Linaclotide-a novel secretagogue in the treatment of irritable bowel syndrome with constipation and chronic idiopathic constipation

Mini-Reviews in Medicinal Chemistry

Volumn 13, Issue 11, 2013, Pages 1685-1690

  Sharma, Shivani ^a   Sharma, Tina ^a   Dhingra, Richa ^a   Tomar, Prince ^a   Singh, Sukhminder ^a   Malhotra, Manav ^a   Bhardwaj, T R ^a  

^a ISF COLLEGE OF PHARMACY   (India)

Author keywords

cGMP; CIC; Guanylate cyclase C; Homeostasis; IBS C; Linaclotide

Indexed keywords

17 METHYLNALTREXONE; ALVIMOPAN; CYCLIC GMP; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; GUANYLATE CYCLASE; GUANYLATE CYCLASE C; LINACLOTIDE; LUBIPROSTONE; NARONAPRIDE; PLACEBO; PRUCALOPRIDE; UNCLASSIFIED DRUG;

ABDOMINAL DISTENSION; ABDOMINAL PAIN; AREA UNDER THE CURVE; ARTICLE; CHRONIC IDIOPATHIC CONSTIPATION; CONSTIPATION; DIARRHEA; DRUG EFFICACY; DRUG INDUCED DISEASE; DRUG SAFETY; DRUG STABILITY; DRUG SUBSTITUTION; DRUG WITHDRAWAL; FLATULENCE; HEADACHE; HUMAN; INCIDENCE; IRRITABLE COLON; LIMIT OF QUANTITATION; MULTICENTER STUDY (TOPIC); NAUSEA; NONHUMAN; OPIOID INDUCED CONSTIPATION; PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); QUALITY OF LIFE; RANDOMIZED CONTROLLED TRIAL (TOPIC); SCORING SYSTEM; SINUSITIS; UPPER RESPIRATORY TRACT INFECTION; VIRAL GASTROENTERITIS;

CHRONIC DISEASE; CLINICAL TRIALS AS TOPIC; CONSTIPATION; CYCLIC GMP; CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR; HALF-LIFE; HUMANS; IRRITABLE BOWEL SYNDROME; PEPTIDES; RECEPTORS, GUANYLATE CYCLASE-COUPLED;

EID: 84888036152     PISSN: 13895575     EISSN: 18755607     Source Type: Journal    
DOI: 10.2174/1389557511313110011     Document Type: Article

References (44)

