Astex Therapeutics Awarded £2 Million from Wellcome Trust for Pioneering HCV Research

Published: Mar 30, 2009

Cambridge, UK, 24th March 2009. Astex Therapeutics Limited, the leading fragment based drug discovery company, today announced that it has received an award of up to £2 million from the Wellcome Trust under its “Seeding Drug Discovery” initiative to support the Company’s pioneering work in the area of infectious disease caused by Hepatitis C Virus (HCV).

The funding will support a project to identify novel inhibitors of Hepatitis C (HCV) NS3 protease - a key enzyme involved in viral replication. Astex has already successfully identified compounds that bind to a novel inhibitory site on the viral enzyme which is highly conserved across all genotypes of the HCV virus. Astex compounds have been shown to inhibit protease activity in drug resistant variants of HCV that have arisen in the clinic during treatment with active site inhibitors. As such the Astex compounds offer the potential to be differentiated from existing HCV protease inhibitors. Astex retains all commercial rights to the resulting drug candidates from this programme.

“We are delighted to have received this significant award from the Wellcome Trust to help us to fund this important project. Through the HCV project we are expanding the Company’s therapeutic focus to include virology alongside our significant oncology portfolio”, said Harren Jhoti, Chief Executive Officer at Astex. “We are very excited by our discovery of a novel allosteric pocket on the HCV protease target. This discovery exemplifies the power of our leading fragment-based drug discovery platform. We will look to exploit this discovery by developing a new generation of HCV protease inhibitors.”

The Seeding Drug Discovery programme is a five year, £91 million Wellcome Trust initiative that aims to develop drug-like, small molecules that will be the springboard for further research and development by the biotechnology and pharmaceutical industry in areas of unmet medical need.

An estimated 170 million people worldwide are infected with the hepatitis C virus (HCV), yet many remain unaware of their condition. The extended period of therapy (48 weeks), the severe side effects and the low response rate (~30%) associated with existing therapies represent significant quality of life and compliance issues for those affected with HCV. Thus, there is an urgent need for better tolerated and more efficacious medications with more manageable treatment options.

Targeting specific proteins required for viral replication has been a successful therapeutic approach in other viral diseases such as HIV. A number of compounds which target an indispensable HCV protein (NS3 protease) have progressed into clinical development (e.g. boceprevir, telaprevir). Though effective, they require frequent dosing and are subject to cross resistance in patient populations.

Astex’s “Fragment-Based Drug Discovery” approach has identified novel inhibitors which bind to a different regulatory site on the target viral protein and its programme aims to optimise these using the protein crystal structure to drive molecular design. Astex’s approach offers the opportunity to move away from peptide-based and macrocyclic derived inhibitors for these challenging drug targets bringing the potential for improved PK profiles and potentially once daily dosing regimes. The project aims to deliver potent and selective compounds with a different resistance profile suitable for monotherapy and combination therapies. This fragment-based approach has proven successful in other projects at Astex, generating experimental drug candidates which are in hospital trials in cancer patients.

Astex Therapeutics

Astex is a UK-based biotechnology company that discovers and develops novel small molecule therapeutics. Using its pioneering fragment-based drug discovery platform Pyramid™, Astex has built a pipeline of five molecularly-targeted oncology drugs, of which three are currently being tested in clinical trials and two are in pre-clinical development. In addition to its proprietary research programmes, Astex’s productivity in lead discovery has been endorsed through numerous partnerships with major pharmaceutical companies, including AstraZeneca, Bayer-Schering, Boehringer Ingelheim, Novartis and Johnson and Johnson.

For further information on Astex please visit the Company’s website at

The Wellcome Trust is the largest charity in the UK. It funds innovative biomedical research, in the UK and internationally, spending over £600 million each year to support the brightest scientists with the best ideas. The Wellcome Trust supports public debate about biomedical research and its impact on health and wellbeing.

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