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Dermatological — MC1R Agonist✓ FDA Approved

Afamelanotide (Melanotan I)

Also known as: Melanotan I · MT-1 · CUV1647 · Scenesse · NDP-alpha-MSH

MW

1647.87 Da

Amino Acids

13 AA

Half-Life

15 hours (sustained from implant)

Route

Implant, SubQ

CAS

75921-69-6

Formula

C78H111N21O19

Amino Acid Sequence

Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2

Mechanism of Action

Afamelanotide (Melanotan I, [Nle4, D-Phe7]-α-MSH) is a 13-amino acid linear analog of α-MSH with a norleucine substitution at position 4 and D-phenylalanine at position 7 for enhanced MC1R selectivity and metabolic stability. FDA-approved as Scenesse.

MC1R SELECTIVITY: More selective for MC1R than Melanotan II — minimal MC3R/MC4R/MC5R activation. This means effective tanning/photoprotection WITHOUT the sexual arousal, appetite suppression, or nausea effects of MT-2.

MC1R → EUMELANIN: MC1R activation on melanocytes → adenylyl cyclase → cAMP → CREB → MITF transcription factor → tyrosinase and TRP-1/TRP-2 upregulation → eumelanin synthesis. Eumelanin is the photoprotective brown-black melanin (vs pheomelanin which is red-yellow and generates ROS upon UV exposure).

EPP APPLICATION: In erythropoietic protoporphyria (EPP), protoporphyrin IX accumulates in skin and causes severe phototoxic reactions upon light exposure. Eumelanin produced by afamelanotide absorbs UV and visible light, reducing protoporphyrin activation and enabling patients to tolerate sunlight.

Dosing Protocol

Low Dose

███ – ███ mcg/day

Standard Dose

███ mcg/day

High Dose

███ – ███ mcg/day

Dosing protocols are for paid members

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Frequency

Subcutaneous implant every 60 days (biodegradable rod).

Half-Life

15 hours (sustained from implant)

Reconstitution Guide

Full reconstitution protocol with BAC water volumes, concentration math, and units-to-draw per dose is available on the Clinical plan.

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Clinical Warnings

FDA-approved only for EPP.

Mole darkening and new nevi — dermatologic monitoring required.

Melanoma screening before and during treatment.

Nausea, headache common.

Hyperpigmentation may be uneven.

Implant insertion requires clinical visit.

Contraindications

Absolute

Severe hepatic impairment

Pregnancy

Relative Cautions

Many moles/nevi

Melanoma history

Side Effect Profile

Mild

  • Nausea
  • Headache
  • Flushing

Moderate

  • Darkening of moles
  • Skin discoloration
  • Abdominal pain

Severe (Rare)

  • Melanoma risk in predisposed individuals

Synergistic Peptides

Melanotan II

Research Status

FDA APPROVED (Scenesse). PMID 26222094 (Langendonk 2015 NEJM): Phase III EPP trial — significant increase in pain-free sun exposure. Also EMA approved.

Frequently Asked Questions

How does Afamelanotide (Melanotan I) work?

Afamelanotide (Melanotan I, [Nle4, D-Phe7]-α-MSH) is a 13-amino acid linear analog of α-MSH with a norleucine substitution at position 4 and D-phenylalanine at position 7 for enhanced MC1R selectivity and metabolic stability. FDA-approved as Scenesse. MC1R SELECTIVITY: More selective for MC1R than Melanotan II — minimal MC3R/MC4R/MC5R activation. This means effective tanning/photoprotection WITHOUT the sexual arousal, appetite suppression, or nausea effects of MT-2. MC1R → EUMELANIN: MC1R acti

What is the standard dose of Afamelanotide (Melanotan I)?

Afamelanotide (Melanotan I) dosing protocols are available with a ClinPep Clinical subscription. Dosing varies by indication and patient factors — consult a licensed healthcare provider. General frequency: Subcutaneous implant every 60 days (biodegradable rod).

What is the half-life of Afamelanotide (Melanotan I)?

The half-life of Afamelanotide (Melanotan I) is 15 hours (sustained from implant). This determines optimal dosing frequency and timing.

Who should not use Afamelanotide (Melanotan I)?

Afamelanotide (Melanotan I) is absolutely contraindicated in: Severe hepatic impairment; Pregnancy. Use with caution in: Many moles/nevi; Melanoma history.

What are the side effects of Afamelanotide (Melanotan I)?

Common mild side effects include: Nausea, Headache, Flushing. Moderate effects: Darkening of moles, Skin discoloration, Abdominal pain.

What peptides stack well with Afamelanotide (Melanotan I)?

Afamelanotide (Melanotan I) is commonly stacked with: Melanotan II.

How do you reconstitute Afamelanotide (Melanotan I)?

Afamelanotide (Melanotan I) is reconstituted with bacteriostatic water. Exact volumes, concentrations, and units-to-draw calculations are available in the ClinPep Clinical plan. Always follow your compounding pharmacy's instructions.