1. Drossman, DA. The functional gastrointestinal disorders and the Rome III process. Gastro, 2006, 130, 1377-1390.
2. Sandler, R. S.; Drossman, DA. Bowel habits in young adults not seeking health care. Dig Dis Sci, 1987, 32, 841-845.
3. Thompson, WG.; Irvine, EJ.; Pare, P.; Ferrazzi, S.; Rance, L. Functional gastrointestinal disorders in Canada: first populationbased survey using Rome II criteria with suggestions for improving the questionnaire. Dig Dis Sci, 2002, 47, 225-235.
4. Ringel, Y.; Sperber, AD.; Drossman, D. A. Irritable bowel syndrome. Annu Rev Med, 2001, 52, 319-338.
5. McCallum, IJ.; Ong, S.; Mercer-Jones, M. Chronic constipation in adults. Brit Med J, 2009, 338, b831.
6. Saito, YA.; Schoenfeld, P.; Locke, GR. The epidemiology of irritable bowel syndrome in North America: a systematic review. Am J Gastroenterol, 2002, 97, 1910-1915.
7. Johanson, JF.; Kralstein, J. Chronic constipation: a survey of the patient perspective. Ali Pharm Ther, 2007, 25, 599-608.
8. Mayer, EA.; Gebhart, GF. Basic and clinical aspects of visceral hyperalgesia. Gastro, 1994, 107, 271-293.
9. Camilleri, M.; Andresen, V. Current and novel therapeutic options for irritable bowel syndrome management. Dig. Liver Dis, 2009, 41, 854-862.
10. Camilleri, M. Evolving concepts of the pathogenesis of irritable bowel syndrome: to treat the brain or the gut? J Pediatr Gastroenterol Nutr, 2009, 48, S46-S54.
11. Drossman, DA.; Chey, WD.; Johanson, JF.; Fass, R.; Scott, C.; Panas, R.; Ueno, R. 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.
12. Lang, L. The Food and Drug Administration approves lubiprostone for irritable bowel syndrome with constipation. Gastro, 2008, 135, 7.
13. McKeage, K.; Plosker, GL.; Siddiqui, MA. Lubiprostone. Drugs, 2006, 66, 873-879.
14. Lacy, BE.; Levy, LC. Lubiprostone: a chloride channel activator. J Clin Gastro, 2007, 41, 345-51.
15. Johanson, JF.; MortonD Geenen, J.; Ueno, R. 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 Gastro, 2008, 103, 70-77.
16. Ironwood and Forest Announce U. S. Availability of Linzess. 17 Dec 2012. (http://www. cnbc. com/id/100320182).
17. Andresen, V.; Camilleri, M.; Busciglio, IA.; Burton, D.; McKinzie, S.; Foxx-Orenstein, A.; Kurtz, CB.; Sharma, V.; Johnston, JM.; Currie, MG.; Zinsmeister, AR. Effect of 5 days linaclotide on transit and bowel function in females with constipation-predominant irritable bowel syndrome. Gastro, 2007, 133, 761-768.
18. Lembo, A.; Schneier, H.; Lavins, BJ.; Shiff, SJ.; MacDougall, JE.; Jia, XD.; Fitch, DA.; O'Dea, C.; Baird, M. 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. Gastro, 2010, 139, S53-S54.
19. Lembo, AJ.; Kurtz, CB.; Macdougall, JE.; Lavins, BJ.; Currie, MG.; Fitch, DA.; Jeglinski, BI.; Johnston, JM. Efficacy of linaclotide for patients with chronic constipation. Gastro, 2010, 138, 886-895.
20. Rogue, MV.; Camilleri, M. Linaclotide, a synthetic guanylate cyclase C agonist, for the treatment of functional gastrointestinal disorders associated with constipation. Expert Rev Gastro Hepatol, 2011, 5, 301-310.
21. Johnston, JM.; Kurtz, CB.; Drossman, DA.; Lembo, AJ.; Jeglinsli, BI.; MacDougall, JE.; Antonelli, SM.; Currie, MG. Pilot study on the effect of linaclotide in patients with chronic constipation. Am J Gastroenterol, 2009, 104, 125-132.
22. Schulz, S.; Green, CK.; Yuen, PST.; Garbers, DL. Guanylyl cyclase is a heat-stable enterotoxins receptor. Cell, 1990, 63, 941-948.
23. Giannella, R. A.; Mann, E. A. E. coli heat-stable enterotoxin and guanylyl cyclase C: new functions and unsuspected actions. Trans. Am. Clin. Climatol. Assoc, 2003, 114, 67-85.
24. Bharucha, AE.; Waldmon, SA. Taking a lesson from microbial diarrheagenesis in the management of chronic constipation. Gastro, 2010, 138, 813-817.
25. - secretion by uroguanylin. The American journal of physiology, 1998, 274, G633-G644.
26. Field, M.; Graf, Jr.; L. H.; Laird, W. J.; Smith, P. L. Heat-stable enterotoxin of Escherichia coli: in vitro effects on guanylate cyclase activity, cyclic GMP concentration, and ion transport in small intestine. Proc. Natl. Acad. Sci. U. S. A, 1978, 75, 2800-2804.
