CRT and Teva’s collaboration yields successful outcome with novel aPKC protein inhibitor cancer drug discovery candidate

The successful multi-year, cross-discipline, collaboration between CRT and Teva has produced a first-in-class, highly selective and orally-active pre-clinical candidate* inhibitor for development by Teva into possible new drug therapies for cancer patients.

The drug compound blocks the atypical class of Protein Kinase C (PKC) proteins that are differentially activated in defined subsets of cancer patients. The aPKC inhibitor pre-clinical candidate was discovered following lead optimisation of early stage compounds identified within the CRT Discovery Laboratories.  Teva provided significant resource and expertise during the collaborative research term to boost existing investment by Cancer Research UK.

The aPKC isoforms PKC iota and PKC zeta are types of enzymes called serine/threonine kinases that have a key role in regulating the formation of tumours (tumourigenesis), the early steps of tumour invasion and metastasis (tumour spread) to distant tissues, and the expansion and growth of cancer stem cells, which contribute to the emergence of tumour resistance to a variety of standard cancer therapies. Inhibition of the aPKC isoenzymes is an attractive target for anti-tumour treatments. Professors Peter Parker and Neil McDonald, at Cancer Research UK’s London Research Institute, significantly contributed to understanding the structural biology of the aPKC drug targets and their validation as important players in cancer cell growth and spread.

“The fruits of this collaboration are significant. These aPKC targets may play a role in a pathway that leads to the formation and progression of cancer. The ability to inhibit this pathway may provide a new approach to the treatment of multiple cancer types in a number of different patient populations”, said Dr. Michael Hayden, Teva’s President of Global R&D and Chief Scientific Officer.

Under the terms of the license, CRT receive an upfront payment, and will be eligible to receive future success-based development milestone payments and royalty payments upon reaching specified targets once the drug is marketed.

Dr Keith Blundy, Cancer Research Technology’s chief executive officer, said: “This successful outcome from our collaboration represents the pinnacle of a highly productive collaboration to discover and develop first-in-class inhibitors of aPKC.By working with our industry partner, Teva and academic collaborators, we’ve accessed a much wider range of specialist expertise and experience, and demonstrated our ability to execute successfully the development of novel inhibitors. This approach has allowed us to move fast on this project, ahead of other commercial and academic groups interested in developing atypical PKC inhibitors.”

For media enquiries please contact the Cancer Research UK press office on 020 3469 8300 or, out-of-hours, the duty press officer on 07050 264 059.

*Pre-clinical candidate:  A drug-like small molecule or biological therapeutic that will progress into preclinical, and if successful, into clinical development and may ultimately become a marketed medicine.

About the atypical isoforms of PKC (PKC iota and zeta):

PKC iota is a well studied member of the PKC family that has been proposed to be an oncogene - a gene that can directly cause cancer. High levels of active PKC iota are found in many cancers including colorectal, ovarian, pancreatic and non-small cell lung (NSCLC), and this predicts a poor clinical outcome.  The less well-studied PKC zeta has also been validated as a cancer target. The high level of selectivity for inhibition of atypical PKCs demonstrated by the developed inhibitors is important as it allows the exclusive targeting of the atypical PKCs.

About the Principal Scientists

Peter Parker is a Principal Scientist at Cancer Research UK’s London Research Institute, and also Professor of Cancer Studies at King’s College London.  Neil McDonald is a Principal Scientist at the London Research Institute and also Professor of Crystallography at Birkbeck College.

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 commercial.cancerresearchuk.org.

About Cancer Research UK

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