EEDi-5285, an orally active and highly potent inhibitor targeting embryonic ectoderm development (EED) protein, exhibits anti-cancer activity. It demonstrates exceptional efficacy with an IC50 value of 0.2 nM, indicating robust binding affinity to the EED protein.

EED:0.2 nM (IC50)

EEDi-5285 effectively suppresses cell proliferation in lymphoma cell lines Pfeiffer and KARPAS422, which possess an EZH2 mutation, demonstrating inhibition concentrations (IC50) of 20 pM and 0.5 nM, respectively[1].

EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment results in complete and durable tumor regression in the KARPAS422 xenograft model. A single 100 mg/kg oral dose reduces H3K27me3 levels at 24 h in KARPAS422 tumor tissue. The compound achieves a Cmax of 1.8 μM, an AUC of 6.0 h▪μg/ml with 10 mg/kg orally, and an oral bioavailability (F) of 75%. It has a moderate volume of distribution of 1.4 L/kg and a terminal T1/2 of approximately 2 h[1].