avadomide

Avadomide is a novel, orally available small molecule that acts as a cereblon-modulating agent with antineoplastic, antiangiogenic, and immunomodulatory activities. It binds to cereblon (CRBN), promoting the recruitment of hematopoietic transcription factors Aiolos and Ikaros to the Cullin 4 RING E3 ubiquitin ligase complex. This leads to their ubiquitination and proteasomal degradation, derepressing interferon-stimulated genes such as DDX58 and IRF7, which induces apoptosis in certain tumor cells. Degradation of Aiolos also derepresses the IL2 gene, enhancing interleukin‑2 production and T-cell proliferation. Avadomide may further activate natural killer (NK) cells for enhanced tumor cell killing. It is under clinical investigation for various cancers including diffuse large B-cell lymphoma (DLBCL), follicular lymphoma, non-Hodgkin lymphoma (NHL), multiple myeloma, solid tumors, and brain cancer[1][2][3][4][8].

Other names

avadomide3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione