Oncothyreon Presented Novel Checkpoint Kinase 1 Inhibitors at AACR Meeting

Oncothyreon Inc.

, a clinical-stage biopharmaceutical company, today announced the presentation of data highlighting the preclinical development of orally bioavailable, potent and selective checkpoint kinase 1 (Chk1) inhibitors. Results were presented at the American Association for Cancer Research (AACR) Annual Meeting 2016 in New Orleans. Chk1 is a protein kinase that plays a major role in the ability of cancer cells to respond to DNA damage and DNA replication stress. As a single agent, Chk1 inhibitors may selectively target cancer cells that have high replication stress, which can be caused by activation of oncogenic signaling and loss of tumor suppressor functions. Chk1 inhibitors may also be used in combination with chemotherapy, potentially enhancing cell death and increasing the efficacy of these agents. "The research presented at AACR describes the results of our efforts to identify highly potent and selective, orally bioavailable Chk1 inhibitors with compelling single-agent and combinatorial anti-tumor activity," said Scott Peterson, Ph.D, Chief Scientific Officer of Oncothyreon. "We believe the Chk1 program warrants further study as part of our strategy to develop a pipeline of novel, orally available, targeted agents designed to improve the lives and outcomes of patients with cancer." The Oncothyreon presentation, titled "Discovery and development of orally available subnanomolar potent checkpoint kinase 1 inhibitors as potential anticancer therapies" (Abstract #2721), highlights preclinical data demonstrating that select Chk1 inhibitors display subnanomolar biochemical and single-digit nanomolar cellular potency against Chk1. In addition, Oncothyreon Chk1 inhibitors are active against a diverse range of cancer cell lines derived from leukemias, lymphomas and solid tumors, and demonstrate synergistic activity in combination with the chemotherapeutic drugs gemcitabine or cytarabine. The pharmaceutical properties of the Chk1 inhibitors also indicate good metabolic stability and pharmacokinetic properties, with good oral bioavailability in preclinical models, which may allow for the development of optimized dosing schedules. The research was conducted pursuant to a research collaboration agreement with Sentinel Oncology.