Arqule completes acquisition and collaboration

Acquisition provides near-term cancer clinical candidate, discovery pipeline and molecular biology expertise while collaboration applies lead generation and optimisation platform to create novel small-molecule candidates for anti-infective targets

ArQule, a drug discovery and development company from Woburn, MA, US, has completed its acquisition of Cyclis Pharmaceuticals, a privately held cancer-therapeutics company. 'We are delighted to complete this acquisition,' said Dr Stephen A Hill, president and ceo of ArQule. 'ArQule is now able to combine its strengths in small-molecule chemistry and intelligent drug design with Cyclis' molecular biology expertise. We believe that this combination has the potential to deliver clinical candidates with improved activity and reduced toxicity over other molecular approaches and traditional cancer chemotherapy.'

'I believe that combining Cyclis' cutting-edge discovery research with ArQule's proven strength in chemistry can produce a uniquely strong drug development platform,' said Dr Samuel K Ackerman, Cyclis president and ceo, who will become an advisor to ArQule following the merger.

The company has also entered into a chemistry collaboration with Novartis Institutes for BioMedical Research, Inc. (NIBRI), an affiliate of Novartis AG. As part of this collaboration, ArQule will apply its integrated chemistry technology platform to generate and optimise small-molecule compounds for NIBRI's anti-infective drug discovery program. 'The addition of Novartis, one of the world's leading R&D organizations, to our list of partners is further validation of our chemistry technologies business, said Dr Hill. 'This announcement confirms our ability to add new customers for our chemistry services while continuing to build our internal proprietary portfolio of discovery and development programs.'

ArQule's portfolio

ArQule's oncology portfolio is based on a novel technology, Activated Checkpoint Therapy (ACT), which involves the activation of cell cycle checkpoint pathways and the resultant apoptosis, or programmed death, of abnormal cells. ArQule expects its lead cancer compound, CO-501, to enter Phase I clinical trials in 2003. In addition to CO-501, ArQule is pursuing a second-generation program based on a similar mechanism of action for the same pathway. ArQule also is applying ACT to two other discovery programs that target different pathways. The first involves discovering compounds to inhibit a series of proteins referred to as Cancer Survival Proteins or CSPs. CSPs are known to block checkpoint-mediated apoptosis. A second discovery effort is aimed at restoring the p53 pathway to cancer cells through an intracellular protein that has been shown to stimulate cancer cell death. In addition to cancer therapeutics, ArQule continues to advance its p38 MAP Kinase program for which the initial indication will be rheumatoid arthritis. The Company has a number of compounds in advanced lead optimisation that have demonstrated functional oral activity in a rat model of rheumatoid arthritis. In this established animal model, the data indicate that ArQule's compounds reduced joint swelling in a dose-dependent manner and were well tolerated at all doses studies. ArQule recently commenced pilot- toxicology studies in order to meet its goal of selecting a GLP-toxicology candidate by the end of the year.