乐伐替尼甲磺酸盐；甲磺酸乐伐替尼；甲磺酸仑伐替尼；lenvatinib Mesilate；lenvatinib Mesylate; 857890-39-2

产品描述

等级：活性药物成分（API）

化学名称：4-{3-氯-4-[（环丙基氨基）氨基]苯氧基}-7-甲氧基-6-喹啉甲酰胺

分子式：C21H19ClN4O4

分子量：426.853

规范：按照ChP/USP/EP建立企业标准

外观:粉

总杂质：不大于0.5%

纯度：不低于99%

残留溶剂：完全符合ICH Q3C要求

致突变杂质：完全符合ICH M8

亚硝胺评估：可用

粒度：可根据客户要求进行普通级或研磨/筛分

储存方法：室温

生产能力：商用

标准包装：1公斤/袋，5公斤/袋或根据客户要求

产品用途

Lenvatinib API是一种受体酪氨酸激酶（RTK）抑制剂，可抑制血管内皮生长因子（VEGF）受体VEGFR1 （FLT1）、VEGFR2 （KDR）和VEGFR3 （FLT4）的激酶活性。Lenvatinib还抑制其他与致病性血管生成、肿瘤生长和癌症进展有关的RTKs，包括成纤维细胞生长因子（FGF）受体FGFR1、2、3和4；这些位于细胞膜上的受体酪氨酸激酶（RTKs）在信号转导通路的激活中起着核心作用，这些信号转导通路参与细胞过程的正常调节，如细胞增殖、迁移、凋亡和分化，以及在致病性血管生成、淋巴生成、肿瘤生长和癌症进展中。特别是，VEGF已被确定为生理性和病理性血管生成的关键调节因子，并且在许多类型的癌症中，VEGF表达的增加与预后不良有关。

Lenvatinib API适用于局部复发或转移性进展性放射性碘（RAI）难治性分化甲状腺癌患者的治疗。大多数甲状腺癌患者通过手术和激素治疗有很好的预后（98%的5年生存率）。然而，对于rai难治性甲状腺癌患者，治疗选择有限，预后较差，这促使人们推动开发更有针对性的治疗方法，如lenvatinib。

联系方式

四川青木制药有限公司

四川省眉山市东坡区经济开发区东区顺江大道南段55号

国际营销部(International):

Email: sales@eastonpharma.cn 

Tel: 028-87827187

国内营销部(Mainland)：

李经理 13880480517   

杨经理 15982276454

Product Description

• Grade: Active Pharmaceutical Ingredient(API)

• Chemical Name: 4-{3-Chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxy-6-quinolinecarboxamide

• Molecular Formula: C21H19ClN4O4

• Molecular Weight: 426.853

• Specification: Enterprise Standard established according to ChP/USP/EP

• Appearance: Powder

• Total impurities: not more than 0.5%

• Purity: not less than 99%

• Residual Solvents: fully comply with ICH Q3C

• Mutagenic impurities: fully comply with ICH M8

• Nitrosamine assessment: available

• Particle size: regular grade or milling/sieving according to customer’s requirement.

• Storage: Room temperature

• Production capacity: Commercial

• Standard Package: 1kg/bag, 5kg/bag or  according to customer’s requirement.

Applications 

• Lenvatinib API is a receptor tyrosine  kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR),  and VEGFR3 (FLT4). Lenvatinib also inhibits other RTKs that have been  implicated in pathogenic angiogenesis, tumor growth, and cancer  progression in addition to their normal cellular functions, including  fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet-derived growth factor receptor alpha (PDGFRα), KIT, and RET. These receptor tyrosine kinases (RTKs) located in the cell membrane play a central role in the activation of signal transduction pathways involved in the normal regulation of cellular processes, such as cell proliferation,      migration, apoptosis and differentiation, and in pathogenic angiogenesis, lymphogenesis, tumor growth, and cancer progression. In particular, VEGF has been identified as a crucial regulator of both physiologic and  pathologic angiogenesis and increased expression of VEGF is associated  with a poor prognosis in many types of cancers.

• Lenvatinib API is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer. Most patients with thyroid cancer have a very good prognosis with treatment (98% 5-year survival rate) involving surgery and hormone therapy. However, for patients with RAI-refractory thyroid cancer, treatment options are limited and the prognosis is poor, leading to a push for the development of more targeted therapies such as lenvatinib.

Contact Information

Sichuan Qingmu Pharmaceutical Co., Ltd.

Add: No. 55, South Shunjiang Avenue, East Economic Development Zone, Dongpo District, Meishan City, Sichuan, 620036, China

International Marketing Department: 

Email: sales@eastonpharma.cn 

Tel: 0086-28-87827187