K36’s program is the first to study targeting the histone lysine methyltransferase NSD2 (MMSET/WHSC1) for the treatment of hematologic and solid tumor malignancies. By targeting NSD2, K36’s clinical pipeline brings the promise of precision medicine to multiple types of malignancies.

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Gintemetostat (KTX-1001) is a first-in-class, oral, highly selective inhibitor of NSD2, which is overexpressed in up to 20% of multiple myeloma patients due to a t(4;14) translocation. The clinical trial K36-MMSET-001 is actively enrolling multiple myeloma patients in the United States, Canada, and Europe.  Updated clinical data presented demonstrated pharmacodynamic target engagement, an encouraging safety profile, and evidence of clinical activity in heavily pretreated patients with relapsed or refractory multiple myeloma.  Expansion cohorts are currently enrolling patients with t(4;14) multiple myeloma who have received 1-3 prior lines of therapy.  These expansions evaluate gintemetostat in combination with carfilzomib, mezigdomide, or pomalidomide.

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The K36-STRIKE-001 trial studies the oral, selective NSD2 inhibitor KTX-2001 for patients with metastatic castration-resistant prostate cancer (mCRPC) both as monotherapy and in combination with the androgen receptor pathway inhibitor darolutamide. The K36-STRIKE-001 trial is actively enrolling at clinical research centers across the United States.