Galapagos completes enrollment in Phase II trial of GLPG0974 to treat ulcerative colitis

A total of 45 patients with mild to moderate ulcerative colitis are enrolled in the trial, which is designed to assess the safety, efficacy, pharmacokinetics and effects on selected biomarkers of GLPG0974.

In the 28-day trial, patients are randomized to receive either 200mg of GLPG0974 twice-daily or placebo (2:1 ratio).

The double-blind, placebo-controlled trial enrolled patients in multiple sites in four countries including Belgium, the Czech Republic, Latvia, and Slovakia, while the topline results are expected to be released in June 2014.

GLPG0974 is a potent inhibitor of FFA2 (free fatty acid receptor 2) and it aims to reduce migration of neutrophils into the gastro-intestinal tract as over-activity of neutrophils damages the bowel tissue and causes chronic inflammation in ulcerative colitis.

According to the company, FFA2 plays a major role in the migration of neutrophils and is over-expressed in ulcerative colitis patients.

Reduction of neutrophil activation and migration by inhibition of FFA2 is expected to offer a new anti-inflammatory treatment approach.

In healthy volunteers, 14 days of once- or twice-daily oral dosing of GLPG0974 was well-tolerated and safe up to the highest doses tested and a sustained suppression of a biomarker for neutrophil activation showed the desired pharmacodynamic activity.

The company said that bacteria produce free fatty acids by fermentation of food fibers in the gut, which attract neutrophils through the activation of the neutrophil FFA2 receptor.

Galapagos and AbbVie have signed a worldwide license agreement in the field of inflammation under which AbbVie will be responsible for further development and commercialization of GLPG0634 after Phase IIb.

Image: Endoscopic image of a bowel section known as the sigmoid colon afflicted with ulcerative colitis. Photo: courtesy of Kauczuk