Icotinib (BPI-2009H), a highly selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI), in two EGFR-mutated lung cancer cell lines compared to A549, a cell line without EGFR mutations. Icotinib blocked EGFR-mediated intracellular tyrosine phosphorylation (IC50 = 45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation.
|Cell lines||A431 cell line|
|Preparation method||MTT assay Cells (103/well) were seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37 ◦C. After 24 h, cells were treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 µM for 96 h. Cell proliferation was calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4.|
|Concentrations||0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 µM|
|Animal models||mice bearing A431, A549, H460 and HCT8 tumor xenografts|
|Dosages||30 mg/kg once a week|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Effect of the CYP2C19 genotype on the pharmacokinetics of icotinib in healthy male volunteers.
Ruan CJ, et al. Eur J Clin Pharmacol. 2012 May 15. PMID: 22585284.
Effects of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in EGFR-mutated non-small cell lung cancer.
Yang G, et al. Oncol Rep. 2012 Jun;27(6):2066-72. PMID: 22446631.
Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies.
Tan F, et al. Lung Cancer. 2012 May;76(2):177-82. PMID: 22112293.
Phase I trial of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in Chinese patients with non-small cell lung cancer.
Wang HP, et al. Chin Med J (Engl). 2011 Jul 5;124(13):1933. PMID: 22088449.
Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors.
Zhao Q, et al. Lung Cancer. 2011 Aug;73(2):195-202. PMID: 21144613.
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