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Synonyms: BIM-22493 | Imcivree® | IRC-022493 | RM-493
setmelanotide is an approved drug (FDA (2020), EMA (2021))
Compound class: Peptide or derivative
Comment: Setmelanotide is an agonist of melanocortin receptors, with approximately 20-fold selectivity for the melanocortin 4 receptor subtype . Chemically it is an eight-amino-acid cyclic peptide, that is able to cross the blood-brain barrier when administered peripherally. Setmelanotide offers anti-obesity potential.
The INN record documents the sequence as N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-cysteinamide, cyclic (2-8)-disulfide.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Chen KY, Muniyappa R, Abel BS, Mullins KP, Staker P, Brychta RJ, Zhao X, Ring M, Psota TL, Cone RD et al.. (2015)
RM-493, a melanocortin-4 receptor (MC4R) agonist, increases resting energy expenditure in obese individuals.
J Clin Endocrinol Metab, 100 (4): 1639-45. [PMID:25675384]
2. Clément K, van den Akker E, Argente J, Bahm A, Chung WK, Connors H, De Waele K, Farooqi IS, Gonneau-Lejeune J, Gordon G et al.. (2020)
Efficacy and safety of setmelanotide, an MC4R agonist, in individuals with severe obesity due to LEPR or POMC deficiency: single-arm, open-label, multicentre, phase 3 trials.
Lancet Diabetes Endocrinol, 8 (12): 960-970. [PMID:33137293]
3. Fani L, Bak S, Delhanty P, van Rossum EF, van den Akker EL. (2014)
The melanocortin-4 receptor as target for obesity treatment: a systematic review of emerging pharmacological therapeutic options.
Int J Obes (Lond.), 38 (2): 163-9. [PMID:23774329]
4. Farooqi IS, O'Rahilly S. (2008)
Mutations in ligands and receptors of the leptin-melanocortin pathway that lead to obesity.
Nat Clin Pract Endocrinol Metab, 4 (10): 569-77. [PMID:18779842]
5. Kumar KG, Sutton GM, Dong JZ, Roubert P, Plas P, Halem HA, Culler MD, Yang H, Dixit VD, Butler AA. (2009)
Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice.
Peptides, 30 (10): 1892-900. [PMID:19646498]
6. Kühnen P, Clément K, Wiegand S, Blankenstein O, Gottesdiener K, Martini LL, Mai K, Blume-Peytavi U, Grüters A, Krude H. (2016)
Proopiomelanocortin Deficiency Treated with a Melanocortin-4 Receptor Agonist.
N Engl J Med, 375 (3): 240-6. [PMID:27468060]