RM-131, a Novel Ghrelin Analog, Demonstrates Potent Prokinetic Activity in Phase 1 Single- and Multiple-dose Studies in Healthy Volunteers

Kaplan, Lester J.; White, Jeffery; Spence, Sharon; Kennedy, Sally; Stoner, Elizabeth; Noonan, Patrick K.; Laken, Haley; Gottesdiener, Keith

doi:10.14309/00000434-201210001-01739

Cited by 3 publications

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“…Relamorelin's prokinetic effects also have been shown by acceleration of gastric emptying in earlier studies in healthy subjects and in diabetic gastroparesis. [8][9][10] A recent trial of relamorelin in patients with chronic idiopathic constipation showed not only acceleration of gastric emptying, but also of colonic transit. 17 In the VS subgroup, relamorelin was effective in improving other diabetic gastroparesis symptoms (nausea, bloating, early satiety, and abdominal pain), whereas in the mITT population only small numeric, but not statistically significant, differences from placebo were seen with relamorelin 10 mg twice daily.…”

Section: July 2016mentioning

confidence: 99%

“…The clinical activity of relamorelin, as evidenced by acceleration of gastric emptying, was shown in phase 1 studies in healthy subjects and in diabetic patients (type 1 and type 2). [8][9][10][11] Toxicologic studies with relamorelin provide very large (>750-fold) safety margins compared with clinical exposures. Given these promising results, we conducted a clinical trial to assess the safety and effectiveness of relamorelin on vomiting and other symptoms of gastroparesis, as well as gastric emptying, in patients with diabetic gastroparesis.…”

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confidence: 99%

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Relamorelin Reduces Vomiting Frequency and Severity and Accelerates Gastric Emptying in Adults With Diabetic Gastroparesis

et al. 2016

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In a clinical trial of patients with diabetic gastroparesis, relamorelin (10 μg twice daily) significantly accelerated gastric emptying and significantly reduced vomiting, compared with placebo. Among patients with baseline vomiting, relamorelin had prokinetic effects and significantly reduced vomiting and also improved other symptoms of diabetic gastroparesis compared with placebo. ClincialTrials.gov number: NCT01571297.

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Section: July 2016mentioning

confidence: 99%

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confidence: 99%

Relamorelin Reduces Vomiting Frequency and Severity and Accelerates Gastric Emptying in Adults With Diabetic Gastroparesis

et al. 2016

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“…Gastric emptying results on days 1 and 7 were similar, with a comparable change in gastric emptying following daily doses of 10, 20, 80, and 300 lg relamorelin. 24…”

Section: Pharmacodynamic Studies In Humansmentioning

confidence: 99%

Emerging treatments in Neurogastroenterology: relamorelin: a novel gastrocolokinetic synthetic ghrelin agonist

Camilleri

Acosta

2014

Neurogastroenterology Motil

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Synthetic ghrelin agonists, predominantly small molecules, are being developed as prokinetic agents that may prove useful in the treatment of gastrointestinal motility disorders. Relamorelin (RM-131) is a pentapeptide synthetic ghrelin analog that activates the growth hormone secretagogue (GHS)-1a (also called the ghrelin) receptor with approximately 6-fold greater potency than natural ghrelin. The ability of relamorelin to stimulate growth hormone (GH) release is comparable to that of native ghrelin. Relamorelin has enhanced efficacy and plasma stability compared to native ghrelin. In this review, we discuss the pharmacokinetics, pharmacodynamics and potential indications for relamorelin. Relamorelin is administered subcutaneously, dosed daily or twice daily. Relamorelin is being studied for the treatment of patients with gastrointestinal motility disorders. Phase IIA pharmacodynamic studies have demonstrated acceleration of gastric emptying in patients with type 1 diabetes mellitus (T1DM) and type 2 DM (T2DM) and upper gastrointestinal symptoms. In a phase IIA study in patients with diabetic gastroparesis, relamorelin accelerated gastric emptying and significantly improved vomiting frequency compared to placebo and improved other symptoms of gastroparesis in a pre-specified subgroup of patients with vomiting at baseline. In patients with chronic idiopathic constipation with defined transit profile at baseline, relamorelin relieved constipation and accelerated colonic transit compared to placebo. These characteristics suggest that this new ghrelin analog shows great promise to relieve patients with upper or lower gastrointestinal motility disorders.

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Relamorelin Relieves Constipation and Accelerates Colonic Transit in a Phase 2, Placebo-Controlled, Randomized Trial

Acosta

Camilleri

Kolar

et al. 2015

Clinical Gastroenterology and Hepatology

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RM-131, a Novel Ghrelin Analog, Demonstrates Potent Prokinetic Activity in Phase 1 Single- and Multiple-dose Studies in Healthy Volunteers

Cited by 3 publications

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Relamorelin Reduces Vomiting Frequency and Severity and Accelerates Gastric Emptying in Adults With Diabetic Gastroparesis

Relamorelin Reduces Vomiting Frequency and Severity and Accelerates Gastric Emptying in Adults With Diabetic Gastroparesis

Emerging treatments in Neurogastroenterology: relamorelin: a novel gastrocolokinetic synthetic ghrelin agonist

Relamorelin Relieves Constipation and Accelerates Colonic Transit in a Phase 2, Placebo-Controlled, Randomized Trial

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