Lenvatinib Mesylate 是一种多靶点抑制剂,作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效,IC50为4 nM/5.2,对VEGFR1/Flt-1作用效果稍弱,作用于VEGFR2/3比作用于FGFR1, PDGFRα/β选择性高10倍左右。
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Takayuki Nakagawa,et al. Lenvatinib in combination with golvatinib overcomes hepatocyte growth factor pathway-induced resistance to vascular endothelial growth factor receptor inhibitor. Cancer Sci. 2014 Jun; 105(6): 723–730. Published online 2014 Apr 28. doi: 10.1111/cas.12409.
[2] Loredana Lorusso,et al. Lenvatinib and other tyrosine kinase inhibitors for the treatment of radioiodine refractory, advanced, and progressive thyroid cancer. Onco Targets Ther. 2016; 9: 6467–6477. Published online 2016 Oct 20. doi: 10.2147/OTT.S84625.
分子式 C21H19ClN4O4.CH4O3S |
分子量 522.97 |
CAS号 857890-39-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02788708 | Fallopian Tube Carcinoma|Recurrent Ovarian Cancer|Primary Peritoneal Carcinoma|Recurrent Endometrial Cancer | Drug: Lenvatinib Mesylate|Drug: Paclitaxel|Other: Pharmacological Study | Floor Backes|Eisai Inc.|Ohio State University Comprehensive Cancer Center | Phase 1 | 2016-05-27 | 2017-02-12 |
NCT02430714 | Thyroid Neoplasms | Drug: Lenvatinib | Eisai Co., Ltd.|Eisai Inc. | 2015-05-20 | 2017-02-20 | |
NCT02973997 | Columnar Cell Variant Thyroid Gland Papillary Carcinoma|Follicular Variant Thyroid Gland Papillary Carcinoma|Poorly Differentiated Thyroid Gland Carcinoma|Recurrent Thyroid Gland Carcinoma|Stage III Differentiated Thyroid Gland Carcinoma|Stage III Thyroid Gland Follicular Carcinoma|Stage III Thyroid Gland Papillary Carcinoma|Stage IV Thyroid Gland Follicular Carcinoma|Stage IV Thyroid Gland Papillary Carcinoma|Stage IVA Differentiated Thyroid Gland Carcinoma|Stage IVA Thyroid Gland Follicular Carcinoma|Stage IVA Thyroid Gland Papillary Carcinoma|Stage IVB Differentiated Thyroid Gland Carcinoma|Stage IVB Thyroid Gland Follicular Carcinoma|Stage IVB Thyroid Gland Papillary Carcinoma|Stage IVC Differentiated Thyroid Gland Carcinoma|Stage IVC Thyroid Gland Follicular Carcinoma|Stage IVC Thyroid Gland Papillary Carcinoma|Tall Cell Variant Thyroid Gland Papillary Carcinoma|Thyroid Gland Oncocytic Follicular Carcinoma | Other: Laboratory Biomarker Analysis|Drug: Lenvatinib|Biological: Pembrolizumab | Academic and Community Cancer Research United|National Cancer Institute (NCI) | Phase 2 | 2017-04-01 | 2017-01-24 |
NCT03048877 | Differentiated Thyroid Cancer | Drug: Apatinib Oral Tablet|Drug: Placebo Oral Tablet | Peking Union Medical College Hospital | Phase 3 | 2016-12-01 | 2017-02-07 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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