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gintemetostat + carfilzomib
- Development stage
- Unknown
- Lead developer
- K36 Therapeutics
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
KTX-1001 + Kyprolis is an investigational combination therapy consisting of gintemetostat (KTX-1001), a first-in-class small molecule inhibitor of the histone methyltransferase MMSET (NSD2/WHSC1), and carfilzomib (Kyprolis), an approved proteasome inhibitor. Developed by K36 Therapeutics, this regimen is primarily being evaluated for the treatment of relapsed or refractory multiple myeloma (RRMM), with a specific focus on patients harboring the t(4;14) chromosomal translocation. This translocation leads to the overexpression of NSD2, which promotes oncogenic dimethylation of histone H3 at lysine 36 (H3K36me2). By inhibiting NSD2, gintemetostat aims to reverse this epigenetic dysregulation, while carfilzomib provides synergistic anti-tumor activity through proteasome inhibition.
- Brand names
- Kyprolis
- Other names
- KTX-1001 + carfilzomibgintemetostat + carfilzomib
02
Targets
NSD2 (Histone-lysine N-methyltransferase NSD2)PSMB5 (Proteasome subunit beta Type-5)PSMB8 (Immunoproteasome)
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