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Weight Management Protocol

SetmelanotideComplete Dosing & Administration Guide

Targeted MC4R agonist for rare genetic obesity caused by melanocortin pathway defects

Dose Range

0.5 mg-3 mgmg

Frequency

Once daily

Route

subcutaneous injection

Cycle Length

Ongoing/indefinite

Dosing

How much
do I take?

Timing

Best time to take

Administer Setmelanotide at the same time each day (or on the same day each week for weekly injections). Many users prefer morning or evening administration. Pick a time you'll remember consistently.

With food?

Setmelanotide injections can be given regardless of meal timing. However, if GI effects occur, administering on an empty stomach or with a light meal may help reduce discomfort.

If stacking

Setmelanotide should be used as directed by your healthcare provider. If combining with other medications or supplements, discuss potential interactions with your provider. Avoid combining with compounds that have overlapping mechanisms unless specifically guided by a medical professional.

Adjusting Your Dose

Increase if

  • +You've tolerated the current dose for the recommended period without significant side effects
  • +Therapeutic goals haven't been met at the current dose level
  • +Your healthcare provider recommends dose escalation based on your response
  • +Lab work or clinical assessments support a higher dose

Decrease if

  • -Side effects are bothersome or impacting daily life despite management strategies
  • -You experience any signs of an adverse reaction
  • -Lab results indicate the need for dose reduction
  • -Your healthcare provider recommends a lower dose based on your response

Signs of right dose

  • Therapeutic goals being met with minimal side effects
  • Stable and consistent response to treatment
  • Lab values or clinical markers trending in the right direction
  • Good tolerance with manageable or absent side effects

Dosing Calculator

Calculate Your Exact Dose

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Step 1: Peptide Weight

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Select Weight

mg

Look for a number followed by 'mg' on the vial label (e.g., 5mg, 10mg)

Administration

How do I
use it?

Reconstitution

What you need

  • Setmelanotide vial (lyophilized powder or solution)
  • Bacteriostatic water or sterile sodium chloride for reconstitution
  • Alcohol swabs for cleaning vial tops and injection sites
  • Appropriately sized syringes with fine-gauge needles (27-30 gauge)
  • Sharps disposal container

Example

Add the recommended volume of bacteriostatic water to the Setmelanotide vial. Gently swirl (do not shake) until the powder is fully dissolved. The resulting solution should be clear. Calculate your individual dose based on the concentration and your prescribed amount.

Your dose of Setmelanotide is determined by your healthcare provider. Using an insulin syringe marked in units, draw up the exact amount prescribed. For example, if the reconstituted concentration is 1mg/mL and your dose is 0.5mg, draw up 0.5mL (50 units on an insulin syringe). Always double-check calculations before injection.

Injection

Route

Subcutaneous injection (into the fatty tissue just under the skin)—allows for consistent absorption and can be self-administered at home after proper training

Best sites

  • Abdomen (stomach area)—at least 2 inches from the belly button, most popular choice for self-injection
  • Front of thighs—middle to upper portion of the outer leg
  • Back of upper arm—outer area (may need assistance from another person)

Technique

  • 1.Wash your hands thoroughly with soap and water before handling supplies
  • 2.Clean the injection site with an alcohol swab and let it air dry completely
  • 3.Pinch a fold of skin at the chosen injection site
  • 4.Insert the needle at a 45-90 degree angle (depending on needle length and body composition)
  • 5.Inject the medication slowly and steadily over 5-10 seconds
  • 6.Release the skin fold and remove the needle, applying gentle pressure with a clean swab
  • 7.Rotate injection sites to prevent tissue irritation or lipodystrophy
  • 8.Dispose of the needle safely in a sharps container—never recap or reuse needles
Full Injection Guide

Storage

Before reconstitution

Store Setmelanotide in the refrigerator at 36-46°F (2-8°C) in its original packaging. Protect from light and moisture. Do not freeze. Check the expiration date before use. Some formulations may be stored at room temperature for limited periods—check your specific product labeling.

After reconstitution

Once reconstituted, Setmelanotide should be kept refrigerated at 36-46°F (2-8°C) and used within the timeframe specified on your product labeling (typically 14-28 days). Label the vial with the reconstitution date. Do not use if the solution appears cloudy, discolored, or contains particles.

Signs of degradation

  • Solution appears cloudy, discolored, or contains visible particles (should be clear)
  • Product has been exposed to temperatures outside the recommended storage range
  • Product has been frozen (unless specifically designed for freeze-thaw stability)
  • Expiration date has passed or reconstituted solution has exceeded its use-by date
  • Unusual odor, color change, or visible contamination

Sample Daily Schedule

As prescribed (once daily)

As prescribed by your healthcare provider injection

Site: subcutaneous injection—rotate sites if applicable

Maintain a consistent schedule for optimal results with Setmelanotide. Set reminders if needed. If you miss a dose, follow your healthcare provider's instructions—do not double up on doses to compensate.

