ArQule is a biotechnology engaged in the research and development of the next generation, small molecule cancer therapeutics. The company’s current discovery efforts are based on the ArQule Kinase Inhibitor Platform (AKIP) and is centered on the identification of novel kinase inhibitors that are potent, selective, and that do not compete with ATP (adenosine triphosphate) for binding to the kinase.
The company reported today the start of patient dosing in a Phase 1 clinical trial with ARQ 087, an orally bioavailable, potent multi-kinase inhibitor with pan-FBFR (fibroblast growth factor receptor) activity. Fibroblast growth factors and their receptors play important roles in cell proliferation, cell differentiation, cell migration, cell survival, protein synthesis, and angiogenesis. Dysregulation of FGFR signaling has been implicated in a number of cancer, fueling significant interest in FGFRs as targets for therapeutic intervention.
The primary objective of the Phase 1 trial of ARQ 087 is to determine its safety, tolerability and recommended Phase 2 dose. Patients with metastatic sold tumors who are refractory to available therapies or for whom no standard systemic therapy exists will be enrolled in the study. The number of patients to be enrolled will depend on the number of patient cohorts investigated until dose-limiting toxicity is reached.
ArQule is looking forward to characterizing the activity of ARQ 087 in a clinical setting. Its chief medical officer, Brian Schwartz, M.D., said, “FGFR has been a difficult target to drug historically, and we are pleased that we have been able to do so through the application of the company’s proprietary ArQule Kinase Inhibitor Platform.”
For additional information about ArQule, the AKIP platform, and the company’s product pipeline, please visit www.ArQule.com
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