Drug intelligence / Profile preview

KTX-1001 + mezigdomide

Development stage: Unknown
Lead developer: K36 Therapeutics
Modality: Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration: Oral

Overview

KTX-1001 + mezigdomide is an investigational combination therapy being developed by K36 Therapeutics for the treatment of relapsed and refractory multiple myeloma, particularly in patients harboring the t(4;14) chromosomal translocation. KTX-1001 (gintemetostat) is a first-in-class, orally available small molecule inhibitor of NSD2 (also known as MMSET), a histone methyltransferase that is overexpressed in the t(4;14) genetic subtype. Mezigdomide is a potent cereblon E3 ligase modulator (CELMoD) developed by Bristol Myers Squibb. Preclinical data suggest synergistic activity between the epigenetic modulation of NSD2 and the protein degradation mediated by mezigdomide. The combination is currently being evaluated in a Phase 1 clinical trial (NCT05651932) alongside dexamethasone.

Other names: gintemetostat + mezigdomideKTX-1001 + CC-92480

Targets

IKZF1 (Ikaros family zinc finger protein 1)CRBN (Cereblon)IKZF3 (Zinc finger protein Aiolos)NSD2 (Histone-lysine N-methyltransferase NSD2)

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