EZM2302

EZM2302 is an inhibitor of protein arginine methyltransferase 4 (PRMT4; IC₅₀ = 6 nM).¹ It decreases asymmetric methylation of the PRMT4 substrate PABP1 (IC₅₀ = 0.038 µM) and increases levels of demethylated SmB (EC₅₀ = 0.018 µM) in RPMI-8226 multiple myeloma cells. EZM2302 inhibits proliferation in a panel of 36 hematopoietic cancer cell lines, with IC₅₀ values of less than 100 μM for nine of the 15 multiple myeloma cell lines included in the panel. It reduces tumor growth and decreases asymmetric PABP1 methylation in tumor tissue in an RPMI-8226 mouse xenograft model when administered at doses of 75, 150, and 300 mg/kg twice per day. Intrathecal injection of EZM2302 (10 µg) reduces acute mechanical allodynia and thermal hyperalgesia in a mouse model of neuropathic pain induced by chronic constriction injury (CCI).²

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1. Drew, A.E., Moradei, O., Jacques, S.L., et al. Identification of a CARM1 inhibitor with potent in vitro and in vivo activity in preclinical models of multiple myeloma. Sci. Rep. 7(1), 17993 (2017).

2. Mo, K., Xu, H., Gong, H., et al. Dorsal root ganglia coactivator-associated arginine methyltransferase 1 contributes to peripheral nerve injury-induced pain hypersensitivities. Neuroscience 394, 232-242 (2018).