JBJ-09-063 is an oral allogenic epidermal growth factor inhibitor currently in preclinical development for the study of non-small cell lung cancer (NSCLC) with epidermal growth factor L858R mutations. The IC50s for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S were 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM, respectively. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and drug-resistant models.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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