Ulcerative colitis is a chronic relapsing inflammatory disease of the large bowel. Current therapies for mild and moderate cases of the disease rely mainly on aminosalicylates, but often efficacy is limited. Resistant or more severe cases can be treated with corticosteroids, immunosuppressants or anti-TNFα agents; however, adverse effects, an inconvenient dosing schedule and prohibitive price limit their long-term use.

Dersalazine sodium is a new chemical entity that will that will provide a new therapeutic alternative to corticosteroids, immunosuppressants and anti-TNFα treatments, helping patients to avoid the adverse effects commonly associated with the use of these therapies with worse tolerability profiles.

Dersalazine sodium is a small molecule drug resulting from the link of a potent Platelet-activating Factor (PAF) antagonist with anti-TNFα properties (UR-12715) and 5-aminosalicylic acid (5-ASA) by an azo bond. It is carried unaltered through the upper gastrointestinal tract until azo-reduction by the colonic bacteria splits the compound into the two metabolites. Unlike other azo-based products, the key anti-inflammatory action of dersalazine sodium is driven by the anti-PAF metabolite, and not by 5-ASA.

Dersalazine sodium has proven safe in a thorough program of toxicology and safety preclinical studies, and was safe and well tolerated in single and multiple escalating dose placebo-controlled studies in healthy volunteers.

A Phase IIa double-blind randomized mesalazine and placebo controlled multicenter trial in patients with mild to moderate UC has been recently completed. A significant and clinically relevant reduction of disease activity was observed only with dersalazine sodium as soon as 14 days, and clinical remission by day 28 was achieved by 46% of dersalazine sodium treated patients, as compared to 12% and 10% in mesalazine and placebo groups respectively.

Palau is seeking a licensing partner for the worldwide development and commercialization of dersalazine sodium.

DERSALAZINE SODIUM KEY FACTS