Phase 1 study of KTX2001 NSD2 inhibitor with darolutamide androgen receptor inhibitor

Study K36-MCRPC-001 is a first-in-human Phase 1 dose escalation trial by K36 Therapeutics, Inc., evaluating KTX2001—an NSD2 histone methyltransferase inhibitor—alone and with darolutamide, an androgen receptor inhibitor small molecule. The trial aims to establish optimal doses while monitoring adverse events and pharmacokinetics in men with metastatic castration-resistant prostate cancer, providing early insights into combining NSD2 inhibition with androgen receptor blockade; later-line mCRPC typically uses ARPIs and taxanes (± PARP for HRR-mut), and this tests epigenetic re-sensitizing of AR blockade.