レンバチニブ 化学特性,用途語,生産方法
用途
レンバチニブ（Lenvatinib）は、エーザイが開発したマルチキナーゼ阻害薬であり、様々ながんの治療に用いられ得る。VEGFR2（英語版）キナーゼおよびVEGFR3（英語版）キナーゼを阻害する。
放射性ヨウ素による治療に抵抗性の甲状腺癌の治療薬として希少疾病用医薬品に指定されている。
効能
抗悪性腫瘍薬, 受容体チロシンキナーゼ阻害薬
説明
Lenvatinib is an inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and VEGFR3 (IC
50s = 4 and 5.2 nM, respectively). It also inhibits the related kinases VEGFR1, FGFR1, PDGFRα, PDGFRβ and Kit (IC
50s = 22, 46, 51, 39, and 100 nM, respectively). Lenvatinib (30 mg/kg, twice per day) reduces tumor growth in an H146 small cell lung cancer mouse xenograft model and induces tumor regression when administered at a dose of 100 mg/kg twice per day. Formulations containing lenvatinib have been used in the treatment of differentiated thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma.
特性
Class: receptor protein-tyrosine kinase
Treatment: DTC, RCC, HCC
Elimination half-life = 28 h
Protein binding = 98–99%
使用
E7080 (Lenvatinib) is a multi-target inhibitor of VEGFR2 and VEGFR3 with IC50 of 4 nM and 5.2 nM, respectively.
定義
ChEBI: A member of the class of quinolines that is the carboxamide of 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxylic acid. A multi-kinase inhibitor and orphan drug used (as its mesylate salt) for the treatment of various types
of thyroid cancer that do not respond to radioiodine.
副作用
The most common side effects of LENVIMA (lenvatinib) in people treated for thyroid cancer include tiredness; joint and muscle pain; decreased appetite; weight loss; nausea; mouth sores; headache; vomiting; rash, redness, itching, or peeling of your skin on your hands and feet; stomach (abdomen) pain; and hoarseness.
The most common side effects of LENVIMA when given with everolimus in people treated for kidney cancer include tiredness; joint and muscle pain; decreased appetite; vomiting; nausea; mouth sores; swelling in your arms and legs; cough; stomach (abdomen) pain; trouble breathing; rash; weight loss; and bleeding.
The most common side effects of LENVIMA in people treated for liver cancer include tiredness; decreased appetite; joint and muscle pain; weight loss; stomach (abdomen) pain; rash, redness, itching, or peeling of your skin on your hands and feet; hoarseness; bleeding; change in thyroid hormone levels; nausea.
レンバチニブ 上流と下流の製品情報
原材料
準備製品