gIcare Pharma Inc., a specialty company develops innovative drugs in gastroenterology, has started a phase IIa study of GIC-1001, a novel  orally-administered opioid agonist drug candidate to provide sedation-free, colonic analgesia in patients undergoing colonoscopy. The double-blind, randomized, placebo-controlled, dose-ranging trial will enroll 240 patients in the US and Canada, to assess the efficacy and safety of GIC-1001 for sedation-less colorectal cancer (CRC) screening using video-colonoscopy.

“GIC-1001 was shown to be safe during phase I trials and we are pleased to announce that the first patient has been enrolled and completed treatment,” said Maxime Ranger, Ph.D., president and chief executive officer, gIcare Pharma Inc.

“The IND has been cleared, and both the FDA and Health Canada agreed with gIcare’s drug development plan. gIcare pharma obtained the support of regulatory agencies in the use of an innovative pain assessment methodology as primary endpoint,” said Sander van Deventer, MD, gastroenterologist and general partner at Forbion Capital.

“Over the last decade, there has been a significant increase in the use of therapeutics that induce moderate and deep sedation  during colonoscopy procedures. Annual sedation-related costs in colonoscopy exceed five billion dollars in the US and have yet to show a true procedural outcome benefitm” said Jamie Stiff, partner at Genesys Capital.

“Contrary to the current standard, GIC-1001 has the potential to provide significant procedural benefit while removing significant costs associated with moderate and deep sedation. It is clear that GIC-1001 aligns with the current US shift from fee-for-service to value-driven healthcare in the era of cost containment,” said Dr Ranger.

The  phase IIa, double-blind, placebo-controlled, dose-ranging study is designed to assess the safety and efficacy of GIC-1001 in 240 adult patients undergoing sedation-free, full colonoscopy. In the study, patients will be randomly assigned to one of three different dose levels (250, 375 or 500 mg) of GIC-1001, or matching placebo, for a three-day dose regimen (three times a day) and a 10th dose will be taken about two hours prior to the colonoscopy. The pharmacokinetics of GIC-1001 will be assessed on a subset of patients (N: 24). gIcare Pharma expects to provide topline results from the study in the second quarter of 2014.

GIC-1001 is an orally-administered, non-centrally-acting opioid agonist interacting with colonic mu- and kappa-opioid receptors. In addition to colon-restricted analgesia, the drug has significant antispasmodic effects, which are expected to reduce colonic spasms, facilitate the insertion and passage of the colonoscope, and then shorten the time to reach the caecum, without interfering with the patient’s normal gastrointestinal tract motility.