Inflammatory Disease Market Opportunity Overview

Chronic inflammatory diseases, which afflict millions of people worldwide, include gouty arthritis, rheumatoid arthritis, inflammatory bowel disease and psoriasis, among others. Our goal is to improve the quality of life for patients with these diseases by developing effective and safe oral therapies for their treatment. Our research and development program is focused on the following inflammatory diseases:

Gouty Arthritis

• Approximately 1.0 million people in the US suffer from gouty arthritis attacks
• Gouty arthritis is usually an extremely painful attack of gout with a rapid onset of joint inflammation. The joint inflammation is precipitated by deposits of uric acid crystals in the joint fluid (synovial fluid) and joint lining (synovial lining). Intense joint inflammation occurs as white blood cells engulf the uric acid crystals and release chemicals of inflammation, causing pain, heat, and redness of the joint tissues.

Rheumatoid Arthritis

• Rheumatoid arthritis afflicts approximately 1% of the world's population¹
• Approximately 1% of Americans, or 2.1 million people, have rheumatoid arthritis²

Inflammatory Bowel Disease

• Affects 1 million Americans, most of whom are diagnosed between age 15 and 35 years³
• Develops in about 30,000 Americans each year³

Mitogen-activated ERK kinase (MEK) is a protein kinase that regulates both the biosynthesis of, and response to, a number of growth factors that drive uncontrolled inflammation associated with many human diseases. Our scientists have discovered multiple series’ of MEK inhibitors that selectively interfere with these critical disease processes. We believe that MEK inhibitors may play an important role in the potential treatment of inflammatory diseases, such as gouty arthritis, rheumatoid arthritis (RA), inflammatory bowel disease (IBD) and psoriasis, due to their ability to down-regulate inflammatory cytokines, such as TNF alpha and their ability to penetrate synovial fluid. We are evaluating a broad range of compounds that inhibit MEK from several distinct chemical classes.

RDEA119, our lead product candidate from this program currently in clinical development for the treatment of both cancer and anti-inflammatory diseases, shown potential as a potent and selective inhibitor of MEK, and has demonstrated the ability to significantly inhibit cytokines, such as TNFα and IL-1ß, which play an important role in inflammation. Preclinical and clinical data suggest that RDEA119 has favorable pharmaceutical-like properties, including the potential for convenient once-daily oral dosing.

Our second-generation MEK inhibitors include a broad range of compounds from several distinct chemical classes, representing new chemical entities. We have selected RDEA436 as our second-generation product candidate from this program. Preclinical data shows that RDEA436 is a potent in vitro and in vivo inhibitor of MEK with low CNS penetration. The results of a human micro-dose pharmacokinetic study demonstrate that RDEA436 has favorable pharmacokinetic properties and a long half-life, indicating the potential for once daily dosing in humans.

For more information regarding these programs please click here to view our most recent company presentation.