產(chǎn)品描述
等級(jí)：活性藥物成分（API）
化學(xué)名稱：4-{3-氯-4-[（環(huán)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
規(guī)范：按照ChP/USP/EP建立企業(yè)標(biāo)準(zhǔn)
外觀:粉
總雜質(zhì)：不大于0.5%
純度：不低于99%
殘留溶劑：完全符合ICH Q3C要求
致突變雜質(zhì)：完全符合ICH M8
亞硝胺評(píng)估：可用
粒度：可根據(jù)客戶要求進(jìn)行普通級(jí)或研磨/篩分
儲(chǔ)存方法：室溫
生產(chǎn)能力：商用
標(biāo)準(zhǔn)包裝：1公斤/袋，5公斤/袋或根據(jù)客戶要求
產(chǎn)品用途
Lenvatinib API是一種受體酪氨酸激酶（RTK）抑制劑，可抑制血管內(nèi)皮生長(zhǎng)因子（VEGF）受體VEGFR1 （FLT1）、VEGFR2 （KDR）和VEGFR3 （FLT4）的激酶活性。Lenvatinib還抑制其他與致病性血管生成、腫瘤生長(zhǎng)和癌癥進(jìn)展有關(guān)的RTKs，包括成纖維細(xì)胞生長(zhǎng)因子（FGF）受體FGFR1、2、3和4；這些位于細(xì)胞膜上的受體酪氨酸激酶（RTKs）在信號(hào)轉(zhuǎn)導(dǎo)通路的激活中起著核心作用，這些信號(hào)轉(zhuǎn)導(dǎo)通路參與細(xì)胞過(guò)程的正常調(diào)節(jié)，如細(xì)胞增殖、遷移、凋亡和分化，以及在致病性血管生成、淋巴生成、腫瘤生長(zhǎng)和癌癥進(jìn)展中。特別是，VEGF已被確定為生理性和病理性血管生成的關(guān)鍵調(diào)節(jié)因子，并且在許多類型的癌癥中，VEGF表達(dá)的增加與預(yù)后不良有關(guān)。
Lenvatinib API適用于局部復(fù)發(fā)或轉(zhuǎn)移性進(jìn)展性放射性碘（RAI）難治性分化甲狀腺癌患者的治療。大多數(shù)甲狀腺癌患者通過(guò)手術(shù)和激素治療有很好的預(yù)后（98%的5年生存率）。然而，對(duì)于rai難治性甲狀腺癌患者，治療選擇有限，預(yù)后較差，這促使人們推動(dòng)開發(fā)更有針對(duì)性的治療方法，如lenvatinib。
聯(lián)系方式
四川青木制藥有限公司
四川省眉山市東坡區(qū)經(jīng)濟(jì)開發(fā)區(qū)東區(qū)順江大道南段55號(hào)
國(guó)際營(yíng)銷部(International):
Email: sales@eastonpharma.cn
Tel: 028-87827187
國(guó)內(nèi)營(yíng)銷部(Mainland)：
李經(jīng)理 13880480517
楊經(jīng)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
關(guān)鍵字： lenvatinib Mesilate;lenvatinib Mesylate;857890-39-2;甲磺酸樂(lè)伐替尼;甲磺酸侖伐替尼;
四川青木制藥有限公司（簡(jiǎn)稱“青木制藥”）成立于2011年，位于四川眉山，現(xiàn)有員工300余人，是一家專業(yè)從事特色原料藥及高端醫(yī)藥中間體研發(fā)、生產(chǎn)與銷售的高新技術(shù)企業(yè)，是成都苑東生物制藥股份有限公司（簡(jiǎn)稱“苑東生物”）的全資子公司。苑東生物成立于2009年，下設(shè)5家全資子公司，現(xiàn)有員工1100余人。苑東生物專注于麻醉鎮(zhèn)痛、糖尿病、心血管、抗腫瘤等重大疾病領(lǐng)域，先后實(shí)現(xiàn)了20余個(gè)制劑產(chǎn)品和近20個(gè)化學(xué)原料藥產(chǎn)品的產(chǎn)業(yè)化。公司于2020年9月在上海證券交易所科創(chuàng)板掛牌上市（股票代碼：688513）。
研發(fā)優(yōu)勢(shì)：
1.QbD+綠色化學(xué)理念
2.中外雙報(bào)
3.API晶型、工藝專利挑戰(zhàn)經(jīng)驗(yàn)
體系優(yōu)勢(shì)：
1.GMP體系健全：10次NMPA檢查，1次美國(guó)FDA檢查
2.符合歐/美/日GMP標(biāo)準(zhǔn): 3*JDMF， 4*USDMF，3*CEP
3.15臺(tái)液相，5臺(tái)氣相，ICP-MS、粒度儀、XRD、TGA、DSC等高端儀器。
工廠優(yōu)勢(shì)
1)2個(gè)API生產(chǎn)車間，16條常規(guī)API獨(dú)立生產(chǎn)線，4個(gè)獨(dú)立潔凈區(qū)，200臺(tái)（套）生產(chǎn)設(shè)備，反應(yīng)體積50~5000L。
2)4條OEB-4獨(dú)立生產(chǎn)線，1個(gè)獨(dú)立潔凈區(qū)，反應(yīng)體積20~1000L。
3)1條特殊反應(yīng)生產(chǎn)線，含6種國(guó)家重點(diǎn)監(jiān)控危險(xiǎn)反應(yīng)的自控系統(tǒng)：氫化、氯化、磺化、重氮化、烷基化、氧化。
4)高溫：250℃； 深冷：-100