FACIT Gains Rights to WDR5 Inhibitors for MLL Leukemia

First-in-class epigenetic modifiers discovered by OICR positioned for collaborative development.

TORONTO, ON (December 8, 2015) – Fight Against Cancer Innovation Trust (“FACIT”) announced the acquisition of exclusive rights to a portfolio of first-in-class WDR5 inhibitors for the treatment of mixed lineage leukemia (MLL). A series of proprietary small molecule inhibitors were optimized based on the discovery of a chemical probe for WDR5. The original WDR5 probe (OICR-9429) was developed by drug discovery scientists at the Ontario Institute for Cancer Research (“OICR”), Structural Genomics Consortium (“SGC”) and other collaborators. As with other technologies within the portfolio, FACIT will be responsible for stewarding commercialization activities for the assets and leveraging development expertise within the OICR network.

MLL1 deregulation is reported in both acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML), and is also common in a variety of solid cancers. The WDR5 protein is critical for the formation and epigenetic activities of MLL1-associated methylation complexes. The series of epigenetic modifiers discovered by OICR target protein-protein interactions within the WDR5/MLL1 complex, and thereby disrupts methylation activities.

“Mixed Lineage Leukemia is an aggressive childhood cancer, making the team highly motivated to accelerate the development of these first-in-class WDR5 inhibitors. We are currently exploring opportunities with strategic pharmaceutical partners, investors and of course, ongoing work with the innovative drug discovery scientists at OICR,” said Jeff Courtney, Chief Commercial Officer of FACIT.

“With the growing recognition of the importance of epigenetic signalling, potent and selective small molecules targeting the WDR5/MLL1 interface present a potential therapeutic intervention in leukemias and some p53/myc-driven cancers. Upcoming healthcare conferences are a timely opportunity to implement our partnering strategy for this promising set of inhibitors as we seek to leverage private sector investment,” remarked David O’Neill, Vice President of Business Development at FACIT.

About WDR5

WDR5 is a scaffolding protein essential for assembly of epigenetic MLL1-associated methyltransferase complexes and proper histone modification, the dysregulation of which is strongly implicated in MLL leukemia. In addition to its importance in MLL leukemia, deregulation of WDR5 itself has been observed in bladder cancer, where overexpression correlates with poor patient survival. MLL1 mutations are common in a variety of solid cancers, including breast, colon, lung, and bladder.

About OICR

OICR is an innovative cancer research and development institute dedicated to prevention, early detection, diagnosis and treatment of cancer. The Institute is an independent, not-for-profit corporation, supported by the Government of Ontario. OICR and its funding partners support research programs that involve more than 1,700 investigators, clinician scientists, research staff and trainees in research institutes and in universities across the Province of Ontario as well as at its headquarters. OICR has key research program efforts underway in small molecules, biologics, stem cells, imaging, genomics, informatics and bio-computing. For more information, please visit the website at www.oicr.on.ca.


FACIT (Fight Against Cancer Innovation Trust) is an independent business entity established by the Ontario Institute for Cancer Research (OICR) to undertake and accelerate development and commercialization activities related to breakthrough cancer research, products and drug discovery from OICR and throughout Ontario. For more information, please visit the website at facit.ca or email info@facit.ca.


David O’Neill PhD
FACIT | Vice President, Business Development
O: 647-260-7973 | david.oneill@facit.ca

Download FACIT NR_Gains Rights to WDR5_2015 1208_final.pdf (276.97 KB)


FACIT actively manages our diverse portfolio of Ontario oncology assets (including therapeutics, imaging, diagnostics, and technology platforms) that span all stages of commercialization, from proof-of-concept to clinical development.



With critical seed funding, FACIT makes it possible for Ontario’s best cancer research discoveries to compete globally and reach patients.