Dapansutrile (also known as OLT1177) exhibits exceptional attributes as a pharmaceutical product, most notably: compelling nonclinical efficacy and early clinical benefit, no observed human toxicity, an attractive pharmacokinetic profile and low cost of goods. Dapansutrile has a unique pharmacological profile, inhibiting inducible interleukin (IL)-1β and IL-18 production.
Dapansutrile's Clean Safety Profile
Clinical Experience to date
Olatec has completed four clinical trials with dapansutrile to date: one Phase 1 study in the oral dosage form as well as one Phase 1 and two Phase 2 studies in the topical dosage form. Across all four of these placebo-controlled clinical studies, dapansutrile has been found to be safe and well tolerated. No treatment-emergent serious adverse events have occurred. Additionally, none of the measured laboratory parameters, or cardiac or respiratory measures have indicated any safety issue with dapansutrile.
Topical Dapansutrile for the Treatment of Chronic Musculoskeletal Pain
Clinical Experience to date
Olatec has completed two placebo-controlled Phase 2 studies with the topical formulation of dapansutrile in patients with osteoarthritis (OA). In both the 2-week Phase 2 study as well as the 6-week Phase 2 study, topically applied dapansutrile demonstrated a reduction of pain that significantly exceeded the Minimal Clinically Important Improvement (MCII) as established in the literature . In both studies, the reduction of pain was most pronounced in the subset of subjects with more severe and advanced OA. In all three studies, dapansutrile exhibited a remarkably clean safety profile. Following approval in the OA indication, the Company plans to expand the label for the topical treatment of chronic musculoskeletal pain.
Musculoskeletal conditions (including osteoarthritis, back pain and tendinitis) afflict over 60 million people in the USA and 17 billion people worldwide, resulting in 156 million annual prescriptions or $21 billion in annual revenues. The market for osteoarthritis treatment is largely dominated by NSAIDs and mild opioids, and is estimated at $8 billion in annual prescription revenues.
Painful chronic musculoskeletal diseases are largely driven by the inflammatory properties of IL-1 and other proinflammatory cytokines. Proinflammatory cytokines are critical mediators in the disturbed metabolism and enhanced catabolism of tissue in an OA joint. Specifically, IL-1β, IL-18 and IL-6 are the main proinflammatory cytokines elevated in the pathophysiology of OA. 
Data from cellular and animal studies have provided substantial evidence that blocking IL-1β production could counteract the degradative mechanisms associated with OA pathology. Elevated tissue levels of IL-1β, IL-18 and IL-6 contribute to the pathogenesis of OA through several mechanisms including downregulation of anabolic events and upregulation of catabolic and inflammatory responses, effects that result in structural damage to the OA joint. 
Innovation in this market has been virtually non-existent for over two decades and currently available pharmaceuticals face challenges due to little or no patent protection and growing safety concerns among regulatory authorities of long-term toxicities associated with these existing drugs. Based on the evidence established to date, Olatec believes that the demonstrated advantages of dapansutrile, if approved, will position it as an important player in the OA market. In 2014, topical dapansutrile was forecasted by an independent strategic consulting firm to potentially achieve over $1 billion in peak annual sales globally, representing approximately 30% market share for topical treatments in the USA.  Olatec is exploring a variety of relevant alternatives for the potential commercialization of topical dapansutrile on a global basis.
Oral Dapansutrile for the Treatment of Acute Gout Flares
Gout in its acute and chronic forms is estimated to afflict over 8.8 million people in the USA, and significantly more worldwide . Acute gout flares are caused by a deposition of monosodium urate crystals around and in the tissues of the joint resulting in severe inflammation and pain.
The inflammation pathway involved in acute gout flares is largely driven by the dramatic increase in IL-1β. Inhibition of IL-1β has been shown in clinical studies to be effective in reducing the inflammation and pain caused by acute gout flares.
A significant opportunity exists for dapansutrile in the treatment of acute gout flares by the IL-1β pathway. Dapansutrile would be the first orally administered, tolerable, safe and effective therapy to reduce the inflammation and pain associated with acute gout flares. Given the large number of patients affected by this disease and the deficiencies of currently available therapies, dapansutrile has the potential to address this large unmet medical need and as a result, has the potential to capture major market share.
Other Disease Indications Currently in Preclinical Development for Dapansutrile
Several preclinical studies are ongoing in translational animal models to establish the disease-modifying activity of dapansutrile in a number of other conditions that have been established as IL-1β mediated diseases.