University of Cambridge
Changing the story of cancer

Pioneering fragment-based drug discovery

Health

The use of fragment-based drug discovery, pioneered by a team of Cambridge chemists and biochemists, led to the foundation of Astex.

This transformed the way in which pharmaceutical companies can identify new lead compounds for drug discovery.

To date, more than 40 compounds discovered using fragment-based drug discovery have reached clinical trials.

The approach allows for the efficient exploration of chemical space by using small fragments to identify hotspots on protein targets, which are then elaborated into larger drug-like molecules.

Astex’s fragment-based drug discovery approach has led to the approval of three drugs in 75 countries, positively impacting patients with breast and urothelial cancer and leukaemia.

Cancer cells

Revolutionising drug discovery with Astex’s Pyramid™ technology

Astex Pharmaceuticals, a subsidiary of Otsuka Pharmaceutical, was founded in 1999 in Cambridge, UK. Co-founded by University of Cambridge researchers Professor Sir Tom Blundell and Professor Chris Abell, it has grown into a leading player in drug discovery and development.

Astex focuses on the discovery and development of drugs for oncology and central nervous system (CNS) disorders. Their mission is to leverage their proprietary fragment-based drug discovery platform, Pyramid™, to create innovative small-molecule therapies that address unmet medical needs. By understanding the molecular basis of diseases, Astex aims to develop targeted therapies that can arrest or reverse disease progression, ultimately improving patient outcomes.

Astex has made significant contributions to the field of drug discovery, particularly through their fragment-based drug discovery (FBDD) approach. This method has led to the development of several successful drugs, including ribociclib (Kisqali), a CDK4/6 inhibitor for breast cancer, and erdafitinib (Balversa), an FGFR inhibitor for urothelial carcinoma. Additionally, Astex has initiated a Phase I clinical study for a new anti-cancer compound, demonstrating their ongoing commitment to advancing cancer treatment. Their collaborative efforts with major pharmaceutical companies and research institutions have been pivotal in bringing these innovative therapies to market.

Over the years, Astex Pharmaceuticals raised a total of $118 million through several funding rounds, with Cambridge Enterprise being a key investor in the earlier stages, supporting the company’s growth and development. Following its merger with SuperGen Inc. in 2011, Astex was acquired by Otsuka Pharmaceutical in 2013 for approximately $866 million, enhancing Otsuka’s drug research and development capabilities and oncology portfolio through Astex’s innovative fragment-based drug discovery technology.

Image credits:

Banner: Unsplash
In text image: Astex Pharmaceuticals