{
    "comments": "Linaclotide represents a first-in-class, oral <a href=\"FamilyDisplayForward?familyId=315#show_object_1750\" target=\"_blank\">guanylate cyclase 2C</a> activator <Reference id=24736/>. It is a synthetic analogue of pathological heat-stable bacterial enterotoxins, and retains the same intrachain disulfide bond structure essential for biological activity. <br>Marketed formulations contain linaclotide acetate (PubChem <a href=\"https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=16158207&loc=ec_rcs\" target=\"_blank\">CID 16158207</a>). See also <Ligand id=9069/>, the second approved GC-C activator.",
    "bioactivityComments": "",
    "clinicalUse": "Used to treat chronic constipation and irritable bowel syndrome (IBS) where constipation is the main symptom (IBS-C).",
    "mechanismOfAction": "Linaclotide mimics the action of heat-stable enterotoxins in the gut which would cause diarrhea <i>via</i> activation of the enzyme guanylate cyclase 2C (GUCY2C) <Reference id=24735/>. Linaclotide activation of guanylate cyclase 2C in the luminal aspect of intestinal epithelium causes increased cGMP levels and this causes activation of the cystic fibrosis transmembrane conductance regulator (CFTR), which controls chloride ion efflux from enterocytes lining the GI tract. The result is a net efflux of water into the intestinal lumen which softens stools and stimulates bowel movements <Reference id=24736/><Reference id=24734/>.",
    "absorptionAndDistribution": "",
    "metabolism": "",
    "elimination": "",
    "populationPharmacokinetics": "",
    "organFunctionImpairment": "",
    "immuno": "",
    "gtmp": ""
}