Oral B-RAF kinase inhibitors find
ArQule, from Woburn, MA has discovered a proprietary series of potent (nanomolar range), orally active inhibitors of RAF kinases with anti-tumour activity in a xenograft human cancer model.
ArQule, from Woburn, MA has discovered a proprietary series of potent (nanomolar range), orally active inhibitors of RAF kinases with anti-tumour activity in a xenograft human cancer model.
'I am extremely encouraged that we have been able to integrate ArQule's proprietary chemistry with the growing strength and stature of the ArQule Biomedical Institute,' said Dr. Stephen Hill, president and ceo of ArQule.
RAF Kinase Inhibitors
This programme comprises a series of compounds which inhibit both B-RAF and c-RAF kinases in the nanomolar range. RAS/RAF pathway mutations underlie upwards of 30% of all human cancers and B-RAF mutations have been implicated in nearly 70% of human melanomas as well as lower percentages of other cancers. Recent clinical experience in the public domain supports the potential of novel therapeutics acting on this pathway. Certain compounds which inhibit RAF kinases may in addition demonstrate anti-angiogenic properties. ArQule intends to thoroughly explore this new series of compounds with the plan of filing an IND between Q4 2005 and Q2 2006. "Activated Checkpoint Therapy (ACT) approaches remain the core focus of ArQule's research and development activities. Preclinical data shows synergistic activity of ACT compounds with a range of other therapeutic agents, including gemcitabine and taxol. In addition, Arqule intend to explore the potential for proprietary therapeutic regimens which combine ACT compounds with more recently validated, targeted approaches such as the RAS/RAF pathway," said Dr Chiang Li, chief scientific officer and vice president, head of ArQule Biomedical Institute.