Review article: Linaclotide for the management of irritable bowel syndrome with constipation

Alimentary Pharmacology and Therapeutics

Volumn 39, Issue 4, 2014, Pages 371-384

  Layer, P ^a   Stanghellini, V ^b  

^a ISRAELITISCHES KRANKENHAUS   (Germany)

^b UNIVERSITY OF BOLOGNA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

LINACLOTIDE; PLACEBO;

ABDOMINAL DISTENSION; ABDOMINAL PAIN; ARTICLE; CONSTIPATION; DIARRHEA; DRUG EFFICACY; DRUG MECHANISM; DRUG RESPONSE; DRUG SAFETY; DRUG TOLERABILITY; FLATULENCE; GASTROINTESTINAL TRANSIT; HEADACHE; HUMAN; IRRITABLE BOWEL SYNDROME WITH CONSTIPATION; IRRITABLE COLON; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; TREATMENT DURATION; TREATMENT OUTCOME; VIRAL GASTROENTERITIS;

ABDOMINAL PAIN; ANIMALS; BIOLOGICAL AVAILABILITY; CONSTIPATION; DIARRHEA; GASTROINTESTINAL TRANSIT; HUMANS; IRRITABLE BOWEL SYNDROME; PEPTIDES; TREATMENT OUTCOME;

EID: 84892893221     PISSN: 02692813     EISSN: 13652036     Source Type: Journal    
DOI: 10.1111/apt.12604     Document Type: Article

References (73)

