For adults with Chronic Idiopathic Constipation (CIC)

Activate 5-HT4 receptors and stimulate colonic peristalsis.1,4*

*Motegrity is a selective serotonin type 4 (5-HT4) receptor agonist.1

Motegrity Mechanism of Action

How does Motegrity (prucalopride) work?

Motegrity provides a different class of CIC treatment that works by stimulating colonic peristalsis to increase bowel motility.1-4

Here’s how:

1 Absorb

One 2 mg oral dose of Motegrity in healthy participants reached peak plasma concentrations within 2-3 hours.1

Learn about median time-to first bowel movement

Molecule of prucalopride

3D representation of
prucalopride

2 Activate

In the colon, Motegrity selectively binds and activates 5-HT4 receptors1,4,5

Motegrity showed no cross-reactivity with 5-HT2A, 5-HT2B, 5-HT3, motilin, or CCK-A receptors in in vitro studies at concentrations exceeding 5-HT4 receptor affinity by 150-fold or greater.1,6

3 Release

Colonic 5-HT4 receptor activation facilitates the release of acetylcholine as seen in in vitro studies1,4,5

4 Move

Colonic peristalsis is stimulated, increasing bowel motility1,4,5

Treatment mechanisms in the management of chronic idiopathic constipation

Want to learn more about
how Motegrity works?

Discover our prokinetic approach by watching these 3 short videos

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Motegrity—A Motility Based Mechanism of Action

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Motegrity—A 5-HT4 Receptor Agonist Prokinetic for Adults with CIC

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Colonic Motility and Accelerated Transit Time

SELECT IMPORTANT SAFETY INFORMATION

Adverse Reactions

Most common adverse reactions (≥2%) are headache, abdominal pain, nausea, diarrhea, abdominal distension, dizziness, vomiting, flatulence, and fatigue.

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Pharmacodynamics of Motegrity

Motegrity is a GI prokinetic that stimulates colonic peristalsis (i.e. HAPCs), which increases bowel motility

In a pharmacodynamic CIC study:

More frequent HAPCs

A single 2 mg dose of Motegrity increased HAPC frequency during the first 12 hours compared to osmotic laxatives.1

Increased HAPC amplitude

Motegrity 4 mg* once daily for 7 days increased HAPC amplitude in healthy participants compared to placebo without affecting colonic phasic activity.1

 

*Twice the max recommended dose of 2 mg.

Accelerate colonic transit time (CTT) in adults with CIC1,11

The effect of once daily Motegrity 2 mg and placebo on mean CTT was studied in an integrated analysis of 3 randomized, placebo-controlled, dose-finding trials in adults (n=280) with CIC. Mean CTT was reduced by 12 hours from a baseline of 65 hours for the Motegrity 2 mg group, compared to an increase of 0.5 hours from a baseline of 66 hours in the placebo group.1,11

†P<0.001 vs. baseline.

A closer look at the colonic 5-HT pathway

Colon icon
  • 95% of endogenous 5-HT is found in the digestive tract12
  • 5-HT is released by enterochromaffin cells in response to distension and other stimuli13
  • There are 5 families of 5-HT receptors in the gut that mediate a number of basic functions, including colonic motility4,14
  • Colonic peristalsis is promoted when 5-HT4 receptor activation stimulates acetylcholine release4,5
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Formulary Coverage

Wondering which plans in your area cover Motegrity? See our patient access coverage tool to find out more.

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IMPORTANT SAFETY INFORMATION

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Please expand for Indication and Important Safety Information.

Contraindications

  • Hypersensitivity to Motegrity. Reactions including dyspnea, rash, pruritus, urticaria, and facial edema have been observed
  • Intestinal perforation or obstruction due to structural or functional disorder of the gut wall, obstructive ileus, severe inflammatory conditions of the intestinal tract such as Crohn's disease, ulcerative colitis, and toxic megacolon/megarectum

Warnings and Precautions

Suicidal Ideation and Behavior: In clinical trials, suicides, suicide attempts and suicidal ideation have been reported. Postmarketing cases of suicidal ideation and behavior as well as self-injurious ideation and new onset or worsening of depression have been reported within the first few weeks of starting Motegrity. A causal association between treatment with Motegrity and an increased risk of suicidal ideation and behavior has not been established. Monitor patients for new onset or worsening of depression and emergence of suicidal thoughts and behavior. Instruct patients to discontinue Motegrity immediately and contact their healthcare provider if they experience any of these symptoms.

Adverse Reactions

Most common adverse reactions (≥2%) are headache, abdominal pain, nausea, diarrhea, abdominal distension, dizziness, vomiting, flatulence, and fatigue.

Use in Specific Populations

  • Lactation: Motegrity is present in breast milk. Consider risks and benefits of breastfeeding
  • Pediatric: Safety and effectiveness in pediatric patients have not been established
  • Renal Impairment: A decreased dosage is recommended in patients with severe renal impairment. Avoid Motegrity in patients with end-stage renal disease requiring dialysis

INDICATION

Motegrity® (prucalopride) is a serotonin-4 (5-HT4) receptor agonist indicated for the treatment of chronic idiopathic constipation (CIC) in adults.

Please click here for full Prescribing Information.

References:

1. Motegrity (prucalopride) Prescribing Information. Lexington, MA: Takeda Pharmaceuticals America, Inc. 2. Camilleri M, Ford AC, Mawe GM, et al. Nat Rev Dis Primers. 2017;3:17095. 3. Tack J, Camilleri M, Chang L, et al. Aliment Pharmacol Ther. 2012;35(7):745-767. 4. Mawe GM, Hoffman JM. Nat Rev Gastroenterol Hepatol. 2013;10(8):473-486. 5. Gershon MD, Tack J. Gastroenterology. 2007;132(1):397-414. 6. Briejer MR, Bosmans JP, Van Daele P, et al. Eur J Pharmacol. 2001;423(1):71-83. 7. Lacy B, Hussain Z, Mearin F. Neurogastroenterol Motil. 2014;26(6):749-763. 8. Izzy M, Malieckal A, Little E, et al. World J Gastrointest Pharmacol Ther. 2016;7(2):334-342. 9. Lacy BE, Levenick JM, Crowell M. Therap Adv Gastroenterol. 2012;5(4):233-247. 10. Menees S, Saad R, Chey WD. Nat Rev Gastroenterol Hepatol. 2012;9(11):661-674. 11. Emmanuel A, Cools M, Vandeplassche L, Kerstens R. Am J Gasteroenterol. 2014;109(6):887-894. 12. Kim DY, Camilleri M. Am J Gastroenterol. 2000;95(10):2698-2709. 13. Kim HS. J Smooth Muscle Res. 2009;45(1):25-29. 14. Kendig DM, Grider JR. Neurogastroenterol Motil. 2015;27(7):899-905.

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