ArQule Enrolls First Patient in Phase 1 Trial with ARQ 087

ArQule, Inc.

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. 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.