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Linaclotide
Linaclotide (marketed under the trade name Linzess and Constella) is a peptide agonist of the guanylate cyclase 2C. This compound reduces activation of colonic sensory neurons, reducing pain; and activates colonic motor neurons, which increases smooth muscle contraction and thus promotes bowel movements. It was approved by the FDA in August 2012 for the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation (IBS-C) in adults.
The National Institutes of Health (NIH) estimates that as many as 20% of Americans may experience signs of irritable bowel syndrome, with approximately one-third of those affected experiencing constipation often accompanied by abdominal pain, affecting as many as 10 million Americans. Laxatives can assist with constipation but do not treat pain, while use of opiates to treat pain can aggravate constipation. While low-cost laxatives and pain killers would likely be tried first, linaclotide targets both associated conditions in a once-daily pill.〔Pollack, Andrew. ("Drug for Irritable Bowel Achieves Goals in Trial" ), ''The New York Times'', September 13, 2010. Accessed September 14, 2010.〕
==Clinical trials==
In Phase I trials reported in January 2009 in ''The American Journal of Gastroenterology'', it was found that 42 patients with chronic constipation who participated in the randomized, double-blind, placebo-controlled study experienced relief and that the medication was well tolerated.〔Jeffrey M Johnston , Caroline B Kurtz , Douglas A Drossman , Anthony J Lembo , Brenda I Jeglinski , James E MacDougall , Stephen M Antonelli & Mark G Currie . ("Pilot Study on the Effect of Linaclotide in Patients With Chronic Constipation" ), ''The American Journal of Gastroenterology'' 104, 125–132 (1 January 2009) | . Accessed September 15, 2010.〕 In results of a first round of Phase III clinical trials announced in September 2010, Ironwood studied approximately 800 patients over 12 weeks who were given linaclotide or a placebo in a randomized double-blind trial. 34% of those receiving linaclotide experienced relief of pain and constipation, compared to 21% of patients who had taken the placebo. 50% of those receiving linaclotide saw a significant reduction in pain, versus 37% with the placebo, with pain reduction starting in the first week on the medication. 6% of patients left the study after experiencing diarrhea, the most commonly reported side effect.〔
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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