Karus's initial focus is the development of a new family of HDAC inhibitors (OS-HDI). HDACs are important drug targets that have attracted considerable pharmaceutical industry attention: one HDAC inhibitor has been approved (Vorinostat®) for the treatment of T-cell lymphoma and a handful are in advanced clinical testing for the treatment of various cancers. HDACs are enzymes that regulate gene activation and expression and Karus's OS-HDI regulate the expression of anti-proliferative proteins such as p21 that are 'silenced' in tumor cells.
Karus has used innovative chemistry to create its OS-HDI, which are synthetic variants of naturally-occurring depsipeptide HDAC inhibitors. The natural depsipeptides, including the Phase II drug Romidepsin®, show considerable promise as new treatments for cancer. Karus has synthetically optimized these natural products for use as human therapeutics: enhancing their potency and removing their liabilities.
Karus believes that its OS-HDI are the most potent HDAC inhibitors known which, combined with their unique pharmacodynamics and exquisite target selectivity, are expected to create best-in-class drugs for the treatment of a wide range of tumors in addition to inflammatory and autoimmune diseases such as rheumatoid arthritis and psoriasis.
Potency and selectivity are key challenges for the next generation of HDAC inhibitors. Karus's OS-HDI exhibit best-in-class biochemical and cellular activity - significantly greater than the approved drug, Vorinostat - and have an exquisite specificity profile for the HDAC superfamily.
Stephen Shuttleworth PhD FRSC, Chief Scientific Officer
Karus Therapeutics Ltd
John Fairclough Centre
University of Southampton
Highfield
Southampton
Hampshire SO17 1BJ
United Kingdom