ORY-1001 (RG-6016) is the only dual KDM1A/LSD1 inhibitor currently being moved forward to Phase I studies, and it is also the only KDM1A inhibitor in development for the treatment of neurodegenerative disease. In THP-1 (MLL-AF9) cells, ORY-1001 results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers. ORY-1001 also induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells. ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth in rodent MV(4;11) xenografts.
|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||Water 60 mg/mL|
KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease.
Maes T, et al. Epigenomics. 2015;7(4):609-26. PMID: 26111032.
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