1. Chang L,. Review article: epidemiology and quality of life in functional gastrointestinal disorders. Aliment Pharmacol Ther 2004; 20: 31-9.
2. Hungin APS, Whorwell PJ, Tack J, et al,. The prevalence, patterns and impact of irritable bowel syndrome: an international survey of 40 000 subjects. Aliment Pharmacol Ther 2003; 17: 643-50.
3. Lovell RM, Ford AC,. Effect of gender on prevalence of irritable bowel syndrome in the community: systematic review and meta-analysis. Am J Gastroenterol 2012; 107: 991-1000.
4. Lovell RM, Ford AC,. Global prevalence of and risk factors for irritable bowel syndrome: a meta-analysis. Clin Gastroenterol Hepatol 2012; 10: 712-21.
5. Wilson S, Roberts L, Roalfe A, et al,. Prevalence of irritable bowel syndrome: a community survey. Br J Gen Pract 2004; 54: 495-502.
6. Hulisz D,. The burden of illness of irritable bowel syndrome: current challenges and hope for the future. J Manag Care Pharm 2004; 10: 299-309.
7. Frank L, Kleinman L, Rentz A, et al,. Health-related quality of life associated with irritable bowel syndrome: comparison with other chronic diseases. Clin Ther 2002; 24: 675-89.
8. Davis RH,. Overcoming barriers in irritable bowel syndrome with constipation (IBS-C). J Fam Pract 2009; 58: S3-7.
9. International Foundation for Functional Gastrointestinal Disorders. IBS patients: their illness experience and unmet needs, 2009. Available at: http://www.aboutibs.org/pdfs/IBSpatients.pdf. Accessed June 6, 2013.
10. Drossman DA, Morris CB, Schneck S, et al,. International survey of patients with IBS: symptom features and their severity, health status, treatments, and risk taking to achieve clinical benefit. J Clin Gastroenterol 2009; 43: 541-50.
11. Bigal ME, Serrano D, Reed M, et al,. Chronic migraine in the population: burden, diagnosis, and satisfaction with treatment. Neurology 2008; 71: 559-66.
12. Young AS, Klap R, Shoai R, et al,. Persistent depression and anxiety in the United States: prevalence and quality of care. Psychiatr Serv 2008; 59: 1391-8.
13. Müller-Lissner S, Tack J, Feng Y, et al,. Levels of satisfaction with current chronic constipation treatment options in Europe-an internet survey. Aliment Pharmacol Ther 2013; 37: 137-45.
14. Emmanuel A, Quigley E, Simrén M, et al,. Factors affecting satisfaction with treatment in European women with chronic constipation: an internet survey. United Eur Gastroenterol J 2013; 1: 375-84.
15. Longstreth GF, Thompson WG, Chey WD, et al,. Functional bowel disorders. Gastroenterology 2006; 130: 1480-91.
16. Mearin F, Balboa A, Badiá X, et al,. Irritable bowel syndrome subtypes according to bowel habit: revisiting the alternating subtype. Eur J Gastroenterol Hepatol 2003; 15: 165-72.
17. Dapoigny M, Bellanger J, Bonaz B, et al,. Irritable bowel syndrome in France: a common, debilitating and costly disorder. Eur J Gastroenterol Hepatol 2004; 16: 995-1001.
18. American Gastroenterological Association. American Gastroenterological Association medical position statement: irritable bowel syndrome. Gastroenterology 2002; 123: 2105-7.
19. Andresen V, Keller J, Pehl C, et al,. Irritable bowel syndrome-the main recommendations. Dtsch Arztebl Int 2011; 108: 751-60.
20. Tort S, Balboa A, Marzo M,., et al. Clinical practice guideline for irritable bowel syndrome. Gastroenterol Hepatol 2006; 29: 467-521.
21. Spiller R, Aziz Q, Creed F, et al,. Guidelines on the irritable bowel syndrome: mechanisms and practical management. Gut 2007; 56: 1770-98.
22. National Collaborating Centre for Nursing and Supportive Care, on behalf of NICE. Clinical practice guideline. Irritable bowel syndrome in adults: diagnosis and management of irritable bowel syndrome in primary care, 2008. Available at: www.ncbi.nlm.nih.gov/books/NBK51953. Accessed July 24, 2012.
23. Brandt LJ, Chey WD, Foxx-Orenstein AE, et al,. An evidence-based position statement on the management of irritable bowel syndrome. American College of Gastroenterology IBS Task Force. Am J Gastroenterol 2009; 104 (Suppl. 1): S1-35.
24. Layer P, Andresen V, Pehl C, et al,. Irritable bowel syndrome: German consensus guidelines on definition, pathophysiology and management. Z Gastroenterol 2011; 49: 237-93.
25. Quartero AO, Meineche-Schmidt V, Muris J, et al,. Bulking agents, antispasmodic and antidepressant medication for the treatment of irritable bowel syndrome. Cochrane Database Syst Rev 2005; 2: CD003460.
26. Ruepert L, Quartero AO, de Wit NJ, et al,. Bulking agents, antispasmodics and antidepressants for the treatment of irritable bowel syndrome. Cochrane Database Syst Rev 2011; 8: CD003460.
27. Francis CY, Whorwell PJ,. Bran and irritable bowel syndrome: time for reappraisal. Lancet 1994; 344: 39-40.
28. Gonlachanvit S, Coleski R, Owyang C, et al,. Inhibitory actions of a high fibre diet on intestinal gas transit in healthy volunteers. Gut 2004; 53: 1577-82.
29. Ford AC,. Management of irritable bowel syndrome. Minerva Gastroenterol Dietol 2009; 55: 273-87.
30. Heitkemper MM,. Evidence-based treatments for irritable bowel syndrome with constipation. J Fam Pract 2009; 58 (5 Suppl.): S13-20.
31. Ford AC, Talley NJ, Spiegel BMR, et al,. Effect of fibre, antispasmodics, and peppermint oil in the treatment of irritable bowel syndrome: systematic review and meta-analysis. BMJ 2008; 337: a2313.
32. Darvish-Damavandi M, Nikfar S, Abdollahi M,. A systematic review of efficacy and tolerability of mebeverine in irritable bowel syndrome. World J Gastroenterol 2010; 16: 547-53.
33. Gorard DA, Libby GW, Farthing MJ,. Influence of antidepressants on whole gut and orocaecal transit times in health and irritable bowel syndrome. Aliment Pharmacol Ther 1994; 8: 159-66.
34. 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 2009; 29: 329-41.
35. Johanson JF, Drossman DA, Panas R, et al,. Clinical trial: phase 2 study of lubiprostone for irritable bowel syndrome with constipation. Aliment Pharmacol Ther 2008; 27: 685-96.
36. Bharucha AE, Waldman SA,. Taking a lesson from microbial diarrheagenesis in the management of chronic constipation. Gastroenterology 2010; 138: 813-7.
37. 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 2010; 86: 760-5.
38. Giannella RA, Mann EA,. E. coli heat-stable enterotoxin and guanylyl cyclase C: new functions and unsuspected actions. Trans Am Clin Climatol Assoc 2003; 114: 67-85.
39. Schlossmann J, Feil R, Hofmann F,. Insights into cGMP signalling derived from cGMP kinase knockout mice. Front Biosci 2005; 10: 1279-89.
40. 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 2010; 649: 328-35.
41. Eutamene H, Bradesi S, Larauche M, et al,. Guanylate cyclase C-mediated antinociceptive effects of linaclotide in rodent models of visceral pain. Neurogastroenterol Motil 2010; 22: 312-e84.
42. Castro J, Harrington AM, Hughes PA, et al,. Linaclotide inhibits colonic nociceptors and relieves abdominal pain via guanylate cyclase-C and extracellular cyclic guanosine 3',5'-monophosphate. Gastroenterology 2013; 145: 1334-46.
43. Silos-Santiago I, Hannig G, Eutamene H, et al,. Gastrointestinal pain: unraveling a novel endogenous pathway through uroguanylin/guanylate cyclase-C/cGMP activation. Pain 2013; 154: 1820-30.
44. Busby RW, Bryant AP, Bartolini WP,. MM-419447 is an active in vivo metabolite of linaclotide, a therapeutic agent in development for the treatment of IBS-C and chronic constipation. Drug Metab Rev 2006; 38: 96-7.
45. Busby RW, Kessler MM, Bartolini WP, et al,. Pharmacologic properties, metabolism, and disposition of linaclotide, a novel therapeutic peptide approved for the treatment of irritable bowel syndrome with constipation and chronic idiopathic constipation. J Pharmacol Exp Ther 2013; 344: 196-206.
46. Currie MG, Kurtz CB, Mahajan-Miklos S, et al,. Effects of single dose administration of MD-110 on safety, tolerability, exposure, and stool consistency in healthy subjects. Am J Gastroenterol 2005; 100 (Suppl. 9): S328 (abs 984).
47. Kurtz CB, Fitch DA, Busby RW, et al,. Effects of multidose administration of MD-1100 on safety, tolerability, exposure, and pharmacodynamics in healthy subjects. Gastroenterology 2006; 130 (Suppl. 2): A26 (abs 132).
48. Lee N, Wald A,. The pharmacokinetics, pharmacodynamics, clinical efficacy, safety and tolerability of linaclotide. Expert Opin Drug Metab Toxicol 2011; 7: 651-9.
49. Chey WD, Lembo AJ, Lavins BJ, et al,. Linaclotide for irritable bowel syndrome with constipation: a 26-week, randomized, double-blind, placebo-controlled trial to evaluate efficacy and safety. Am J Gastroenterol 2012; 107: 1702-12.
50. Rao S, Lembo AJ, Shiff SJ, et al,. A 12-week, randomized, controlled trial with a 4-week randomized withdrawal period to evaluate the efficacy and safety of linaclotide in irritable bowel syndrome with constipation. Am J Gastroenterol 2012; 107: 1714-24.
51. Lucas KA, Pitari GM, Kazerounian S, et al,. Guanylyl cyclases and signaling by cyclic GMP. Pharmacol Rev 2000; 52: 375-414.
52. Laney DW Jr, Bezerra JA, Kosiba JL, et al,. Upregulation of Escherichia coli heat-stable enterotoxin receptor in regenerating rat liver. Am J Physiol 1994; 266: G899-906.
53. Scheving LA, Russell WE,. Guanylyl cyclase C is up-regulated by nonparenchymal cells and hepatocytes in regenerating rat liver. Cancer Res 1996; 56: 5186-91.
54. ® Summary of Product Characteristics, 2012. Available at: http://www.ema.europa.eu/docs/en- GB/document-library/EPAR-Product-Information/human/002490/WC500135622.pdf. Accessed January 24, 2013.
55. 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. Gastroenterology 2007; 133: 761-8.
56. 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. Gastroenterology 2010; 139: 1877-86.
57. European Medicines Agency. Points to consider on the evaluation of medicinal products for the treatment of irritable bowel syndrome, 2003. Available at: http://www.ema.europa.eu/docs/en-GB/document-library/Scientific- guideline/2009/09/WC500003187.pdf. Accessed November 15, 2011.
58. Food and Drug Administration. Guidance for industry. Irritable bowel syndrome-clinical evaluation of products for treatment, 2010. Available at: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/ Guidances/UCM205269.pdf. Accessed November 15, 2011.
59. Quigley EMM, Tack J, Choi HS, et al,. Randomised clinical trials: linaclotide phase 3 studies in IBS-C-a prespecified further analysis based on European Medicines Agency-specified endpoints. Aliment Pharmacol Ther 2013; 37: 49-61.
60. Johnston JM, Kurtz CB, Drossman DA, et al,. Pilot study on the effect of linaclotide in patients with chronic constipation. Am J Gastroenterol 2009; 104: 125-32.
61. European Medicines Agency. Committee for Medicinal Products for Human Use (CHMP) assessment report: Constella, 2012. Available at: http://www.ema.europa. eu/docs/en-GB/document-library/EPAR-Public-assessment-report/human/002490/ WC500135624.pdf. Accessed December 23, 2012.
62. Macdougall JE, MacKinnon DP, Lavins BJ, et al,. Mediation analysis supports a direct effect of linaclotide on relief of abdominal pain independent of constipation improvement. Poster presented at the Digestive Disease Week (DDW), San Diego, CA, USA, 19-22 May 2012.
63. Li P, Waldman SA,. Corruption of homeostatic mechanisms in the guanylyl cyclase C signaling pathway underlying colorectal tumorigenesis. Cancer Biol Ther 2010; 10: 211-8.
64. Lin JE, Valentino M, Marszalowicz G, et al,. Bacterial heat-stable enterotoxins: translation of pathogenic peptides into novel targeted diagnostics and therapeutics. Toxins (Basel) 2010; 2: 2028-54.
65. Dibonaventura M, Sun SX, Bolge SC, et al,. Health-related quality of life, work productivity and health care resource use associated with constipation predominant irritable bowel syndrome. Curr Med Res Opin 2011; 27: 2213-22.
66. Fortea J, Prior M,. Irritable bowel syndrome with constipation: a European-focused systematic literature review of disease burden. J Med Econ 2013; 16: 329-41.
67. Goldenberg MM,. Pharmaceutical approval update P T 2012; 37: 620-49.
68. Tack J, Müller-Lissner S, Bytzer P, et al,. A randomised controlled trial assessing the efficacy and safety of repeated tegaserod therapy in women with irritable bowel syndrome with constipation. Gut 2005; 54: 1707-13.
69. Kim YS, Choi SC, Park JM, et al,. The effect of tegaserod on symptoms and quality of life in Korean women with irritable bowel syndrome with constipation. J Neurogastroenterol Motil 2010; 16: 61-70.
70. Walters SJ, Brazier JE,. Comparison of the minimally important difference for two health state utility measures: EQ-5D and SF-6D. Qual Life Res 2005; 14: 1523-32.
71. Pickard AS, Neary MP, Cella D,. Estimation of minimally important differences in EQ-5D utility and VAS scores in cancer. Health Qual Life Outcomes 2007; 5: 70.
72. Lembo A, Carson R, Shiff SJ, et al,. Factors contributing to treatment satisfaction in patients with irritable bowel syndrome with constipation (IBS-C) treated with linaclotide vs placebo. Poster 1401 presented at the Digestive Disease Week (DDW), San Diego, CA, USA, 19-22 May 2012.
73. Blackshaw LA, Brierley SM,. Emerging receptor target in the pharmacotherapy of irritable bowel syndrome with constipation. Exp Rev Gastroenterol Hepatol 2013; 7: 15-9.