27. Andresen, V.; Camilleri, M. Linaclotide acetate. Guanylate cyclase C receptor agonist treatment of irritable bowel syndrome and treatment of constipation. Drugs of the Future, 2008, 33, 570-576.
28. Field, M.; Rao, M. C.; Chang, E. B. Intestinal electrolyte transport and diarrheal disease. N Engl J. Med, 1989, 321, 879-883.
29. 2+-dependent HCO3 secretion. American Journal of Physiology, 1997, 505, 411-423.
30. Sato, T.; Ozaki, H.; Hata, Y.; Kitagawa, Y.; Katsube, Y.; Shimonishi, Y. Structural characteristics for biological activity of heat-stable enterotoxin produced by enterotoxigenic Escherichia coli: X-ray crystallography of weakly toxic and nontoxic analogs. Biochemistry, 1994, 33, 8641-8650.
31. Vaandrager, A. B.; Smolenski, A.; Tilly, BC.; Houtsmuller, AB.; Ehlert, EM.; Bot, AG.; Edixhoven, M.; Boomaars, WE.; Lohmann, SM.; de Jonge, HR. Membrane targeting of cGMP-dependent protein kinase is required for cystic fibrosis transmembrane conductance regulator Cl channel activation. Proc. Natl. Acad. Sci. U. S. A, 1998, 95, 1466-1471.
32. Bueno, L.; Beaufraud, C.; Mahajan-Miklos, C.; Bryant, A.; Eutamene, H. Antinociceptive actions of MD-1100 (linaclotide), a novel therapeutic agent for C-IBS, in animal models of visceral pain. Am J Gastroentrerol, 2004, 99, A283.
33. Skelton, N. J.; Garcia, K. C.; Goeddel, D. V.; Quan, C.; Burnier, J. P. Determination of the solution structure of the peptide hormone guanylin: observation of a novel form of topological stereoisomerism. Biochemistry, 1994, 33, 13581-13592.
34. Busby, RW.; Bryant, AP.; Bartolini, WP.; Cordero, EA.; Hannig, G.; Kessler, MM.; Mahajan-Miklos, S.; Pierce, CM.; Solinga, RM.; Sun, LJ.; Tobin, JV.; Kurtz, CB.; Currie, MG. Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit. Eur J Pharm, 2010, 649, 328-335.
35. Lembo, AJ.; Johnston, JM.; MacDougall, JE.; Lavins, BJ.; Fitch, DA.; Jeglinski, BI.; Kurtz, CB.; Drossman, DA.; Currie, CJ. Linaclotide significantly improved bowel habits and relieved abdominal symptoms in adults with chronic constipation: data from a large 4-week, randomized, double-blind, placebo-controlled study. Gastro, 2008, 135, 295.
36. Longstreth, GF.; Thompson, WG.; Chey, WD.; Longstreth, GF.; Houghton, LA.; Mearin, F.; Spiller, RC. Functional bowel disorders. Gastroenterology, 2006, 130, 1480-1491.
37. Tack, J. Current and Future therapies for chronic constipation. Best Prac Res Clin Gastro, 2011, 25, 151-158.
38. Lembo, AJ.; Schneier, H.; Shiff, S.; Kurtz, CB.; MacDougall, JE.; Jia, XD.; Shao, JZ.; Lavins, BJ.; Currie, MG.; Fitch, DA.; Jeglinski, BI.; Eng, P.; Fox, SM.; Johnston, JM. Two randomized trials of linaclotide for chronic constipation. N Engl J Med, 2011, 365, 527-536.
39. Johnston, JM.; Kurtz, CB.; MacDougall, JE.; Lavins BJ.; Currie, MG.; Fitch, DA.; O'Dea, C.; Baird, M.; Lembo, AJ. Linaclotide improves abdominal pain and bowel habits in a Phase IIb study of patients with irritable bowel syndrome. Gastro, 2010, 139, 1877-1886.
40. Rao, S.; Lembo, AJ.; Shiff, SJ.; Lavins BJ.; Currie, MG.; Jia, XD.; Shi, K.; Shao, JZ.; Eng, P.; Fox, SM.; Schneier, H.; Johnston, JM.; Kurtz, CB.; MacDougall, JE. Efficacy and safety of once daily linaclotide in patients with irritable bowel syndrome with constipation: a 12-week, randomized, double-blind, placebocontrolled Phase 3 trial followed by a 4-week randomized withdrawal period. Gastro, 2011, 140, S-138.
41. Chey, WD.; Lembo, A.; MacDougall, JE.; Lavins, BJ.; Schneier, H.; Johnston, JM. Efficacy and safety of once-daily linaclotide administered orally for 26 weeks in patients with IBS-C: results from a randomized, double-blind, placebo-controlled Phase 3 trials. Gastro, 2011, 40, S-135.
42. Carson, R.; Tourkodimitris, S.; Lewis, BE.; Johnston, JM. Effect of linaclotide on quality of life in adults with irritable bowel syndrome with constipation: pooled results from two randomized, doubleblind, placebo-controlled Phase 3 trials. Gastro, 2011, 140-151.
43. Lee, N.; Wald, A. The pharmacokinetics, pharmacodynamics, clinical efficacy, safety and tolerability of linaclotide. Expert Opin Drug Metab Toxicol, 2011, 7, 651-659.
44. Arshad, N.; Visweswariah, S. S. The multiple and enigmatic roles of guanylyl cyclase in intestinal homeostasis. FEBS Letters, 2012, 586, 2835-2840.