Triple©\negative breast cancer (TNBC) is the most aggressive breast cancer subtype. ClpP is a component of the ClpXP protein complex localized in the mitochondrial matrix. Modifiers of ClpP activity have demonstrated anti-cancer properties. TR-107 is a potent chemical activator of the human mitochondrial protease ClpP, with excellent potency, specificity and drug-like properties. TR©\107 shows ClpP©\dependent growth inhibition in the low nanomolar range that is equipotent to Paclitaxel in TNBC cell models.  The pharmacokinetic properties of TR©\107 were compared with other known ClpP activators including ONC201 and ONC212. TR©\107 displayed excellent exposure and serum t1/2 after oral administration. Pharmacokinetic analysis were evaluated for pharmacokinetic properties in ICR mice by Medicilon.

Reference

Emily M J Fennell, et al. Characterization of TR-107, a novel chemical activator of the human mitochondrial protease ClpP. Pharmacol Res Perspect. 2022 Aug;10(4):e00993. doi: 10.1002/prp2.993.