Guide to Melanotan 1 Peptide
The well-known medication to manage erythropoietic protoporphyria disorder is Afamelanotide, which is also called Melanotan 1 peptide (3).
Erythropoietic protoporphyria is an inherited condition which primarily occurs to the abnormally elevated levels of certain chemicals (called the porphyrins) in the human body. These high levels of chemicals are present due to the absence of certain enzymes in the body which are vital for the synthesis of hemoglobin (1,2).
This is an extremely rare disorder that reportedly only occurs in 1 person amongst 75000 to 200,000 people (2) and occurs during infancy when first exposed to the sun.
While the severity of this condition varies, it usually depends on the lengths of sun exposure causing stinging, burning sensations, which may also lead to permanent lesions on skin (2).
What is Melanotan 1 peptide?
Melanotan 1 is a synthetic peptide similar to the endogenous alpha melanocyte stimulating hormone (α-MSH)(3).
Melanotan 1 is composed of 13 amino acids, same as α-MSH, but differs by only two amino acids from the endogenous peptide hormone.
This structural difference is primarily why the synthetic peptide has an improved biological effect, since it allows the peptide to exert higher affinity towards the target cells and has a longer half-life (3).
Melanotan I (Afamelanotide) is sold under the brand name of Scenesse (3).
The naturally occurring peptide hormone α-MSH was first isolated in the 1950s, and its role in promoting melanin production was known in the 1960s (4).
In 2006, Melanotan I was then licensed by an Australian start-up company to pursue it as a tanning agent (5).
Because the isolated peptide hormone was found to have a short half-life, the Australian company collaborated with another research company to develop a synthetic formulation to aid longer activity. Thus, after several studies the synthetic Melanotan I, Afamelanotide was synthesized.
This synthetic medication Afamelanotide was approved by the EU in 2014 and recently approved by the US FDA in late 2019 (3). Despite being approved relatively recently, this medication has been available as an orphan drug in the US markets since 2008 (3).
Mechanism of Action
Melanotan I primarily mimics the function of the endogenous α-MSH and binds to the melanocortin receptors (3).
Patients suffering from erythropoietic porphyria do not possess the enzyme called ferrochelatase. This enzyme is required to add iron into the protoporphyrin chemical to synthesize heme (heme, or haem, is a precursor to hemoglobin synthesis, which is required to maintain optimal oxygen levels in the bloodstream)(9). As a result of the enzyme deficiency, the body accumulates excessive protoporphyrin chemicals. When exposed to UV rays of the sun, protoporphyrin, which is photodynamic in nature, produces reactive oxygen that damages internal tissues (3).
Melanotan I, similar to endogenous α-MSH, binds to the melanocortin receptors and stimulates the production of eumelanin, which is a photoprotective compound. This eumelanin subsequently protects the tissues from any damage induced by UV exposure (3). Moreover, eumelanin production also leads to skin tanning.
The main benefit of synthetic Melanotan I is that it is not dependent on UV exposure to exert its effects. The endogenous α-MSH only functions once exposed to UV radiation.
Uses of Melanotan 1
The main uses of the Melanotan I peptide are:
- Used in the management of erythropoietic protoporphyria
- Used to induce skin tanning, as desired
- Used indoors without sunlight exposure
- Used outdoors, safely in combination with sunlight
Research and Clinical Studies on Melanotan
Clinical Trials on Patients Suffering from Erythropoietic Porphyria
There were three clinical trials (6) conducted to examine the effects of Melanotan on the erythropoietic porphyria patients. Trials were conducted in 244 patients, both males and females, and mostly aged between 18 to 64 years.
All patients were divided into two groups, one that was treated with the peptide and the other that was treated with placebo. Patients received the implants (of either the peptide or placebo) every two months and were monitored for 180 days. The patients reported the number of hours they were exposed to direct sunlight and if they experienced any pain on sunlight exposure.
Similar to Trial I, patients were divided into groups receiving the implants (of either the peptide or placebo) every two months and were monitored for 270 days.
In this trial, patients were subject to a randomized study where they received a total of 3 implants of either the Melanotan I or the placebo, via subcutaneous route and were monitored for 180 days. The main aim of this trial was to assess any potential adverse effects of the peptide.
