KT-413

KT-413 is a novel, potent, and selective heterobifunctional small molecule protein degrader developed for the treatment of relapsed/refractory MYD88-mutant diffuse large B-cell lymphoma (DLBCL) and potentially other MYD88-mutant indications and IL-1R/NFκB-driven malignancies. It functions by mediating the degradation of interleukin-1 receptor associated kinase 4 (IRAK4) as well as the IMiD substrates Ikaros (IKZF1) and Aiolos (IKZF3), utilizing both targeted protein degradation and molecular glue mechanisms. By degrading these proteins, KT-413 aims to maximize NFκB inhibition while upregulating type I interferon response, restoring apoptotic signaling in cancer cells. Preclinical studies have shown strong antitumor activity in cell line-derived and patient-derived xenograft models of MYD88-mutant DLBCL. A phase 1 clinical trial is ongoing for B-cell lymphomas including MYD88 mutant ABC DLBCL[1][2][3][4][5][6][8].

Other names

IRAK IMiD degraderIRAKIMiD