Ghrelin / Relamorelin (RM-131)

Acosta A, Camilleri M, Kolar G, Iturrino J, Szarka L, Boldingh A, Burton D, Ryks M, Rhoten D, Zinsmeister AR, Spence S, Gottesdiener K, Vazquez-Roque ML. A Phase II Placebo-Controlled Trial of Efficacy, Safety, and Pharmacodynamics of Relamorelin in Chronic Constipation. American College of Gastroenterology 2014 Annual Scientific Meeting (ACG 2014), October 21, 2014.

Van der Ploeg L, Laken H, Sharma S, Datta R, HalemH, Dong J, Touvay C, Teillot M, Noonan P, Tartaglia L, Stoner L, Henderson B, Gottesdiener K, Culler M. Preclinical Gastrointestinal Prokinetic Efficacy and Endocrine Effects of the Ghrelin Mimetic RM-131. Life Sci. 2014 Jul 25, 109(1):20-9. doi: 10.1016/j.lfs.2014.06.003.

Acosta A, Kolar G, Iturrino J, Szarka L, Boldingh A, Burton D, Ryks M, Rhoten D, Zinsmeister AR, Camilleri M. A Phase II, Single-Center, Randomized, Double-Blind, Placebo-Controlled, Multiple-Dose, Parallel-Group Study to Evaluate the Pharmacodynamics of RM‑131 in Patients with Chronic Constipation. Digestive Disease Week, May 3, 2014.

Sha L, Farrugia1 G, Van der Ploeg LHT, Szurszewski JH. Effect of RM-131 on Circular Smooth Muscle Cells in Human and Mouse Colon and on Colonic Intraluminal Pressure in Conscious Mice. Digestive Disease Week, May 3, 2014.

Kaplan LM, McCallum R, Koch K, Sederman R, Henderson B. High Prevalence and Underdiagnosis of Gastroparesis Symptoms Among Patients with Type 1 and Type 2 Diabetes Mellitus. Digestive Disease Week, May 20, 2013.

Shin A, Camilleri M, Busciglio I, Burton D, Smith SA, Vella A, Ryks M, Rhoten D, Zinsmeister AR. Phase 1, Randomized, Placebo-Controlled, Single-Dose, Two-Period, Crossover Study of RM-131 on Pharmacodynamics and Symptoms in Type 1 Diabetics with Documented Delayed Gastric Emptying. Digestive Disease Week, May 20, 2013.

Shin A, Camilleri M, Busciglio I, Burton D, Smith SA, Vella A, Ryks M, Rhoten D, Zinsmeister AR. The Ghrelin Agonist RM-131 Accelerates Gastric Emptying of Solids and Reduces Symptoms in Patients with Type 1 Diabetes Mellitus. Clin Gastroenterol Hepatol. 2013 Apr 29 [Epub ahead of print]. PubMed PMID: 23639598. doi: 10.1016/j.cgh.2013.04.019.

Shin A, Camilleri M, Busciglio I, Burton D, Stoner E, Noonan P, Gottesdiener K, Smith SA, Vella A, Zinsmeister AR. Randomized Controlled Phase Ib Study of Ghrelin Agonist, RM-131, in Type 2 Diabetic Women With Delayed Gastric Emptying: Pharmacokinetics and pharmacodynamics. Diabetes Care. 2012 Sep 6 [Epub ahead of print]. PubMed PMID: 22961573. doi: 10.2337/dc12-1128.

Datta R, Soulard C, Teillot M, Touvay C, Halem H, Dong J, Culler M. RM-131: A Potent Gastroprokinetic Agent. Digestive Disease Week, May 7, 2011.

MC4 / Setmelanotide (RM-493)

Chen KY, Muniyappa R, Abel BS, Mullins KP, Staker P, Brychta RJ, Zhao X, Ring M, Psota TL, Cone RD, Panaro BL, Gottesdiener KM, Van der Ploeg LHT, Reitman ML, Skarulis MC. RM-493, a Melanocortin-4 Receptor (MC4R) Agonist, Increases Resting Energy Expenditure in Obese Individuals. J. Clin. Endocrinol. Metab. 2015 Apr, 100(4):1639-45. doi: 10.1210/jc.2014-4024.

Clemmensen C, Finan B, Fischer K, Tom RZ, Legutko B, Sehrer L, Heine D, Grassl N, Meyer CW, Henderson B, Hofmann SM, Tschöp MH, Van der Ploeg L, Müller TD. Dual Melanocortin-4 Receptor and GLP-1 Receptor Agonism Amplifies Metabolic Benefits in Diet-Induced Obese Mice. EMBO Mol Med. 2015 Feb 4, doi: 10.15252/emmm.201404508.

Muniyappa R, Chen K, Brychta R, Abel B, Mullins K, Staker P, Van der Ploeg L, Connors H, Gottesdiener K, Reitman ML, Skarulis MC. A Randomized, Double-Blind, Placebo-Controlled, Crossover Study to Evaluate the Effect of a Melanocortin Receptor 4 (MC4R) Agonist, RM-493, on Resting Energy Expenditure (REE) in Obese Subjects. International Society of Endocrinology and the Endocrine Society (ICE/ENDO 2014), June 22, 2014.

Schaaf CP, Gonzalez-Garay ML, Xia F, Potocki L, Gripp KW, Zhang B, Peters BA, McElwain MA, Drmanac R, Beaudet AL, Caskey CT, Yang Y. Truncating Mutations of MAGEL2 Cause Prader-Willi Phenotypes and Autism. Nat.Genet. (November 2013) 45, 1405–1408.

Mercer RE, Michaelson SD, Chee MJS, Atallah TA, Wevrick1 R, Colmers WF. Magel2 is Required for Leptin-Mediated Depolarization of POMC Neurons in the Hypothalamic Arcuate Nucleus in Mice. PLOS Genet.. 2013;9(1):e1003207. doi: 10.1371/journal.pgen.1003207. Epub 2013 Jan 17.

Kievit P, Halem H, Marks DL, Dong JZ, Glavas MM, Sinnayah P, Pranger L, Cowley MA, Grove KL, Culler MD. Chronic Treatment With a Melanocortin 4 Receptor Agonist Causes Weight Loss, Reduces Insulin Resistance, and Improves Cardiovascular Function in Diet-Induced Obese Rhesus Macaques. Diabetes. 2012 Oct 9 [Epub ahead of print]. doi:10.2337/db12-0598.

Roubert P, Dubern B, Plas P, Lubrano-Berthelier C, Alihi R, Auger F, Deoliveira D, Dong J, Basdevant A, Thurieau C, Cle´ment K. Novel Pharmacological MC4R Agonists can Efficiently Activate Mutated MC4R from Obese Patient with Impaired Endogenous Agonist Response. J Endocrinol. (2010) 207, 177-183.