Linaclotide: A Novel Approach to the Treatment of Irritable Bowel Syndrome

OBJECTIVE: To review the pharmacology, pharmacokinetics, efficacy, and safety of linaclotide for irritable bowel syndrome (IBS). DATA SOURCES: A literature search using PubMed (1966-August 2011) and International Pharmaceutical Abstracts (1970-July 2011) was conducted using the terms linaclotide and MD-1100. Additional publications were identified by reviewing bibliographies. Abstracts were included in the absence of published full studies. Product information was requested from the manufacturer. STUDY SELECTION AND DATA EXTRACTION: The search was limited to English-language publications. All available clinical trials of linaclotide pertinent to the pharmacology, pharmacokinetics, efficacy, and safety of linaclotide as a treatment for IBS were included. Animal studies were included in the absence of data in humans. DATA SYNTHESIS: Linaclotide is a guanylate cyclase-C agonist currently being studied in Phase 3 trials for the treatment of IBS with constipation Controlled clinical trials have found that linaclotide significantly improves the number of complete spontaneous bowel movements per week, in addition to symptoms such as abdominal pain/discomfort, bloating, and straining. The most common adverse event associated with linaclotide is diarrhea. CONCLUSIONS: Linaclotide appears to be a safe and effective treatment for IBS. Additional clinical trials will more fully elucidate the safety profile of linaclotide and better define its place in therapy.