Lenvatinib Mesylate is the mesylate salt of Lenvatinib, an orally active small-molecule tyrosine kinase inhibitor used in targeted cancer therapy. It inhibits multiple receptor tyrosine kinases involved in tumor growth, angiogenesis and cancer progression.
Lenvatinib primarily targets vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3) and also inhibits fibroblast growth factor receptors (FGFR1–4), platelet-derived growth factor receptor alpha (PDGFRα), KIT and RET.
By inhibiting these signaling pathways, Lenvatinib can interfere with tumor angiogenesis and proliferative signaling. Lenvatinib Mesylate is therefore an important pharmaceutical API for the development and manufacture of oncology formulations.
Lenvatinib Mesylate is a synthetic small-molecule pharmaceutical compound. It has the molecular formula C21H19ClN4O4 · CH4O3S and a molecular weight of approximately 634.0 g/mol.
The CAS Number of Lenvatinib Mesylate is 857890-39-2.
The mesylate salt improves the pharmaceutical properties of Lenvatinib and is the form used in marketed oral pharmaceutical formulations.
Lenvatinib is a multi-targeted tyrosine kinase inhibitor. It inhibits signaling mediated by VEGFR1, VEGFR2 and VEGFR3, thereby reducing VEGF-driven angiogenesis.
It also inhibits FGFR1, FGFR2, FGFR3 and FGFR4, which can contribute to tumor growth and resistance mechanisms. Additional kinase targets include PDGFRα, RET and KIT.
Through simultaneous inhibition of these pathways, Lenvatinib suppresses signaling associated with tumor-cell proliferation, vascular development and tumor progression.
Lenvatinib Mesylate is used in oral oncology formulations for approved indications including certain forms of thyroid cancer, renal cell carcinoma, hepatocellular carcinoma and endometrial carcinoma, depending on the applicable regulatory approval and combination regimen.
Its use and combination with other anticancer agents depend on the specific cancer type and approved labeling.
Lenvatinib Mesylate API can be evaluated using validated analytical procedures for identification, assay, related substances, water content, residual solvents, elemental impurities and other applicable quality attributes.
HPLC and suitable spectroscopic and chromatographic techniques may be used for identity, assay and purity testing. Control of related substances and degradation products is important for pharmaceutical-grade Lenvatinib Mesylate.
Acceptance criteria should be based on the applicable pharmacopoeial requirements, approved manufacturer's drug-substance specification, Certificate of Analysis and relevant regulatory requirements.
Lenvatinib Mesylate should be stored in a tightly closed pharmaceutical-grade container under controlled storage conditions. The material should be protected from excessive heat, moisture, direct light and contamination. Specific storage requirements should follow the applicable manufacturer's approved specification.
Lenvatinib Mesylate API may be supplied for qualified pharmaceutical manufacturing, formulation development, research and analytical applications. Product specifications, Certificate of Analysis, packaging details and regulatory documentation should be confirmed according to the intended application.
Lenvatinib Mesylate API is available for pharmaceutical development and manufacturing requirements subject to applicable quality and regulatory requirements. Customers can request product specifications, analytical documentation, Certificate of Analysis, packaging information and commercial details for their specific requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| 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% |