used as an active ingredient in pharmaceutical formulations for metastatic colorectal cancer. The FDA-approved product FRUZAQLA contains fruquintinib in 1 mg and 5 mg capsules.
The API is relevant to:
Fruquintinib is a white to off-white powder. Its aqueous solubility is strongly dependent on pH. FDA data report approximately 0.9 μg/mL at pH 6.8, increasing substantially under acidic conditions to approximately 129.9 μg/mL at pH 1.
This pH-dependent solubility is an important consideration during preformulation, dissolution and analytical method development.
| 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 10 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |