Linaclotide, a synthetic guanylate cyclase C agonist, for the treatment of functional gastrointestinal disorders associated with constipation

References

• Higgins PD, Johanson JF. Epidemiology of constipation in North America: a systematic review. Am. J. Gastroenterol.99, 750–759 (2004).
   PubMed Web of Science ®Google Scholar
• Choung RS, Locke GR 3rd, Schleck CD et al. Cumulative incidence of chronic constipation: a population-based study 1988–2003. Aliment. Pharmacol. Ther.26, 1521–1528 (2007).
   PubMed Web of Science ®Google Scholar
• Sonnenberg A, Koch TR. Physician visits in the United States for constipation: 1958 to 1986. Dig. Dis. Sci.34, 606–611 (1989).
   PubMed Web of Science ®Google Scholar
• Bongers ME, Benninga MA, Maurice-Stam H et al. Health-related quality of life in young adults with symptoms of constipation continuing from childhood into adulthood. Health Qual. Life Outcomes7, 20 (2009).
   PubMed Web of Science ®Google Scholar
• Wang JP, Duan LP, Ye HJ et al. [Assessment of psychological status and quality of life in patients with functional constipation]. Zhonghua Nei Ke Za Zhi47, 460–463 (2008).
   PubMedGoogle Scholar
• Johanson JF, Drossman DA, Panas R et al. Clinical trial: Phase 2 study of lubiprostone for irritable bowel syndrome with constipation. Aliment. Pharmacol. Ther.27, 685–696 (2008).
   PubMed Web of Science ®Google Scholar
• Drossman DA, Chey WD, Johanson JF et al. Clinical trial: lubiprostone in patients with constipation-associated irritable bowel syndrome – results of two randomized, placebo-controlled studies. Aliment. Pharmacol. Ther.29, 329–341 (2009).
   PubMed Web of Science ®Google Scholar
• Johanson JF, Morton D, Geenen J et al. Multicenter, 4-week, double-blind, randomized, placebo-controlled trial of lubiprostone, a locally-acting type-2 chloride channel activator, in patients with chronic constipation. Am. J. Gastroenterol.103, 170–177 (2008).
   PubMed Web of Science ®Google Scholar
• Gershon MD, Tack J. The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gastroenterology132, 397–414 (2007).
   PubMed Web of Science ®Google Scholar
• Frampton JE. Prucalopride. Drugs69, 2463–2476 (2009).
   PubMed Web of Science ®Google Scholar
• Camilleri M, Kerstens R, Rykx A et al. A placebo-controlled trial of prucalopride for severe chronic constipation. N. Engl. J. Med.358, 2344–2354 (2008).
   PubMed Web of Science ®Google Scholar
• Bouras EP, Camilleri M, Burton DD et al. Prucalopride accelerates gastrointestinal and colonic transit in patients with constipation without a rectal evacuation disorder. Gastroenterology120, 354–360 (2001).
   PubMed Web of Science ®Google Scholar
• Emmanuel AV, Roy AJ, Nicholls TJ et al. Prucalopride, a systemic enterokinetic, for the treatment of constipation. Aliment. Pharmacol. Ther.16, 1347–1356 (2002).
   PubMed Web of Science ®Google Scholar
• Quigley EM, Vandeplassche L, Kerstens R et al. Clinical trial: the efficacy, impact on quality of life, and safety and tolerability of prucalopride in severe chronic constipation – a 12-week, randomized, double-blind, placebo-controlled study. Aliment. Pharmacol. Ther.29, 315–328 (2009).
   PubMed Web of Science ®Google Scholar
• Camilleri M, Vazquez-Roque MI, Burton D et al. Pharmacodynamic effects of a novel prokinetic 5-HT receptor agonist, ATI-7505, in humans. Neurogastroenterol. Motil.19, 30–38 (2007).
   PubMed Web of Science ®Google Scholar
• Manini ML, Camilleri M, Goldberg M et al. Effects of velusetrag (TD-5108) on gastrointestinal transit and bowel function in health and pharmacokinetics in health and constipation. Neurogastroenterol. Motil.22, 42–49, e7–e8 (2010).
   PubMed Web of Science ®Google Scholar
• Goldberg M, Li YP, Johanson JF et al. Clinical trial: the efficacy and tolerability of velusetrag, a selective 5-HT4 agonist with high intrinsic activity, in chronic idiopathic constipation – a 4-week, randomized, double-blind, placebo-controlled, dose-response study. Aliment. Pharmacol. Ther.32, 1102–1112 (2010).
   PubMed Web of Science ®Google Scholar
• Ao M, Venkatasubramanian J, Boonkaewwan C et al. Lubiprostone activates Cl(-) secretion via cAMP signaling and increases membrane CFTR in the human colon carcinoma cell line, T84. Dig. Dis. Sci.56, 339–351 (2011).
   PubMed Web of Science ®Google Scholar
• Bijvelds MJ, Bot AG, Escher JC et al. Activation of intestinal Cl- secretion by lubiprostone requires the cystic fibrosis transmembrane conductance regulator. Gastroenterology137, 976–985 (2009).
   PubMed Web of Science ®Google Scholar
• Lunsford TN, Harris LA. Lubiprostone: evaluation of the newest medication for the treatment of adult women with constipation-predominant irritable bowel syndrome. Int. J. Womens Health2, 361–374 (2010).
