NX-2127 (ETX2514 Triethylamine) is an orally active BTK inhibitor that induces degradation of mutant BTKC481S in cells.NX-2127 has potent antiproliferative activity and inhibits the proliferation of BTKC481S mutant TMD8 cells.NX-2127 potently catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) at 25 nM and 54 nM, respectively. NX-2127 is associated with the immune system, stimulating T cell activation and increasing IL-2 production in primary human T cells.

NX-2127 inhibits the proliferation of BTK-C481S mutant TMD8 cells with an EC50 value of <30 nM.[1]
NX-2127 increases IL-2 production in primary human T cells.[1]

NX-2127 (1 mg/kg; oral; once daily for 14 days) showed efficient degradation of BTK in cynomolgus monkeys.[1]
NX-2127 (oral administration) results in dose-proportional exposure and degradation of BTK in plasma to less than 10% of baseline levels in circulating and splenic B cells.[1]
NX-2127 produces superior tumor growth inhibition (TGI) in WT TMD8 and C481S mutant xenograft models in mice.[1]