Safety

Is it
safe?

Safety Profile

Setmelanotide demonstrates favorable tolerability in Phase 3 trials with safety data from over 200 patients across POMC, PCSK1, LEPR-deficient, and Bardet-Biedl syndrome populations. The most common adverse effect is dose-dependent skin hyperpigmentation (>60% of patients) due to off-target MC1R activation on melanocytes—a manageable, reversible pharmacological effect rather than true toxicity. Serious psychiatric adverse events including depression and suicidal ideation require baseline mental health screening and ongoing monitoring in all patients.

Safety evidence comes from Phase 3 trials (IMCIVREE, VENTURE) in pediatric and adult populations with confirmed genetic melanocortin pathway defects, with long-term follow-up data supporting chronic administration. FDA approval in 2020 and EMA approval in 2021 validate the benefit-risk profile in eligible populations. Ongoing Phase 2 studies in hypothalamic obesity, Prader-Willi syndrome, and Alström syndrome continue to characterize safety in expanded indications.

Common Side Effects

Experienced by some users

Skin Hyperpigmentation

The most characteristic side effect, occurring in >60% of patients. Results from off-target activation of MC1R on melanocytes. Manifests as generalized darkening of skin that develops gradually over weeks to months.

Management: Expected pharmacological effect of melanocortin receptor activation. Monitor skin changes at regular intervals. Perform baseline and periodic skin examinations including dermoscopy for nevus surveillance. Hyperpigmentation may partially reverse upon treatment discontinuation.

Injection Site Reactions

Local reactions including erythema, pruritus, induration, and mild pain at the injection site. Reported in approximately 20-30% of patients in clinical trials.

Management: Rotate injection sites between abdomen, thigh, and upper arm. Clean site before injection. Apply cold compress if needed. Reactions typically mild and self-limiting.

Nausea

Reported in clinical trials, typically mild to moderate. May be related to central MC4R-mediated effects on appetite and gastrointestinal motility.

Management: Usually resolves with continued treatment. Take with food if helpful. Slow dose titration may reduce incidence.

Diarrhea

Gastrointestinal disturbance reported in some patients, generally mild and transient.

Management: Maintain adequate hydration. Typically self-limiting and does not require dose adjustment.

Less Common

  • Hair Color Darkening and Nevus Changes

These typically resolve with continued use or dose adjustment.

Stop and Seek Help If

  • ×Severe or worsening side effects that don't improve with dose adjustment or supportive care
  • ×Signs of an allergic reaction—rash, hives, swelling, or difficulty breathing
  • ×Your healthcare provider recommends discontinuation based on your clinical response
  • ×Development of any new medical condition that may be contraindicated with Setmelanotide
  • ×Pregnancy or planning to become pregnant (unless specifically approved for use during pregnancy)
  • ×Abnormal lab results or clinical markers that suggest adverse effects

Setmelanotide should only be started, adjusted, or discontinued under medical supervision. This information is for educational purposes only and does not replace professional medical advice. Never stop a prescribed treatment without consulting your healthcare provider first, as abrupt discontinuation may have consequences.

Interactions

With other peptides

  • Essential for confirming melanocortin pathway mutations and identifying eligible patients for targeted MC4R agonist therapy
  • Complementary approach to support dietary and lifestyle modifications alongside pharmacological hunger reduction
  • Supports healthy eating patterns as hyperphagia resolves and appetite normalizes with treatment

With medications

  • !Other MC4R Agonists - Redundant mechanism of action with increased risk of melanocortin-related side effects including excessive hyperpigmentation
  • !Medications Affecting Melanocortin Signaling - Potential unpredictable interactions with melanocortin pathway signaling and altered efficacy or safety profile
  • !Photosensitizing Agents - May exacerbate skin pigmentation changes and increase risk of melanocytic nevus development in the setting of MC1R activation

With supplements

  • Multivitamins - Generally safe to take alongside Setmelanotide. Space doses apart if taking oral formulations to ensure optimal absorption.
  • Electrolyte supplements - Helpful if experiencing any GI side effects that could lead to dehydration. Safe to combine.

Want the Full Picture?

View the complete Setmelanotide research profile including mechanism of action, clinical studies, effectiveness timeline, and FAQ.

View Full Setmelanotide Profile

Medical Disclaimer

Setmelanotide is an investigational research compound not approved by the FDA for human therapeutic use. This information is for educational purposes only and should not be construed as medical advice. Always consult with a qualified healthcare provider before starting any new supplement or treatment protocol.

Last updated: 2/8/2026