4-ASA-NA (AGI-022)

We are developing a modified release oral formulation of 4-aminosalicylate sodium (4-ASA-Na) for the induction and maintenance of remission of mild to moderate ulcerative colitis (UC). UC is a chronic, recurrent, relapsing and remitting inflammatory disease of the colon and/or rectum. We believe that our 4-ASA-Na product may offer certain advantages compared with current 5-aminosalicylic acid (5-ASA) based therapies which are commonly used to treat UC, including a superior tolerability profile, and a more reliable delivery to the affected sites in UC leading to a higher efficiency of therapy with potential dosing advantages.

In March 2006, we reported on the outcome of a human pharmacokinetics trial in 16 human subjects designed to characterise the in-vivo drug release profile and pharm-acokinetics of three delayed release/controlled release formulations of AGI-022 compared with a reference solution of 4-ASA-Na. The study demonstrated delayed and controlled in-vivo release profiles consistent with targeted colonic delivery. A lead formulation has been selected as optimal and will be the basis for future clinical development.

Based on the positive Phase I results, we have decided to progress this product into Phase II clinical evaluation for the treatment of UC. The goal of the planned Phase II study will be to confirm the efficacy/dosage advantages of the product in UC patients. Formulation development work and scale-up of manufacture is now underway and a Phase II trial design is being developed.