ArQule, Inc. (Nasdaq: ARQL) today announced the commencement of patient dosing in a Phase 1 clinical trial with ARQ 087, an orally bioavailable, potent multi-kinase inhibitor with pan-FGFR (fibroblast growth factor receptor) activity.
“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 (AKIP™),” said Brian Schwartz, M.D., chief medical officer of ArQule. “We look forward to characterizing the activity of ARQ 087 in the clinical setting.”
The primary objective of the Phase 1 trial with ARQ 087 is determine its safety, tolerability and recommended Phase 2 dose. Patients with metastatic solid tumors who are refractory to available therapies or for whom no standard systemic therapy exists will be enrolled. The number of patients expected to be enrolled will depend on the number of patient cohorts investigated until dose-limiting toxicity is reached.
Fibroblast growth factors (FGF) and their receptors (FGFR) 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 cancers, including squamous non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), gastric, liver, breast, ovarian, endometrial, and bladder carcinomas, fueling significant interest in FGFRs as targets for therapeutic intervention.
ArQule is a biotechnology company engaged in the research and development of next-generation, small-molecule cancer therapeutics. The Company’s targeted, broad-spectrum products and research programs are focused on key biological processes that are central to human cancers. ArQule’s lead product, in Phase 2 and Phase 3 clinical development, is tivantinib (ARQ 197), an oral, selective inhibitor of the c-MET receptor tyrosine kinase. The Company’s pipeline consists of ARQ 621, designed to inhibit the Eg5 kinesin motor protein, ARQ 736, designed to inhibit the RAF kinases, and ARQ 087, designed to inhibit fibroblast growth factor receptor (FGFR). ArQule’s current discovery efforts, which are based on the ArQule Kinase Inhibitor Platform (AKIP™), are focused on the identification of novel kinase inhibitors that are potent, selective and do not compete with ATP (adenosine triphosphate) for binding to the kinase.