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Research Overview
Selective MC4R agonist; directly activates hypothalamic melanocortin-4 receptors to restore appetite regulation in patients with loss-of-function mutations in the leptin/melanocortin pathway (POMC, PCSK1, LEPR, BBS). MC1R cross-activity causes universal skin hyperpigmentation.
Setmelanotide activates the melanocortin-4 receptor (MC4R) in the hypothalamus — the central appetite-regulation hub of the brain. In patients with loss-of-function mutations in genes critical to the leptin-melanocortin pathway (POMC, PCSK1, LEPR), signalling to hypothalamic MC4R is absent or severely reduced, causing extreme hyperphagia (pathological overeating) and early-onset severe obesity.
By directly activating MC4R, setmelanotide bypasses the genetic defect in the upstream signalling chain to restore appetite regulation. Clinical trials in POMC-deficient and LEPR-deficient patients demonstrated dramatic reductions in hunger and clinically meaningful weight loss — effects that are essentially specific to patients with the relevant genetic disruption, rather than reflecting general appetite suppression in all patients.
Skin hyperpigmentation is a universal side effect because MC4R and the related MC1R receptor (which controls melanin production) share the melanocortin pathway. Setmelanotide's MC1R activity produces predictable skin darkening in all patients, which is important for informed consent and patient monitoring.
Sold strictly as a research chemical for non-human, in-vitro, and laboratory use
FDA approved compound
Prescription availability in Australia and internationally
In Australia, setmelanotide (imcivree) has no TGA approval for therapeutic use. It is sold by Capital Peptides strictly as a research chemical for non-human, in-vitro, and laboratory research use only.
Setmelanotide (Imcivree) research is most relevant to protocols examining:
Genetic obesity research
POMC, PCSK1, and LEPR deficiency studies
Bardet-Biedl syndrome and melanocortin pathway research
MC4R pharmacology and appetite regulation studies
Researchers studying leptin pathway restoration in monogenic obesity
Initial phase
Compound begins accumulating in target tissue. Most researchers note subtle changes by end of week one. Baseline measurements recommended.
Early response
Measurable effects begin to establish. Mid-cycle assessment is appropriate at this point in well-designed protocols.
Peak activity window
Primary outcomes are typically strongest in this window. Human trial literature provides benchmarks for comparison.
Washout & review
Allow full washout (~5× half-life: ~11 hours). Review data, confirm baseline recovery before any repeat protocol.
Selective MC4R agonist; directly activates hypothalamic melanocortin-4 receptors to restore appetite regulation in patients with loss-of-function mutations in the leptin/melanocortin pathway (POMC, PCSK1, LEPR, BBS). MC1R cross-activity causes universal skin hyperpigmentation.
| Parameter | Value |
|---|---|
| Dose range | 1–3 mg/day (subcutaneous |
| Alt. dose 2 | titrated) |
| Schedule | Once daily |
| Route | Subcutaneous |
| Half-life | ~11 hours |
MC1R activation across all skin types)
reported in trials)
For research use only. Capital Peptides products are not approved by the TGA for therapeutic use. By purchasing you confirm you are a licensed research entity or qualified professional.