Development Pipeline
Development Pipeline | HIV | Cancer | Inflammatory Diseases
Chronic inflammatory diseases, which afflict millions of people worldwide, include rheumatoid arthritis, gout, inflammatory bowel disease and psoriasis. 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:
Gout
- An estimated 3-5 million people in the U.S. and approximately 5 million people in the European Union suffer from gout, which is the most common form of inflammatory arthritis in men over 40
- There have been no new therapies approved by the U.S. Food and Drug Administration for the treatment of hyperuricemia associated with gout in the past 40 years
Rheumatoid Arthritis
- Rheumatoid arthritis afflicts approximately 1% of the world's population1
- Approximately 1% of Americans, or 2.1 million people, have rheumatoid arthritis2
- 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 rheumatoid arthritis (RA), inflammatory bowel disease (IBD) and psoriasis, due to their ability to down-regulate inflammatory cytokines, such as TNF alpha. We are evaluating a broad range of compounds that inhibit MEK from several distinct chemical classes.
RDEA119, our lead development candidate from this program, has shown potential as a potent and selective inhibitor of MEK, and has demonstrated the ability to significantly inhibit cytokines, such as TNFa 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. In addition to RDEA119, we have completed a human micro-dose pharmacokinetic study of RDEA436, our lead second-generation MEK inhibitor, which has demonstrated the potential for once-daily oral dosing.
Gout, also known as metabolic arthritis, is a painful and debilitating disease caused by abnormally elevated levels of uric acid in the blood stream. These abnormally elevated levels lead to the deposition of uric acid crystals in and around the connective tissue of the joints and in the kidneys, leading to inflammation, the formation of disfiguring nodules (tophi), intermittent attacks of severe pain (acute flares), and kidney damage (nephropathy). While gout is a treatable condition, there are limited treatment options, and a number of adverse effects are associated with current therapies.
RDEA594, our lead development candidate for the treatment of patients with gout, is a major metabolite of RDEA806, our lead development compound for the treatment of HIV. RDEA594 does not have significant antiviral activity. Based on extensive in vitro and in vivo experiments, we believe that RDEA594 exhibits a concentration-dependent inhibitory effect on the URAT1 transporter-mediated uptake of uric acid. These effects are believed to result in the increase in urinary excretion of uric acid and reduction of serum uric acid levels observed following administration of RDEA806 in Phase 1 and Phase 2 clinical trials that included over 100 subjects. Approximately 90% of hyperuricemic patients are considered to be under-excretors of uric acid, so increasing excretion may provide the most physiologically appropriate treatment.
For more information regarding these programs please click here to view our most recent company presentation.
