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Karus Commences Preclinical Development of Novel Immune and Inflammation Programmes


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Karus Therapeutics Ltd, a company engaged in the discovery and development of de novo designed molecular-targeted small molecule drugs to treat inflammation and cancer, has commenced preclinical development of its HDAC6 and PI3-Kinase inhibitor programmes for the treatment of immune and inflammatory diseases such as rheumatoid arthritis (RA). Karus aims to initiate clinical trials for both programmes in 2011.

Karus’s highly potent and selective small molecule inhibitors of HDAC6 and PI3-Kinase p110-delta regulate T-helper 17 (Th17) cell function and inhibit the production of interleukins 17, 21 and 23 (IL-17, IL-21, IL-23). Th17 cells play a key role in the pathogenesis of immune and inflammatory diseases such as RA, multiple sclerosis, psoriasis, systemic lupus erythematosus and organ transplant rejection.

Karus’s compounds have been shown to inhibit the production of Th17 cell pro-inflammatory cytokines and, in preclinical models of RA, display efficacy comparable to the anti-TNF biologics.

Simon Kerry, CEO of Karus Therapeutics said: “There is a significant opportunity for the development of an important new class of anti-inflammatory drugs which selectively target Th17 cells via a novel mechanism of action. We are very excited by the potential of our development candidates as oral treatments for RA and other inflammatory diseases.”

Karus’s CSO, Dr Stephen Shuttleworth, will be presenting preclinical data from Karus’s PI3K p110-delta and dual p110-delta/beta inhibitor programmes, at the inaugural Targeting the PI3K Pathway conference held as part of Cambridge Healthtech Institute’s 8th International Discovery on Target conference in Boston between 2-3 November 2010.

Dr Shuttleworth’s presentation, entitled, “Design and Development of Novel, Isoform-Selective PI3K Inhibitors for the Treatment of Immune-Inflammatory Diseases and Cancer”, will discuss inhibitors of PI3K p110-delta, already acknowledged as an important target in the treatment of immune and inflammatory conditions, and inhibitors of PI3K p110-beta, which is emerging as an important target in these disease areas.
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