Melanotan I
Afamelanotide
Overview
Melanotan I (Afamelanotide) is a synthetic alpha-melanocyte-stimulating hormone (alpha-MSH) analog approved in Europe and Australia under the brand name Scenesse as an implant for prevention of phototoxicity in adults with erythropoietic protoporphyria (EPP). Unlike Melanotan II it is more selective for MC1R and does not significantly activate MC3R MC4R or MC5R meaning it produces skin darkening without the sexual side effects associated with Melanotan II. It has completed multiple Phase 3 clinical trials and has regulatory approval making it one of the few melanocortin peptides with an established clinical evidence base.
Compound Data
Molecular Formula
C78H111N21O19
Molecular Weight
1646.80 g/mol
IUPAC Name
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-6-amino-1-[(2S)-2-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
PubChem CID
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Mechanism of Action
Melanotan I acts primarily as a selective MC1R agonist on melanocytes — the pigment-producing cells in the skin. MC1R activation stimulates the production and release of eumelanin the dark brown-black form of melanin that provides UV protection. By increasing eumelanin production prior to sun exposure Melanotan I effectively pre-tans the skin and increases its natural UV photoprotection. In the EPP indication this protection from UV-triggered protoporphyrin accumulation reduces the severe phototoxic pain attacks that characterize the condition. The selectivity for MC1R over MC4R means Melanotan I does not produce the central sexual and appetite-modulating effects seen with non-selective melanocortin agonists like Melanotan II.
Dosage Information
Typical Dose
16 mg implant (FDA/EMA approved dose for EPP)
Frequency
Implant replaced every 2 months
Administration
Subcutaneous implant (approved use) or injection (research use)
Notes
Approved as a slow-release implant for EPP. Research use of injectable form for tanning is off-label and unregulated. The implant provides sustained low-level release over 60 days.
Potential Side Effects
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Quick Facts
- Administration
- Subcutaneous implant (approved use) or injection (research use)
- Typical Dose
- 16 mg implant (FDA/EMA approved dose for EPP)
- Frequency
- Implant replaced every 2 months
- References
- 0 curated + 47 from PubMed
- Clinical Trials
- 23 registered
- Evidence Score
- 80.0 / 100