FORMA Therapeutics and Cancer Research Technology to Discover Cancer Drugs Targeting Deubiquitinating Enzymes (DUBs)

WATERTOWN, Mass. & LONDON — FORMA Therapeutics and Cancer Research Technology, Ltd. (CRT), the commercialization company of Cancer Research UK (CRUK), announced today a bold research initiative to discover innovative tools, technologies and therapeutic drug candidates against a variety of protein homeostasis regulators called, deubiquitinating enzymes (DUBs). Under this agreement, FORMA will pair its ultra-efficient drug discovery capabilities with CRT's expertise in translating academic discoveries through its Discovery Laboratories (CRT-DL) and the exclusive world-class academic network of CRUK Principal Investigators.

"This initiative with CRT and CRUK has the potential to significantly accelerate our understanding of the relevant biological applications of DUBs, a key class of enzymes involved in regulating protein homeostasis," said Steven Tregay, Ph.D., President and CEO, FORMA Therapeutics. "We are particularly looking forward to working closely in this initiative with CRT's Discovery Laboratories and a group of preeminent investigators, who bring critical insights in this area of important biology and have proven track records in basic and translational research."

Keith Blundy, CEO of Cancer Research Technology stated, "Cancer Research UK's breadth of research combined with CRT-DL's drug discovery capabilities are a unique platform that has secured the FORMA relationship and will contribute to bringing breakthrough cancer therapeutics to patients."

Protein ubiquitination is involved in many cellular processes and its regulation is controlled in part by DUBs. Ubiquitin "tags" proteins for degradation, and DUBs remove this tag, providing a tool for manipulating protein levels (protein homeostasis) in a cell. Ubiquitin biology is therefore complex and important to a broad range of human diseases. FORMA and CRT-DL will leverage their combined strengths to explore the protease enzymes that regulate ubiquitin-dependent pathways implicated in cancer.

"DUBs represent an attractive area for drug discovery exploration. As key regulators of ubiquitin recycling, processing, proofreading and disassembly, there is a tremendous opportunity to build a franchise of complementary therapeutics targeting the diverse collections of protein complexes," stated Kenneth W. Bair, Ph.D., Chief Scientific Officer and Head of Research and Development for FORMA Therapeutics. Dr. Bair further noted that a tremendous investment is being made by several groups to propel protein homeostasis research and discoveries into the practice of medicine.

As part of this agreement, a collaborative consortium will be formed consisting of FORMA Therapeutics Inc. and up to ten FORMA ADDCos (Asset Discovery and Development Company) subsidiaries, Cancer Research Technology – Discovery Laboratories (CRT-DL) and initially five Principal Investigators including:

• Professors Michael Clague and Sylvie Urbé - University of Liverpool, Liverpool, UK
• Dr. Benedikt Kessler – The University of Oxford, UK
• Dr. David Komander – Medical Research Council, Laboratory of Molecular Biology, Cambridge, UK
• Dr. Huib Ovaa – Chemical Biology Laboratory, Netherlands Cancer Institute, The Netherlands.

These investigators will focus on furthering the consortium's understanding of biological and structural insights of DUBs, and assist the discovery teams to ensure the most relevant screening technologies and secondary characterization assays are deployed for selection of lead candidates. FORMA will provide research funding support and defined compensation payments for DUB-specific ADDCo programs that achieve specified milestones.

Rob Sarisky, Chief Business Officer, FORMA Therapeutics, stated, "We are pleased to have CRT participate as a cornerstone partner in FORMA's launch of the ADDCo framework. This vehicle allows our not-for-profit collaborators to access a capital efficient engine operating at scale, attain financial returns mirroring their contributions and collectively advance medical science within the framework of a unified team."

Harpal Kumar, Chief Executive of Cancer Research UK, added, "Our research is saving lives. We are making great progress in uncovering the causes of cancer to find better ways to tackle the disease. But there is much still to do and highly collaborative partnerships focused on novel biological pathways to deliver new treatments are urgently needed. This alliance with FORMA allows us to explore a very exciting emerging area of biology to identify and develop potential new cancer drugs that will hopefully benefit patients in the future."

About FORMA Therapeutics

FORMA Therapeutics targets essential cancer pathways to create transformative small molecule cancer therapies. FORMA's novel approach to accessing high value drug targets, many of which pose significant challenges to conventional discovery approaches, leverages the integration of its innovative drug discovery technologies and oncology expertise, enabling efficient screening, discovery and rational development of small molecule drug candidates with qualified cellular mechanisms of action. FORMA is leveraging translational and clinical development capabilities through their strategic relationship with Dr. Daniel Von Hoff and Translational Drug Development (TD2) to build a robust pipeline of transformative cancer therapies in areas such as tumor metabolism, epigenetics, protein homeostasis, and protein-protein interactions. FORMA is headquartered in Watertown, MA. www.formatherapeutics.com

About Cancer Research Technology

Cancer Research Technology (CRT) is a specialist commercialisation and development company, which aims to develop new discoveries in cancer research for the benefit of cancer patients. CRT works closely with leading international cancer scientists and their institutes to protect intellectual property arising from their research and to establish links with commercial partners. CRT facilitates the discovery, development and marketing of new cancer therapeutics, vaccines, diagnostics and enabling technologies. CRT is a wholly owned subsidiary of Cancer Research UK, the world's leading cancer charity dedicated to saving lives through research. Further information about CRT can be found at www.cancertechnology.com

About Cancer Research UK

Cancer Research UK is the world's leading cancer charity dedicated to saving lives through research. The charity's pioneering work into the prevention, diagnosis and treatment of cancer has helped save millions of lives. Cancer Research UK receives no government funding for its life-saving research. Every step it makes towards beating cancer relies on every pound donated. Cancer Research UK has been at the heart of the progress that has already seen survival rates in the UK double in the last forty years. Cancer Research UK supports research into all aspects of cancer through the work of over 4,000 scientists, doctors and nurses. Together with its partners and supporters, Cancer Research UK's vision is to bring forward the day when all cancers are cured.

For further information about Cancer Research UK's work or to find out how to support the charity, please call 0300 123 1022 or visit www.cancerresearchuk.org. Follow us on Twitter and Facebook