ktx-2001 + darolutamide

KTX-2001 + darolutamide is an investigational **combination drug therapy** being tested for metastatic castration-resistant prostate cancer (mCRPC)[1][2][5][7]. KTX-2001 is a selective small molecule inhibitor of **nuclear receptor-binding SET domain protein 2 (NSD2)**, also known as MMSET/WHSC1, designed to block histone methylation at H3K36me2 and disrupt oncogenic pathways driven by NSD2[2][5][9]. **Darolutamide** is a marketed androgen receptor inhibitor that blocks androgen signaling critical to prostate cancer progression. The combination aims to synergistically inhibit both epigenetic drivers and androgen receptor signaling, potentially overcoming treatment resistance seen in advanced prostate cancers[1][2]. The regimen is administered orally, both as monotherapy and in combination, in ongoing clinical trials. KTX-2001 is developed and sponsored by K36 Therapeutics, with darolutamide provided by Bayer for clinical studies[2].

Brand names

Nubeqa (for darolutamide)

Other names

MMSET inhibitor + androgen receptor inhibitor