TRPH-395

TRPH-395 is a first-in-class, orally available small molecule inhibitor of WD repeat domain 5 (WDR5), an epigenetic scaffolding protein that organizes histone-modifying complexes involved in transcriptional regulation, particularly in leukemias and other blood cancers.[1][2][3][9][13] Discovered at the Ontario Institute for Cancer Research and advanced by Triphase Accelerator (with commercialization support via FACIT/Propellon Therapeutics), the drug is designed to disrupt WDR5-mediated protein–protein interactions, thereby impairing histone methylation and oncogenic transcriptional programs in leukemia, lymphoma, and potentially solid tumors.[1][2][3][7][9][11][13] Celgene (now part of Bristol Myers Squibb) entered into a strategic option-to-acquire agreement valued at up to approximately $1 billion to develop TRPH-395 for blood cancers, though the asset has remained in the preclinical stage publicly, with broad anti-proliferative activity reported across a range of cancer cell lines.[2][5][7][9][11][13][14]