- |||||||||| KTX-1001 / K36 Therap
Ktx-1029, a Potent, Selective MMSET/NSD2 Inhibitor Is Effective in t(4; 14) Multiple Myeloma Preclinical Models (Halls G-H (San Diego Convention Center)) - Nov 6, 2024 - Abstract #ASH2024ASH_5329;
P1
KTX-1029 compliments the orally-available clinical candidate, KTX-1001 that is being evaluated in an ongoing clinical trial for relapsed/refractory MM patients. Preclinical data with KTX-1029 adds to the body of evidence for targeting MMSET in MM patients with t(4; 14) and for further exploration of combination regimens with MM standards of care.
- |||||||||| KTX-1001 / K36 Therap
Ectopic NSD2 Remodels H3K36me2 and DNA Methylation to Promote Oncogenic Gene Expression in Multiple Myeloma (Halls G-H (San Diego Convention Center)) - Nov 6, 2024 - Abstract #ASH2024ASH_4814;
P, P1
Currently, KTX-1001 is a first-in-class catalytic NSD2 inhibitor in a phase 1 clinical trial (NCT05651932)...We will present these results alongside data from extended NSD2 inhibitor treatments. We posit that elevated NSD2 in t(4; 14) MM causes excessive H3K36me2 leading to relative DNA hypermethylation and transcriptional dysregulation which can be reversed through extended pharmacologic inhibition of NSD2.
- |||||||||| Tazverik (tazemetostat) / Eisai, Ipsen, KTX-1001 / K36 Therap
Review, Journal: NSD family proteins: Rising stars as therapeutic targets. (Pubmed Central) - Feb 19, 2024
The NSD family of H3K36 methyltransferase enzymes-including NSD1 (KMT3B), NSD2 (MMSET/WHSC1), and NSD3 (WHSC1L1)-are now receiving drug development attention, with the exciting advent of an NSD2 inhibitor (KTX-1001) advancing to Phase I clinical trials for relapsed or refractory multiple myeloma...Multiple studies have implicated NSD proteins in human disease, noting impacts from translocations, aberrant expression, and various dysfunctional somatic mutations. Here, we review the biological functions of NSD proteins, epigenetic cooperation related to NSD proteins, and the accumulating evidence linking these proteins to developmental disorders and tumorigenesis, while additionally considering prospects for the development of innovative epigenetic therapies.
- |||||||||| KTX-1001 / K36 Therap
Trial in Progress: A Phase 1 Study of KTX-1001, an Oral, First-in-Class, Selective MMSET Inhibitor in Patients with Relapsed and Refractory Multiple Myeloma (SDCC - Halls G-H) - Nov 3, 2023 - Abstract #ASH2023ASH_4332;
P1
This Phase 1 study will evaluate a potential treatment for RRMM utilizing KTX-1001, which is a novel, first-in-class, potent, oral small-molecule MMSET inhibitor. The study is open and actively enrolling patients at centers in the United States, Spain, France, and Canada.
- |||||||||| KTX-1001 / K36 Therap
Review, Journal: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2). (Pubmed Central) - Aug 14, 2023
In this Perspective, the structures and functions of NSD2, its roles in various human diseases, and the recent advances in drug discovery strategies targeting NSD2 have been summarized. The challenges, opportunities, and future directions for developing NSD2 inhibitors and degraders are also discussed.
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