Setmelanotide
Setmelanotide (brand name Imcivree) is a synthetic cyclic octapeptide and an agonist at the melanocortin-4 receptor (MC4R). It was developed and approved as a prescription medicine for chronic weight management in rare genetic forms of obesity within the MC4R signalling pathway (including POMC, PCSK1 and LEPR deficiency as well as Bardet-Biedl syndrome). The following information is provided for informational and educational purposes only.
Mechanism of action
Setmelanotide is an agonist at the melanocortin-4 receptor (MC4R), a central receptor of the hypothalamic melanocortin pathway involved in the control of energy balance, satiety and body weight. In certain genetic defects (e.g. in POMC, PCSK1 or LEPR), the natural activation of MC4R is reduced. Setmelanotide activates MC4R directly, thereby bypassing the upstream defect. This description is mechanistic and neutral and does not constitute a recommendation for use.
Evidence at a glance
What the studies show
Where studies disagree
How serious is the pigment and nevus risk of melanocortin activation?
Pharmacokinetics
Theoretical concentration curve at a half-life of 11 h. Pure pharmacokinetic model — not a dosing recommendation.
Open in PK tool →Routes of administration in the literature
Safer use & risks
Known adverse events from studies
Interactions & combinations
Anecdotal observations
What online communities discuss
Legal status by country
Reconstitution calculator
Peptides ship as a dry powder. Once dissolved in a liquid (reconstitution), this calculator answers a single question: how much substance is in one millilitre of solution afterwards?
- 1Enter the vial's substance amount (printed on the label).
- 2Enter how much solvent you add.
- 3Result = concentration in mg per mL.
Study register
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
Efficacy and safety of setmelanotide, a melanocortin-4 receptor agonist, in patients with Bardet-Biedl syndrome and Alström syndrome: a multicentre, randomised, double-blind, placebo-controlled, phase 3 trial with an open-label period
Proopiomelanocortin Deficiency Treated with a Melanocortin-4 Receptor Agonist
Sources & method
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