How long should you cycle Afamelanotide (Melanotan I)?

Afamelanotide (Melanotan I) cycle protocols vary by indication. Detailed cycle length, on/off schedules, and monitoring guidelines are available with ClinPep Clinical access. Consult your healthcare provider for personalized cycling guidance.

References & Citations

10 PubMed studies · 3 clinical trials

New pharmacotherapies for the erythropoietic protoporphyrias: an analysis of trial protocols from a patient perspective.

Dechant Cornelia, Wäscher Sebastian, Granata Francesca, Gusset Nicole et al.. Orphanet journal of rare diseases. 2025

PubMed: 41466311DOI ↗C — Research Article

The erythropoietic protoporphyrias (EPP) are a group of ultra-rare (1:100.000) inborn errors of the heme biosynthesis characterised by painful phototoxic reactions in tissue exposed to visible light.

Letter to the Editor - Qualitative evidence submitted by patients to NICE: need for more quality or unrealistic and unfair requirements?

Falchetto Rocco, Barman-Aksözen Jasmin. Journal of comparative effectiveness research. 2025

PubMed: 41165369DOI ↗C — Research Article

Burden of illness and unmet needs in patients with erythropoietic protoporphyria and X-linked protoporphyria: A large US nationwide claims analysis.

DerSarkissian Maral, Norregaard Chelsea, Romdhani Hela, Muthukumar Aruna et al.. Journal of managed care & specialty pharmacy. 2025

PubMed: 41118158DOI ↗C — Research Article

Erythropoietic protoporphyria (EPP) and X-linked protoporphyria (XLP) are rare genetic disorders caused by the accumulation of the toxic metabolite protoporphyrin IX, which results in painful phototox

Polymorphism of Melanocortin Receptor Genes-Association with Inflammatory Traits and Diseases.

Bardhan Mainak, Anand Ayush, Javed Amaan, Chilo Maria Andrea et al.. Diseases (Basel, Switzerland). 2025

PubMed: 41002740DOI ↗C — Research Article

Melanocortin receptors (MCRs) are responsible for various functions ranging from skin pigmentation, regulation of appetite, stress response and cognition, steroid synthesis, and energy balance to cell

Erythropoietic protoporphyria in childhood: clinical clues, missed diagnoses and emerging therapy.

Toenne Moritz, Schaefer Tim. European journal of pediatrics. 2025

PubMed: 40858983DOI ↗C — Research Article

Erythropoietic protoporphyria (EPP) is a rare photodermatosis presenting in early childhood with severe pain upon exposure to visible light, including sunlight and artificial sources, often without vi

Afamelanotide in managing cutaneous phototoxicity in erythropoietic protoporphyria: a Scottish perspective.

Dawe Robert S, Kerr Alastair, Eadie Ewan, Waterston Suzanne et al.. Clinical and experimental dermatology. 2025

PubMed: 40692281DOI ↗C — Research Article

German Cohort Observational Study to Investigate the Short- and Long-Term Safety and Clinical Effectiveness of Afamelanotide 16 mg (SCENESSE) in Patients With Erythropoietic Protoporphyria (EPP).

Homey Bernhard, Schelonke Kathrin, Schlegel Carla Marie, Bruch-Gerharz Daniela et al.. Photodermatology, photoimmunology & photomedicine. 2025

PubMed: 40082741DOI ↗C — Research Article

Afamelanotide 16 mg (SCENESSE) is the first approved treatment for erythropoietic protoporphyria (EPP). EPP is a rare autosomal recessive inherited disorder of the haem biosynthesis pathway, wh

Discovery of MT-7117 (Dersimelagon Phosphoric Acid): A Novel, Potent, Selective, and Nonpeptidic Orally Available Melanocortin 1 Receptor Agonist.

Sato Atsushi, Morokuma Kenji, Adachi Takashi, Andou Junki et al.. Journal of medicinal chemistry. 2024

PubMed: 39641249DOI ↗C — Research Article

Activation of the melanocortin 1 receptor (MC1R) mediates melanogenesis in melanocytes, anti-inflammatory effects in inflammatory cells, and antifibrotic effects in fibroblasts. Thus, MC1R agonists ar

Registered Clinical Trials

Afamelanotide and Narrow-Band Ultraviolet B (NB-UVB) Light in the Treatment of Nonsegmental Vitiligo

NCT01382589COMPLETEDPHASE2

A Study to Assess the Changes in Pigmentation and Safety of Afamelanotide in Patients With Vitiligo on the Face

NCT05210582UNKNOWNPHASE2

Implant Pharmacokinetic and Pharmacodynamic Study

NCT03634137COMPLETEDPHASE1

Symptom Indications

Erythropoietic protoporphyria (EPP)Sun sensitivity disorders

Full Clinical Access

Complete Afamelanotide (Melanotan I) Protocol

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This information is for educational and research reference purposes only. ClinPep does not provide medical advice, diagnosis, or treatment recommendations. All protocols should be reviewed by a licensed healthcare provider.