Melanotan 1
Afamelanotide (Melanotan I)
Melanotan I (afamelanotide) is a synthetic analogue of alpha-melanocyte-stimulating hormone (α-MSH) that binds melanocortin receptors to stimulate melanogenesis, producing a protective tan without UV exposure. It is FDA-approved (as Scenesse) for the prevention of phototoxicity in adults with erythropoietic protoporphyria (EPP), and is also used off-label to increase skin pigmentation and for photoprotection. Unlike Melanotan II, it is highly selective for MC1R and does not produce significant sexual side effects.
Mechanism of Action
Afamelanotide acts as a potent agonist at the melanocortin-1 receptor (MC1R) on melanocytes, triggering a cAMP-mediated signaling cascade that upregulates tyrosinase activity and shifts melanin production toward eumelanin (brown/black pigment) over pheomelanin. This eumelanin production increases skin pigmentation and provides intrinsic photoprotection by absorbing and dissipating UV radiation. Because its selectivity is strongly weighted toward MC1R over MC3R, MC4R, and MC5R, it avoids the centrally mediated effects on appetite and sexual function seen with less selective melanocortin agonists.
Evidence by Health Goal(14 goals)
Dosing Protocols
Morning administration preferred; implant placed by a clinician subcutaneously
Cycle: Implant: every 60 days year-round for EPP. Off-label: 4–6 week loading phase, then as-needed maintenance
The approved 16mg implant (Scenesse) is administered by a healthcare professional. Research-grade vials require reconstitution with bacteriostatic water and subcutaneous injection. Refrigeration required. Off-label dosing is not clinically validated.
Safety & Side Effects
Afamelanotide has a well-characterized safety profile from clinical trials supporting its EPP approval, with the most serious long-term concern being stimulation of melanocytic nevi requiring regular dermatological monitoring. It is a prescription-only medication in the EU, Australia, and other jurisdictions; research-grade vials exist in a legal grey area in many countries, and use outside of medical supervision carries risks related to product purity, dosing accuracy, and unmonitored nevi changes.
Possible Side Effects
- !Nausea, especially during initial loading injections
- !Facial flushing and warmth within 30–60 minutes of injection
- !Transient fatigue and mild lethargy post-dose
- !Injection site reactions including pain, bruising, or induration
- !Hyperpigmentation of pre-existing moles and nevi (requires monitoring)
- !Headache, typically mild and transient
- !Yawning (less common than with Melanotan II but occasionally reported)
- !Increased blood pressure transiently post-injection
Interactions
- -Photosensitizing drugs (e.g., tetracyclines, fluoroquinolones, amiodarone) — additive phototoxicity risk, though mechanistically afamelanotide is used to counter this in EPP
- -Immunosuppressants — may alter melanocyte immune signaling; use with caution in transplant patients
- -May transiently elevate blood pressure — use caution in patients on antihypertensives or with cardiovascular conditions
- -Concurrent use with other melanocortin peptides (e.g., Melanotan II, BPC-157 combinations) — additive hormonal stimulation effects, unpredictable interactions
- -Hormonal contraceptives — estrogen may independently increase melanin production; combined effects on pigmentation are additive and unpredictable
Cost & Where to Buy
Research-grade afamelanotide vials (typically 10mg) from peptide vendors cost approximately $30–80 per vial; a monthly supply depends on protocol. The approved Scenesse 16mg implant costs several thousand dollars per dose and is covered by insurance in some countries for EPP only. Off-label research use pricing reflects peptide vendor market rates.
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