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 2016.

ArQule has a long history of kinase drug discovery and development, having discovered and introduced eight kinase inhibitors into human clinical trials with a ninth about to enter the clinic.  Our drug discovery efforts have been informed by our historical expertise in chemistry, our work in rational drug design and in part by work done to better understand the binding mode of our kinase inhibitor, tivantinib, which targets the MET receptor kinase without competing with ATP. Our research programs in kinase inhibition evaluated the entire human kinome and identified comparable sites in approximately 270 kinases, some having roles in different therapeutic areas.  We also identified and developed kinase inhibitors that bind to an allosteric site. This body of work led to a deeper understanding of certain types of kinase inhibitors and their regulation and the ability to identify, distinguish and produce certain types of inhibitors.

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 either directly or with collaborators and to interrogate our library against new targets, including those in immunotherapy.

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