Melanotan II
Synthetic cyclic heptapeptide non-selective melanocortin receptor agonist (Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2). Developed at the University of Arizona. Promotes melanogenesis (skin tanning via MC1R), central sexual arousal (MC4R), and appetite modulation. UNAPPROVED GLOBALLY. Subject of multiple FDA, EMA, and international regulatory public health warnings due to severe adverse events including systemic hypertension, rhabdomyolysis, renal failure, melanoma exacerbation, and priapism. Prohibited by WADA.
60-Second Scientific Briefing
Melanotan II is a synthetic cyclic lactam analogue of alpha-melanocyte-stimulating hormone (alpha-MSH). Non-selectively stimulates melanocortin receptors (MC1R, MC3R, MC4R, MC5R). Illicitly promoted for skin tanning and libido enhancement. It is NOT FDA-approved and carries severe health warnings for atypical melanocytic nevi, melanoma risk, and systemic toxicities.
What is Melanotan II?
Pharmacological Classification & Molecular IdentitySynthetic cyclic heptapeptide lactam analogue of alpha-MSH designed with enhanced resistance to enzymatic degradation.
Verified Chemical & Regulatory Registry Identifiers
Mechanism of Action & Receptor Targets
Biological Pathway and Target BindingBiological pathway and target receptor binding mechanism.
Receptor Selectivity: Stimulates MC1R on epidermal melanocytes to drive eumelanin synthesis, while also stimulating central MC4R and MC3R pathways.
Regulatory & FDA Approval Status
Legal and Regulatory ClassificationsNOT approved by the US FDA or EMA. The FDA has issued multiple warning letters against illegal marketing of Melanotan II for tanning or health claims. Prohibited by WADA under S0.
Melanotan II is not approved for commercial sale, prescription therapy, or compounded medication distribution. It exists strictly within authorized scientific and clinical research frameworks.
Human Evidence & Clinical Trials
Clinical Study Readouts and Evidence SynthesesEarly human pilot studies demonstrated melanogenesis and sexual arousal; full clinical development was abandoned due to systemic side effects including blood pressure changes and melanocytic changes.
Clinical Evidence
Early human pilot studies demonstrated melanogenesis and sexual arousal; full clinical development was abandoned due to systemic side effects including blood pressure changes and melanocytic changes.
Safety Profile & Clinical Limitations
Documented Adverse Events and Known UncertaintiesFacial flushing, severe nausea, vomiting, darkening of existing nevi (moles), development of new dysplastic nevi, systemic hypertension, priapism, and rhabdomyolysis in reported overdoses.
Long-term causal relationship with cutaneous malignant melanoma and systemic cardiovascular toxicity.
Dose Approval Status
Commercial Dosing Status and Policy DirectivesNOT ESTABLISHED. Dangerous unapproved substance with no recognized safe human dosage.
Under Egypt Peptides medical governance policies, no personal dosages, titration intervals, cycles, stacking recommendations, or self-injection instructions may be provided for unapproved investigational compounds. Clinical study protocols represent controlled experimental research parameters exclusively.
What is Known vs. What is Unknown
Evidence Comparison and Clinical Evidence Boundaries✓ Confirmed Scientific Evidence
- Synthetic cyclic heptapeptide lactam analogue of alpha-MSH designed with enhanced resistance to enzymatic degradation.
- Targets & Selectivity: Stimulates MC1R on epidermal melanocytes to drive eumelanin synthesis, while also stimulating central MC4R and MC3R pathways.
- Early human pilot studies demonstrated melanogenesis and sexual arousal; full clinical development was abandoned due to systemic side effects including blood pressure changes and melanocytic changes.
- Safety considerations: Facial flushing, severe nausea, vomiting, darkening of existing nevi (moles), development of new dysplastic nevi, systemic hypertension, priapism, and rhabdomyolysis in reported overdoses.
? Unknown / Under Ongoing Investigation
- Long-term causal relationship with cutaneous malignant melanoma and systemic cardiovascular toxicity.
Verified Questions & Answers
10 Verified scientific answers with permanent anchor keysMelanotan II is classified as a Non-Selective Melanocortin Receptor Agonist. Molecular structure: Synthetic cyclic heptapeptide lactam analogue of alpha-MSH designed with enhanced resistance to enzymatic degradation..
Pharmacological classification and molecular integrity are documented in verified regulatory and scientific literature.
Melanotan II exerts biological activity via Stimulates MC1R on epidermal melanocytes to drive eumelanin synthesis, while also stimulating central MC4R and MC3R pathways..
