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Weight & MetabolismCyclic octapeptide melanocortin-4 (MC4) receptor agonist

Setmelanotide

Setmelanotide is studied as a cyclic octapeptide melanocortin-4 (mc4) receptor agonist in biochemical and physiological models.

ApprovedPreclinical Models Only (Animal / Lab)Also known as: Imcivree, RM-493, BIM-22493Skip to Human Evidence ↓
Other Research Areas

Setmelanotide Biological Classification

Research Record

Investigated within physiological and chemical models.

At a glancePlain English, then the evidence
Not graded

What kind of compound

Peptide

Cyclic octapeptide melanocortin-4 (MC4) receptor agonist.

Human testing on file

0human records

0 animal · 0 total indexed. No plain-English evidence summary on file.

Regulatory position

FDA-approved drug substance

Studied for

Melanocortin analogues

Reviewed 15 September 2026

Known safety concerns in this file

  • No sourced human safety summary is recorded for this compound.

Commonly compared with

No comparison set is recorded for this compound yet.

Open side-by-side comparison →
1

What is Setmelanotide?

Setmelanotide is classified as a cyclic octapeptide melanocortin-4 (mc4) receptor agonist. An approved cyclic melanocortin-4 receptor agonist for rare genetic and acquired forms of obesity. It belongs to the same melanocortin analogue family as bremelanotide, afamelanotide and melanotan II, each with its own regulatory position.

2

Why are people interested in it?

Researchers and clinicians study Setmelanotide primarily to understand its biological interactions, receptor binding affinity, and potential role within its biochemical class.

Primary Research Categories

  • Melanocortin analogues
  • Approved drug substances
3

How does it work in the body?

Setmelanotide interacts with specific cellular receptors and metabolic pathways corresponding to its structural classification as a cyclic octapeptide melanocortin-4 (mc4) receptor agonist.

In Everyday Language: In laboratory settings, Setmelanotide interacts with specific cellular targets to modulate biological signaling pathways associated with cyclic octapeptide melanocortin-4 (mc4) receptor agonist biology.
Cellular & Receptor Signaling: Setmelanotide interacts with specific cellular receptors and metabolic pathways corresponding to its structural classification as a cyclic octapeptide melanocortin-4 (mc4) receptor agonist.

Biological Pathway Overview

Setmelanotide Receptor & Target Interactions

This compound is evaluated in scientific research for its interactions with target cellular receptors and signaling cascades. Consult the evidence section below for specific peer-reviewed papers.

Target Pathway

Engages specific cellular signaling cascades characteristic of its structural family.

Endocrine/Paracrine Activity

Investigated for its regulatory effects on local tissue synthesis and cellular signaling.

4

What has actually been demonstrated in humans?

Preclinical Models Only (Animal / Lab)

Evidence for Setmelanotide is currently derived primarily from laboratory or preclinical models. Consult the published evidence file for specific indexed studies.

Pharmaceutical Reality vs. Unregulated Research Chemicals

Setmelanotide is not an FDA-approved medication. Always verify chemical identity and testing documentation before interpreting research literature.

5

What is still uncertain or unknown?

Controlled human clinical trials evaluating Setmelanotide for therapeutic efficacy, safety, and pharmacokinetics are limited or absent in peer-reviewed Western registries.

Regulatory Position: Setmelanotide is an investigational or unapproved compound. It is not approved by the FDA as a commercial pharmaceutical.

No evidence records in this file yet.

What Has Actually Been Studied

    What is Still Unknown

    What we know

      Editorial reading of the records below, labelled as Therapept analysis. How records are built

      What remains uncertain

        Preparation and Handling

        Lyophilized peptides ship as freeze-dried powders; whatever happens next involves diluents, concentrations and storage conditions that are compound- and product-specific.

        United States Regulatory Status

        FDA-approved drug substance

        Application: NDA 213793 (IMCIVREE)

        Approved Indication: Marketed in the United States as IMCIVREE, approved to reduce excess body weight and maintain weight reduction in specified patients with acquired hypothalamic obesity, Bardet-Biedl syndrome, or obesity due to POMC, PCSK1 or LEPR deficiency confirmed by genetic testing.

        • IMCIVREE (setmelanotide acetate), NDA 213793, approved 25 November 2020 as a new molecular entity under priority review.
        • The label effective 1 April 2026 includes acquired hypothalamic obesity alongside the genetic indications.
        • Not named on the WADA 2026 Prohibited List.
        Technical Chemical SpecificationsClick to view CAS, sequence, and molecular formulas
        Molecular weight
        1117.3 Da (anhydrous free base, FDA label)
        Sequence length
        97 chars
        CAS number
        920014-72-8
        PubChem CID
        11993702
        Compound class
        Cyclic octapeptide melanocortin-4 (MC4) receptor agonist
        Sequence
        Ac-Arg-cyclo[Cys-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH2, with a disulfide bond between residues 2 and 8
        Molecular formula
        C49H68N18O9S2
        Molecular weight
        1117.3 Da (anhydrous free base, FDA label)
        CAS number
        920014-72-8
        PubChem CID
        11993702

        Sources

        1. PubChem CID 11993702
        2. Drugs@FDA — NDA 213793 (IMCIVREE)
        3. DailyMed — IMCIVREE prescribing information
        4. WADA 2026 Prohibited ListEffective 1 January 2026.

        Last reviewed 15 September 2026 · Compiled by Therapept Editorial · How these records are built