Science

An important focus of oncology research and development activities conducted by biopharmaceutical companies involves a class of proteins known as kinases, which play pivotal roles in modulating diverse cellular activities and have been identified as important drug targets in a number of cancers and other diseases. The historic success of kinase inhibitors such as Tarceva®, Gleevec® and Nexavar® focused attention on the kinase field, resulting in the increased development of next-generation inhibitors like Imbruvica® and Jakofi® that have achieved, or are about to achieve, blockbuster status. The global market for protein kinase inhibitors is expected to exceed $40 billion in 2017.

ArQule has a long history of kinase drug discovery and development, having discovered and introduced nine kinase inhibitors into clinical trials. Our drug discovery efforts have been informed by our historical expertise in chemistry, our work in rational drug design and by our insight into kinase binding and regulation. We have applied this knowledge to produce significant chemical matter for a number of kinase targets and to build an extensive library of proprietary compounds with the potential to target multiple kinases in oncology and other therapeutic areas, such as rare diseases. We expect to bring further preclinical programs forward and to interrogate our library against new targets beyond kinases either directly or with collaborators.

Our proprietary pipeline of product candidates is directed toward molecular targets and biological processes with demonstrated roles in the development of both human cancers and rare, non-oncology diseases. All of these programs are being developed in targeted, biomarker-defined patient populations. By seeking out subgroups of patients that are most likely to respond to our drugs, we intend to identify small, often orphan, indications that allow for focused and efficient development. At the same time, in addition to pursuing these potentially fast-to-market strategies, we also pursue development in other indications that could allow us to expand the utility of the drugs if approved.

 

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