Name | Lenvatinib |
CAS number | 417716-92-8 |
Description | Lenvatinib is an orally administered, small molecule, multi-targeted receptor tyrosine kinase inhibitor, assigned the CAS Registry Number 417716-92-8. |
Structural formula | |
Molecular Formula | C21H19ClN4O4 |
Molecular Weight | 426.85 g/mol |
Appearance | White powder |
Quality Standard | 99% |
Storage Condition | Cool dry place( away from the light) |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Lenvatinib is an orally administered, small molecule, multi-targeted receptor tyrosine kinase inhibitor, assigned the CAS Registry Number 417716-92-8. Its molecular structure is designed to competitively inhibit the ATP-binding sites of a broad spectrum of kinase targets. This structural design underpins its ability to simultaneously block signaling through vascular endothelial growth factor receptors, fibroblast growth factor receptors, platelet-derived growth factor receptor alpha, RET, and KIT. This multi-kinase inhibition profile is central to its therapeutic mechanism against various cancers.
The primary antitumor activity of lenvatinib stems from its dual action on both tumor angiogenesis and direct tumor proliferation. By potently inhibiting VEGFRs, it disrupts the formation of new tumor blood vessels. Concurrently, its inhibition of FGFRs and other pathways directly interferes with oncogenic signaling within the tumor cells themselves. This comprehensive blockade aims to starve the tumor of its blood supply while simultaneously hindering its growth and survival, making it effective against tumors dependent on these pathways.
Lenvatinib has several significant clinical applications. It is approved for the first-line treatment of advanced renal cell carcinoma, typically in combination with a programmed death-1 inhibitor. It is also a standard therapy for advanced, progressive radioactive iodine-refractory differentiated thyroid cancer. Furthermore, in combination with an anti-PD-1 antibody, it is indicated for the treatment of advanced endometrial carcinoma that is not microsatellite instability-high or mismatch repair deficient and has progressed following prior systemic therapy.
This medication is administered orally in capsule form, taken once daily with or without food. The dosage varies based on the cancer type and combination therapy, requiring careful adherence. It exhibits dose-dependent pharmacokinetics and is metabolized primarily by cytochrome P450 3A4, necessitating caution and potential dose adjustments when co-administered with strong CYP3A4 inducers or inhibitors. Treatment requires diligent patient monitoring for efficacy and the management of adverse effects.
The safety profile of lenvatinib is characterized by a high incidence of treatment-related adverse events, many of which are dose-dependent. The most common and clinically significant include hypertension, proteinuria, fatigue, diarrhea, decreased appetite, nausea, stomatitis, weight loss, and palmar-plantar erythrodysesthesia syndrome. Serious risks include cardiac dysfunction, arterial thromboembolic events, hepatotoxicity, renal failure, gastrointestinal perforation, and reversible posterior leukoencephalopathy syndrome. Proactive management, including dose interruptions, reductions, and supportive care, is essential for maintaining patients on therapy.
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