Astex Therapeutics, the UK-based biotechnology company developing targeted therapies for oncology, confirms the commencement of a phase I study for AZD5363, a Protein Kinase B (PKB, also known as Akt) inhibitor. AZD5363 is a clinical candidate selected in January 2010 by AstraZeneca subsequent to its collaborative programme with Astex. The collaborative programme originated from an earlier Astex collaboration with The Institute of Cancer Research (ICR) and Cancer Research Technology Limited (CRT) which began in 2003.

AZD5363 is an orally active selective inhibitor of PKB/Akt, a key enzyme in the PI3K/PKB/mTOR tumour cell survival pathway, and dysregulation of this pathway leads to tumour resistance to a number of important anti-cancer drugs. Inhibition of PKB/Akt has potential in the treatment of a broad range of cancer types.

The phase I study, being conducted at multiple centres in Europe, is designed to investigate the safety, tolerability and preliminary anti-cancer activity of AZD5363 in patients with advanced solid tumours, and to identify a dose and schedule that can be used in phase II trials.

Commenting on the announcement, Harren Jhoti, chief executive officer of Astex, said: “We are delighted that the long-standing collaboration between AstraZeneca, Astex, The Institute of Cancer Research and Cancer Research Technology, has delivered this exciting new compound. We anticipate that targeted agents like AZD5363, when fully researched, will provide new therapeutic options to patients with cancers of high unmet medical need. This is the second of our partnered programmes to commence human clinical trials, and is a further example of the productivity of our drug discovery partnerships with major pharmaceutical companies.”

Astex discovers and develops novel small molecule therapeutics. Using its pioneering fragment-based drug discovery platform Pyramid, Astex has built a pipeline of molecularly-targeted oncology drugs, of which three are currently being tested in clinical trials with others in discovery and pre-clinical development.