Collaboration aims to discover drugs against cancer and inflammatory diseases.

Karus Therapeutics signed a collaboration agreement with Queen Mary, University of London to develop small molecule inhibitors of selected isoforms of phosphoinositide 3-kinases (PI3K) as treatments against inflammatory diseases and cancer.

The ultimate aim is to develop best-in-class PI3K inhibitors with unique selectivity profiles. “PI3K inhibition has emerged as an important therapeutic strategy for the treatment of cancer and inflammatory diseases,” comments Stephen Shuttleworth, Ph.D., CSO. “Our collaboration is focused on the characterization and development of a novel class of PI3K inhibitors.”
Karus was established in 2006 to design and develop small molecule anticancer and anti-inflammatory therapeutics that function through the regulation of epigenetic mechanisms and lipid kinase signaling pathways. The company’s two PI3K inhibitor programs in these indications are expected to move into full preclinical development in 2010.

Karus’ second therapeutic focus is on the discovery of novel histone deacetylase (HDAC) inhibitors. Its most advanced programs aim to develop novel, re-engineered HDAC inhibitors that display best-in-class in vitro potency and in vivo efficacy but lack the off-target and toxicity that generally limit the use of such molecules. The three lead HDAC inhibitor programs are in development for the treatment of solid tumors, rheumatoid arthritis, psoriasis, and organ transplant rejection. Karus says clinical trials could start during early 2010.

In June 2009, Karus also signed a collaborative research program with the Queen Elizabeth Hospital Renal Transplant Unit in London to investigate the in vitro mechanisms of action of histone deacetylase inhibitors in specific leukocyte subsets, allogenic responses, and in vivo models of transplant rejection.

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