Lenvatinib Mesylate CAS 857890-39-2

what is Lenvatinib mesylate?

Lenvatinib mesylate is used alone or with other drugs to treat certain types of endometrial cancer, renal cell carcinoma (a type of kidney cancer), hepatocellular carcinoma (a type of liver cancer), and thyroid cancer. It is also being studied in the treatment of other types of cancer. Lenvatinib mesylate blocks certain proteins, which may help keep cancer cells from growing and may kill them. It may also prevent the growth of new blood vessels that tumors need to grow. Lenvatinib mesylate is a type of tyrosine kinase inhibitor and a type of antiangiogenesis agent. Also called Lenvima.

Product name	lenvatinib Mesylate
CAS	857890-39-2
Molecular formula	C22H23ClN4O7S
Molecular weight	522.95862
EINECS Number	812-398-0
Storage condition	-20°C Freezer
Appearance	white powder
melting point	>220°C (dec.)
Solubility	Soluble in DMSO (small amount), methanol (small amount)

Does Lenvatinib Mesylate have biological activity?

LenvatinibMesylate (E7080) is a synthetic and orally active inhibitor of tyrosinekinase, which can inhibit vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor (PDGFR α), stem cell factor receptor (Kit (c-Kit)), and rearrange them during transfection (RET (c-RET)). Lenvatinib mesylate has potential anti-tumor activity.

 

What cancer treatments can Lenvatinib mesylate be used for?

Endometrial carcinoma that is advanced and got worse after other systemic therapies. It is used with pembrolizumab in patients whose cancer is not microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR) and cannot be treated with surgery or radiation therapy.

Hepatocellular carcinoma (a type of liver cancer). It is used as the first treatment in patients whose cancer cannot be removed by surgery.

Renal cell carcinoma (a type of kidney cancer) that is advanced. It is used:With everolimus in adults who have received angiogenesis inhibitor therapy.With pembrolizumab as the first treatment in adults.

Thyroid cancer in certain patients whose cancer got worse, came back, or has spread to other parts of the body and did not respond to treatment with radioactive iodine.If you have same need,Click email：sales1@faithfulbio.com

 

Product Specification

Analysis tests	Standard	Result
Appearance	yellow to white powder	Conforms
Identification	H-NMR	Conforms
Individual impurity	≤0.5%	0.23%
Total impurity	≤1.0%	0.33%
Purity	≧99.0%	99.67%

Conclusion：Conform with specification and qualified.

 

Does Lenvatinib Mesylate have any Adverse effects?

Hypertension (high blood pressure) was the most common side effect of Lenvatinib Mesylate in studies (73% of patients, versus 16% in the placebo group), followed by diarrhoea (67% vs. 17%) and fatigue (67% vs. 35%). Other common side effects included decreased appetite, hypotension (low blood pressure), thrombocytopenia (low blood platelet count), nausea, muscle and bone pain.

 

What is Pharmacokinetics for Lenvatinib Mesylate?

 

Lenvatinib Mesylate is absorbed quickly from the gut, reaching peak blood plasma concentrations after one to four hours (three to seven hours if taken with food). Bioavailability is estimated to be about 85%. The substance is almost completely (98–99%) bound to plasma proteins, mainly albumin. Lenvatinib is metabolized by the liver enzyme CYP3A4 to desmethyl-lenvatinib (M2). M2 and lenvatinib itself are oxidized by aldehyde oxidase (AO) to substances called M2' and M3', the main metabolites in the feces. Another metabolite, also mediated by a CYP enzyme, is the N-oxide M3. Non-enzymatic metabolization also occurs, resulting in a low potential for interactions with enzyme inhibitors and inducers. Terminal half-life is 28 hours, with about two thirds being excreted via the feces, and one quarter via the urine.

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