K36’s program is the first to study the promise of targeting the methyltransferase nuclear receptor SET domain-containing 2 (NSD2, also known as MMSET) for the treatment of hematologic and solid tumor malignancies. By targeting NSD2, K36’s clinical pipeline aims to specifically address an underlying driver of cancer in multiple types of malignancies.

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Gintemetostat (KTX-1001) is a first-in-class, oral, highly selective inhibitor of MMSET, 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 resulting in the expansion of the K36-MMSET-001 trial. Expansion cohorts are currently enrolling patients with t(4;14) multiple myeloma who have received 1-3 prior lines of therapy and are evaluating gintemetostat in combination with carfilzomib, pomalidomide, and mezigdomide-based regimens.

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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 across clinical research centers in the United States.