   PubMedGoogle Scholar
• Camilleri M, Bharucha AE, Ueno R et al. Effect of a selective chloride channel activator, lubiprostone, on gastrointestinal transit, gastric sensory, and motor functions in healthy volunteers. Am. J. Physiol. Gastrointest. Liver Physiol.290, G942–G947 (2006).
   PubMed Web of Science ®Google Scholar
• Sweetser S, Busciglio IA, Camilleri M et al. Effect of a chloride channel activator, lubiprostone, on colonic sensory and motor functions in healthy subjects. Am. J. Physiol. Gastrointest. Liver Physiol.296, G295–G301 (2009).
   PubMed Web of Science ®Google Scholar
• Shailubhai K, Talluto C, Comiskey S et al. Phase II clinical evaluation of SP-304, a guanylate cyclase-C agonist, for treatment of chronic constipation. Am. J. Gastroenterol.105, S487–S488 (2010).
   Google Scholar
• Simren M, Abrahamson H, Bajor A et al. The IBAT inhibitor A3309 – a promising treatment option for patients with chronic idiopathic constipation. Gastroenterology138, S223 (2010).
   Google Scholar
• Bharucha AE, Linden DR. Linaclotide – a secretagogue and antihyperalgesic agent – what next? Neurogastroenterol. Motil.22, 227–231 (2010).
   PubMed Web of Science ®Google Scholar
• Lucas KA, Pitari GM, Kazerounian S et al. Guanylyl cyclases and signaling by cyclic GMP. Pharmacol. Rev.52, 375–414 (2000).
   PubMed Web of Science ®Google Scholar
• Bryant AP, Busby RW, Bartolini WP et al. Linaclotide is a potent and selective guanylate cyclase C agonist that elicits pharmacological effects locally in the gastrointestinal tract. Life Sci.86, 760–765 (2010).
   PubMed Web of Science ®Google Scholar
• Harris LA, Crowell MD. Linaclotide, a new direction in the treatment of irritable bowel syndrome and chronic constipation. Curr. Opin. Mol. Ther.9, 403–410 (2007).
   PubMed Web of Science ®Google Scholar
• Schulz S, Lopez MJ, Kuhn M et al. Disruption of the guanylyl cyclase-C gene leads to a paradoxical phenotype of viable but heat-stable enterotoxin-resistant mice. J. Clin. Invest.100, 1590–1595 (1997).
   PubMed Web of Science ®Google Scholar
• Busby RW, Bryant AP, Cordero EA et al. The molecular target of MD-1100 is guanylate cyclase-C (GC-C), an apical receptor on intestinal epithelial cell. Gastroenterology128, A464 (2005).
   Google Scholar
• Busby RW, Bryant AP, Bartolini WP et al. Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit. Eur. J. Pharmacol.649, 328–335 (2010).
   PubMed Web of Science ®Google Scholar
• Bryant AP, Busby RW, Cordero EA et al. MD-1100, a therapeutic agent in development for the treatment of IBS-C, enhances intestinal secretion and transit, decreases visceral pain and is minimally absorbed in rats. Gastroenterology128, A464 (2005).
   Google Scholar
• Bryant AP, Busby RW, Cordero EA et al. The characterization of an active metabolite of MD-1100, a therapeutic agent in development for the treatment of IBS-C and chronic constipation. Gastroenterology130, Abstract T2034 (2006).
   Google Scholar
• Eutamene H, Bradesi S, Larauche M et al. Guanylate cyclase C-mediated antinociceptive effects of linaclotide in rodent models of visceral pain. Neurogastroenterol. Motil.22, 312-e84 (2010).
   PubMedGoogle Scholar
• Currie MG, Kurtz CB, Mahajan-Miklos S et al. Effects of single dose administration of MD-1100 on safety, tolerability, exposure, and stool consistency in healthy subjects. Am. J. Gastroenterol. S328 Poster 894 (2005).
   Google Scholar
• Kurtz CB, Fitch DA, Busby RW et al. Effects of multidose administration of MD-1100 on safety, tolerability, exposure, and pharmacodynamics in healthy subjects. Gastroenterology130, A26, Abstract 132 (2006).
   PubMed Web of Science ®Google Scholar
• Andresen V, Camilleri M, Busciglio IA et al. Effect of 5 days linaclotide on transit and bowel function in females with constipation-predominant irritable bowel syndrome. Gastroenterology133, 761–768 (2007).
   PubMed Web of Science ®Google Scholar
• Johnston JM, Kurtz CB, Drossman DA et al. Pilot study on the effect of linaclotide in patients with chronic constipation. Am. J. Gastroenterol.104, 125–132 (2009).
   PubMed Web of Science ®Google Scholar
• Lembo AJ, Kurtz CB, Macdougall JE et al. Efficacy of linaclotide for patients with chronic constipation. Gastroenterology138, 886–895, e1 (2010).
   PubMed Web of Science ®Google Scholar
• Johnston JM, Kurtz CB, Macdougall JE et al. Linaclotide improves abdominal pain and bowel habits in a Phase IIb study of patients with irritable bowel syndrome with constipation. Gastroenterology139, 1877–1886, e2 (2010).
   PubMed Web of Science ®Google Scholar
• Lembo AJ, Schneier H, Lavins BJ et al. Efficacy and safety of once daily linaclotide administered orally for 12-weeks in patients with chronic constipation: results from 2 randomized, double-blind, placebo-controlled Phase 3 trials. Gastroenterology138, S53–S54 (2010).
   Google Scholar