gintemetostat + pomalidomide

KTX-1001 + Pomalyst is an investigational combination therapy being developed by K36 Therapeutics for the treatment of relapsed or refractory multiple myeloma (RRMM), particularly in patients harboring the t(4;14) chromosomal translocation. This regimen combines gintemetostat (KTX-1001), a first-in-class, oral, selective small molecule inhibitor of the histone methyltransferase NSD2 (also known as MMSET or WHSC1), with pomalidomide (Pomalyst), an immunomodulatory drug (IMiD). In t(4;14) multiple myeloma, NSD2 is overexpressed, leading to pathological dimethylation of histone H3 lysine 36 (H3K36me2) and the activation of oncogenic gene expression programs. Pomalidomide acts by binding to the cereblon (CRBN) E3 ubiquitin ligase complex, which triggers the degradation of the transcription factors Ikaros and Aiolos, essential for myeloma cell survival. The combination is being evaluated in the Phase 1 clinical trial NCT05651932 to leverage the synergistic effects of epigenetic modulation and targeted protein degradation.

Brand names

PomalystImnovid

Other names

KTX-1001 + Pomalystgintemetostat + PomalystKTX-1001 + pomalidomide