Receptor binding affinity and selectivity dictate the physiological response observed in laboratory and clinical trials.
Regulatory status: NOT approved by the US FDA or EMA. The FDA has issued multiple warning letters against illegal marketing of Melanotan II for tanning or health claims. Prohibited by WADA under S0.
Investigational and research-only compounds cannot be legally distributed or marketed as prescription drugs.
- World Anti-Doping Agency (WADA) Prohibited List: Non-Approved Substances (S0) and Peptide Hormones (S2) (World Anti-Doping Agency, 2024-01-01)
- FDA Bulk Drug Substances Used in Compounding Under Section 503A of the FD&C Act (Category 2 Safety Evaluation) (U.S. Food and Drug Administration, 2023-09-29)
Clinical evaluation status: Early human pilot studies demonstrated melanogenesis and sexual arousal; full clinical development was abandoned due to systemic side effects including blood pressure changes and melanocytic changes.
Clinical trial readouts and systematic analyses establish the boundary between demonstrated findings and experimental hypotheses.
Reported safety profile: Facial flushing, severe nausea, vomiting, darkening of existing nevi (moles), development of new dysplastic nevi, systemic hypertension, priapism, and rhabdomyolysis in reported overdoses.
Adverse reaction monitoring and contraindications are critical parameters in pharmacological risk-benefit evaluation.
- FDA Bulk Drug Substances Used in Compounding Under Section 503A of the FD&C Act (Category 2 Safety Evaluation) (U.S. Food and Drug Administration, 2023-09-29)
- Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization (Peptides, 2006-04-01)
Key scientific uncertainties: Long-term causal relationship with cutaneous malignant melanoma and systemic cardiovascular toxicity.
Egypt Peptides enforces strict transparency regarding scientific limitations and gaps in longitudinal clinical data.
- FDA Bulk Drug Substances Used in Compounding Under Section 503A of the FD&C Act (Category 2 Safety Evaluation) (U.S. Food and Drug Administration, 2023-09-29)
NOT ESTABLISHED. Dangerous unapproved substance with no recognized safe human dosage.
Under medical governance mandates, clinical study dosages represent strictly controlled experimental parameters and must never be interpreted as individual therapeutic advice.
- FDA Bulk Drug Substances Used in Compounding Under Section 503A of the FD&C Act (Category 2 Safety Evaluation) (U.S. Food and Drug Administration, 2023-09-29)
Storage status: NOT ESTABLISHED. Illegal for commercial prescription or over-the-counter human distribution.
Peptide integrity degrades rapidly when exposed to elevated temperatures, repeated freeze-thaw cycles, or direct UV light exposure.
- FDA Bulk Drug Substances Used in Compounding Under Section 503A of the FD&C Act (Category 2 Safety Evaluation) (U.S. Food and Drug Administration, 2023-09-29)
Yes. Unapproved pharmacological substances are strictly prohibited at all times in competitive sports under WADA Category S0 (Non-approved substances) or Category S2.
Athletes subject to drug testing face strict liability and multi-year competition bans upon detection of prohibited peptides or their metabolites.
- World Anti-Doping Agency (WADA) Prohibited List: Non-Approved Substances (S0) and Peptide Hormones (S2) (World Anti-Doping Agency, 2024-01-01)
- FDA Bulk Drug Substances Used in Compounding Under Section 503A of the FD&C Act (Category 2 Safety Evaluation) (U.S. Food and Drug Administration, 2023-09-29)
Egypt Peptides provides peer-reviewed scientific reference monographs for research documentation. We strictly prohibit individual medical consultations, reconstitution guides, stacking recipes, or off-label use instructions.
All scientific claims must link to verified authoritative sources (FDA, PubMed, ClinicalTrials.gov) with zero tolerance for ungrounded marketing claims.
Authoritative Sources & Literature Registry
Regulatory dossiers, clinical trial registries, and peer-reviewed studiesWorld Anti-Doping Agency (WADA) Prohibited List: Non-Approved Substances (S0) and Peptide Hormones (S2) ↗
https://www.wada-ama.org/en/prohibited-list
FDA Bulk Drug Substances Used in Compounding Under Section 503A of the FD&C Act (Category 2 Safety Evaluation) ↗
https://www.fda.gov/drugs/human-drug-compounding/bulk-drug-substances-used-compounding-under-section-503a-fdc-act
Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization ↗
https://doi.org/10.1016/j.peptides.2005.01.029