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.
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How serious is the pigment and nevus risk of melanocortin activation?
Farmacokinetiek
Theoretische concentratiecurve bij een halfwaardetijd van 11 h. Puur farmacokinetisch model — geen doseringsaanbeveling.
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Reconstitutie-calculator
Peptiden komen als droog poeder. Eenmaal opgelost in een vloeistof (reconstitutie) beantwoordt deze calculator één enkele vraag: hoeveel stof zit er daarna in één milliliter oplossing?
- 1Voer de hoeveelheid stof van de flacon in (staat op het etiket).
- 2Voer in hoeveel oplosmiddel je toevoegt.
- 3Resultaat = concentratie in mg per mL.
Studieregister
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
Bronnen & methode
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