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Setmelanotide

Metabolic & Weight Loss

Setmelanotide is an FDA- and EMA-approved MC4R (melanocortin 4 receptor) agonist used for the treatment of genetic obesity syndromes such as POMC, LEPR, or PCSK1 deficiency. It acts centrally to restore appetite regulation and reduce hyperphagia, leading to significant weight loss in responsive populations. It is considered one of the first targeted obesity treatments based on melanocortin biology and is being explored for broader metabolic use.

Reconstitute
null mL BAC + 10mg vial
Daily Range
1–3 mg Subcutaneous (SQ)
Once daily
Standard Dose
2 mg
Cycle
4–8 weeks
then reassess
melanocortin 4 receptorweight managementgenetic obesity

Dosing & Reconstitution Guide

Maximum dose typically 20mg daily. Monitor for skin darkening and other melanocortin-mediated effects. Discontinue if severe adverse effects occur.

Standard / Gradual Approach

standard
PhaseDoseVolume
Week 11mg
Week 22mg
Week 33mg
Week 44mg

Protocol Summary

Subcutaneous (SQ): Once daily · Dose range 1–3 mg with gradual titration
Cycle Length: 4–8 weeks typical; reassess before extending

Frequency & Cycling

SubQ Injection

Administered once daily. Initiate at 1 mg and titrate to 2–3 mg based on response. Long-term or continuous use is permitted with regular monitoring of BMI, leptin response, appetite suppression, and metabolic labs. Typically not cycled unless due to tolerability issues or therapeutic plateau.

🧪 Quick Start

Potential Benefits & Use Cases

Setmelanotide is FDA-approved for specific genetic obesity conditions. Use outside approved indications requires medical supervision.
Studied for targeted appetite suppression via MC4R pathway
Investigated for metabolic regulation in POMC, PCSK1, and LEPR deficiency models
Explored as a selective alternative to alpha-MSH analogs in rodent obesity studies
May enhance energy expenditure in preclinical obesity models
Clinical research interest in rare, monogenic obesity disorders
Clinical data Strong preclinical Limited data

Mechanism of Action

→Melanocortin 4 receptor agonist

Lifestyle & Optimization

timing

Consistent daily injection timing.

diet

Consistent meal timing with balanced macronutrients. Monitor appetite changes carefully.

exercise

Exercise 4–5 times weekly to support metabolic health.

sleep

Sleep 7–9 hours nightly for metabolic regulation.

Peptide Research & Preclinical Studies

Evidence-Based Research Findings

Study TitleType
IMCIVREE, INN-setmelanotideReference
Pharmacologic Treatment of Overweight and Obesity in AdultsReview
Pharmacotherapy of obesity: an update on the available medicationsReview

Side Effects & Safety

Common Side Effects

• Nausea
• Vomiting

Contraindications & Warnings

• Severe allergic reactions

Long-Term Safety Data

• Potential unknown long-term effects

🧮 Dose Calculator

Concentration
50.0
mcg/unit
Draw Volume
10
units (0.100 mL)
For a 500 mcg dose, draw 10 units on a U-100 insulin syringe
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Bioavailability & Absorption

SubQ Injection
Subcutaneous route is the preferred method of administration, allowing direct absorption into the bloodstream.
Oral Administration
Setmelanotide is not orally bioavailable.
Half-Life
12 hours
Degradation
Setmelanotide is metabolized and excreted primarily via the kidneys.
Tissue Specificity
It targets pathways involved in regulating hunger and energy expenditure.
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Peptide Details

Molecular Weight
1020.18
Formula
C49H69N15O7
Sequence
H-Asp-Lys-Val-Met-Asp-Glu-D-Phe-D-Trp-Lys-(gamma-turn)-Gln-His-Edge-NH2
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Legal Status & Regulatory

RegionStatus
FDAApproved
EUApproved
AustraliaNot Approved
CanadaApproved

Storage Instructions

Lyophilized (Powder)
Store solution at 2-8°C. Do not freeze. Maintain in original vial and protect from light. Once opened, solution is stable for 30 days post-opening if refrigerated.
Reconstituted (Mixed)
Refrigerate at 2–8°C after reconstitution. Use within 28 days.