BYL719 is an orally bioavailable, next generation PI3K α- isoform specific inhibitor with potential antineoplastic activity. BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations. In vivo, BYL719 shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 has a low clearance, a half-life of 8.5 h in humans and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC. BYL719 is currently in phase II clinical trial in adult patients with selected advanced solid tumors.
|Source||Int J Cancer (2015). Figure 1. BYL719|
|Method||Caspase 3/7 activity assay|
|Cell Lines||HOS and MOS-J cells|
|Incubation Time||24 and 48 hr|
|Results||After 72 hr of treatment, BYL719 significantly inhibited the cell growth of all osteosarcoma cell lines tested in a dosedependent manner with an IC50 ranging from 6 to 15 μM and with the IC90 from 24 to 42 μM at 72 hr.|
|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.
|Solubility||DMSO 72 mg/mL|
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