Cancer

Oncology Market Opportunity Overview

Worldwide, an estimated 24.6 million people are living with cancer (within three years of diagnosis)¹
Approximately 10.5 million Americans are living with cancer²
There is a need for novel, targeted therapies with potentially greater efficacy and less toxicity.

We have developed inhibitors of mitogen-activated ERK kinase (MEK) for the treatment of cancer. Defects in the RAS/RAF/MEK/ERK signaling pathway are closely associated with the development of human tumors, such as melanoma, colon, lung and thyroid cancers. Since MEK is believed to play an important role in cancer cell proliferation, apoptosis and metastasis, inhibiting MEK signaling has promise in the treatment of many types of cancer. In April 2009, we entered into a license agreement with Bayer HealthCare to develop and commercialize our MEK inhibitors for the treatment of cancer.

Cancer Facts & Figures. Atlanta, GA: American Cancer Society; 2007.
Parkin DM, Bray F, Ferlay J, Pisani P. Global cancer statistics, 2002. CA: Cancer J Clin. 2005;55:74-108. Information current as of May 1, 2007.

RDEA119

RDEA119, currently in clinical development both as a single agent and in combination with sorafenib (Nexavar®; Bayer HealthCare, Onyx Pharmaceuticals), is a potent, non-ATP competitive, highly-selective inhibitor of MEK.
Preclinical and clinical data suggest that RDEA119 has favorable properties, including oral dosing, excellent selectivity and limited retention in the brain, which may result in a reduced risk of central nervous system (CNS) side effects at doses expected to be effective, a problem associated with other members of this class of compounds. In addition, RDEA119 has been shown to suppress tumor cell growth in-vitro and in-vivo. Phase 1 data have demonstrated that RDEA119 has a long half-life and favorable pharmacokinetic properties, allowing for once-daily oral dosing. Preclinical in-vitro and in-vivo oncology studies have demonstrated significant potential synergy across multiple tumor types when RDEA119 is used in combination with other approved anti-cancer therapeutics, including sorafenib. RDEA119 is currently being evaluated in advanced cancer patients with different tumor types as a single agent in a Phase 1 clinical study as well as in combination with sorafenib in a Phase 1/2 clinical study. Under the terms of our license agreement with Bayer, we are responsible for the completion of the studies currently being conducted with RDEA119. Thereafter, Bayer will be responsible for the further development and commercialization of RDEA119 and any of our other MEK inhibitors.