Race Oncology Ltd (ASX:RAC) is forging ahead with its Pillar 3 ‘Beyond Zantrene’ strategy by aiming to add new drugs for use in cancer and other indications to its pipeline.
To help the precision oncology company in its pursuit, the Monash Fragment Platform (MFP) at Monash University in Melbourne has been contracted to complete a fragment-based screening program to discover novel drugs that inhibit the m6A RNA demethylases FTO and ALKBH5.
Led by eminent medicinal chemist and director of the MFP Professor Martin Scanlon, the project will begin immediately using the latest techniques in nuclear magnetic resonance spectroscopy (NMR). Results will be reported over the next 12 months.
Race will own all the intellectual property developed in the project, which is expected to cost $286,786.
“Addition of new FTO inhibitors to Race’s drug pipeline creates major value as it grows Race ‘Beyond Zantrene’ and positions us as a world-leading RNA epitranscriptomics pharma company,” Race chief executive officer Phil Lynch said.
Stopping the major culprits
Important scientific discoveries made over the last decade have identified dysregulation (loss of control) of RNA epigenetics (epitranscriptomics) as a key driver of cancer and other complex diseases.
They are caused by the Fatso/FaT and Obesity associated (FTO) and ALKBH5 proteins, two of the only m6A RNA demethylases found in humans. Changes in the expression of FTO or ALKBH5 have a profound impact on cancer growth, spread and resistance to treatment.
Inhibiting FTO or ALKBH5 activity is able to kill or slow the growth of a wide range of cancers, including leukaemia, breast, lung, ovarian, gastric, brain, melanoma, pancreatic, kidney and many more.
Race’s most advanced asset Zantrene® is a potent inhibitor of FTO and is the only m6A RNA demethylase inhibitor and RNA epitranscriptomic drug in the clinic.
Expanding portfolio
Race principal scientist Professor Mike Kelso said: “Race is extremely pleased to be working with Professor Scanlon and his experienced team on this important project. The discovery and patenting of new FTO and ALKBH5 inhibitors will greatly strengthen Race’s drug development pipeline and add valuable assets to our expanding IP portfolio.
“Drawing on my career in medicinal chemistry, I relish the downstream challenge of evolving molecules discovered in this campaign into clinic-ready FTO and ALKBH5 inhibitors as innovative new treatments for cancer and other diseases.”
Professor Scanlon said: “Developing next-generation medicines requires outstanding discovery science. The Monash Fragment Platform was established to help researchers accelerate this long and complex journey. We are delighted to be working with Race to use our established Fragment-Based Screening technology to identify novel inhibitors for FTO and ALKBH5.”
A Professor of Medicinal Chemistry at the Monash Institute of Pharmaceutical Sciences, Scanlon has published more than 100 papers in high-ranking international journals and has led more than 30 successful fragment-based discovery campaigns at MFP for academic and industry clients since its inception in 2015.