Lenvatinib Mesylate

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Cat Number

API857890392

CAS Number

857890-39-2

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Product Detail Description Scientific Support Customer Q&A

CAS Number

857890-39-2

Storage

Store at room temperature

Synonyms

E-7080 MESYLATE; Lenvatinib methanesulfonate; 3J78384F61; CHEBI:85995; DTXSID90235081; N-(4-((6-Carbamoyl-7-methoxyquinolin-4-yl)oxy)-2-chlorophenyl)-N'-cyclopropylurea monomethanesulfonate

Molecular Formula

C22H23ClN4O7S

Molecular Weight

523

Smiles

COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl.CS(=O)(=O)O

Appearance

White to off-white solid

Melting Point

>220°C (dec.)

General Description

Lenvatinib mesylate is a potent, orally available receptor tyrosine kinase (RTK) inhibitor with a unique binding mode.

Mechanism of Action

Lenvatinib potently inhibits the kinase activities of multiple proangiogenic and oncogenic receptors, including vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR1-3) and fibroblast growth factor receptors 1 through 4 (FGFR1-4). It also targets the rearranged during transfection (RET) proto-oncogene. This blockade leads to the inhibition of the VEGF receptor signal transduction pathway, suppression of endothelial cell proliferation and migration, and the induction of vascular endothelial cell apoptosis.

Application

Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer. It is also approved for use in combination with everolimus for advanced renal cell carcinoma and as a first-line treatment for unresectable hepatocellular carcinoma.

In this phase 3 trial (827 patients with advanced endometrial cancer after platinum‑based chemotherapy), lenvatinib plus pembrolizumab significantly improved progression‑free survival (median 6.6 vs. 3.8 months in pMMR population; HR 0.60) and overall survival (median 17.4 vs. 12.0 months; HR 0.68) compared with physician‑choice chemotherapy (doxorubicin or paclitaxel). Grade ≥3 adverse events occurred in 88.9% of the combination arm versus 72.7% of chemotherapy. The combination provides superior survival outcomes, albeit with higher toxicity.

Fig. 1 Progression-free Survival. (Makker V, et al., 2022)

References

Makker V, et al. Lenvatinib plus Pembrolizumab for Advanced Endometrial Cancer. N Engl J Med. 2022;386(5):437-448.

Does Lenvatinib Mesylate require protection from light during long-term storage?

Yes, it is photosensitive. Light exposure can cause photodegradation and discoloration. Store in light-resistant containers, preferably amber glass or original packaging.

What is the recommended storage temperature for Lenvatinib Mesylate?

Store at controlled room temperature (15-25°C). Avoid temperatures above 30°C, which can accelerate oxidative degradation of the quinoline ring.

Is Lenvatinib Mesylate hygroscopic, and how is this managed?

It is slightly hygroscopic. Under high humidity, it may absorb moisture and clump. Storage in tightly sealed containers with desiccant is recommended.

How is the impurity lenvatinib N-oxide (an oxidative degradation product) monitored?

This degradation product is quantified using a stability-indicating HPLC method, ensuring it remains below ICH qualification thresholds.