The outcome of this study was that the patients who received the peptide were able to spend more time in sunlight with no pain (approximately 64 hours) as compared to patients who were treated with placebo (approximately 40 hours).
Studies Demonstrating Synergistic Effects of Peptide in Combination with UV Radiation
The main aim of this study (7) was to establish the safety of the peptide when used in combination with UV-B light or sunlight.
The study was divided into three phase 1 clinical trials.
In the first study, 4 subjects were administered with 0.08 mg/kg subcutaneous daily dose of peptide and 4 subjects were administered with placebo, for 10 days. Once dose was administered, all subjects were exposed to UV irradiation in the neck area.
In the second, 12 subjects were administered with increased dosing of 0.16 mg/kg subcutaneous dose every day for 10 days. 7 subjects were exposed to UV irradiation in the buttock area during administration and 5 subjects were exposed to UV radiation after administration.
The last study was carried out in 8 subjects where some volunteers were administered with 0.16 mg/kg subcutaneous peptide dose daily for 5 days each week for 4 weeks and some volunteers were given no treatment. All subjects were then exposed to sunlight to half of the back for 3 to 5 days per week.
The outcome of the study was that as the dose increased, the tanning of the skin also increased causing small sunburn cells. In the final study, there was significantly improved tanning in volunteers subject to peptide and sunlight both compared to the ones only exposed to sunlight. Also, the peptide treated volunteers maintained the skin tan for at least 3 weeks longer than the control group.
There were some minimal side effects such as nausea and facial flushing, with no other adverse events reported.
This study demonstrates that Melanotan I can safely be used in combination with UV radiation to promote enhanced tanning.
Side Effects of Melanotan 1
The common side effects of the Melanotan I peptide include (6):
- Reactions at the site of injection
- Throat pain and cough
- Lethargy and dizziness
- Skin darkening (if not desired)
- Induced sleep
- Skin irritation
- Possible respiratory tract infection
Since the peptide causes darkening of the skin, it is recommended to have the skin regularly examined.
The peptide is usually administered as subcutaneous implants with slow drug releasing properties (3).
Most of the drug is released within 48 hours, with more than 90% of the drug released within the first 5 days of administration (3).
The peptide appears to be completely cleared from the body within 10 days, since no traces of the peptide were found in the clinically tested patients after 10 days (3).
The peptide is extensively metabolized and is eliminated from the body either via fecal or biliary route.
Melanotan 1 Half-life
The half-life of the peptide is about 30 minutes. This half-life is extended to 15 hours via administration of the slow-release implants given via subcutaneous route (3).
Below listed is a unique and extensive user experience case study (8) that provides an enhanced meaning to future motives for use and injection practices.
In this case, the user, an exotic dancer, had no prior experience of self-injecting the drugs and was introduced to the synthetic medication via peer support. The user was aware of the injecting practices i.e., not to use the same needle more than once, storing the product under refrigerated conditions, and using sterilized water to dissolve the powder (8). She was also aware to self-manage in the event of nausea and other side effects.
As per the user, she experienced feelings of self confidence and perceived attractiveness due to the effectiveness of the product in darkening her skin.
There were no long term or chronic outcomes reported. This demonstrated that the long-term use of the product is potentially safe and well tolerated by the body.
While the peptide has recently been approved for use in erythropoietic porphyria patients, it is only available for use via prescriptions only.
Melanotan I is a synthetic peptide composed of 13 amino acids and is analogous to the human hormone called α-melanocyte-stimulating hormone (α-MSH).
Melanotan I binds to the melanocortin receptors and stimulates the production of eumelanin, which is a photoprotective compound. This increased production leads to skin darkening and protects the tissue cells from UV induced damage.
Clinical trials conducted so far have demonstrated safe use of the peptide with minimal side effects. Official analysis is yet to be conducted, however, based on user experience, it has been presumed that the peptide is well tolerated and leads to no chronic events when used long term.
The peptide was recently approved by the US FDA in late 2019 for use via prescriptions only(6). However, it has been made easily available through online platforms and is also administered in beauty and tanning salons (8). Several regulatory bodies have issued warning letters in the past to warn consumers to avoid random use of the peptide.
Additional research on the peptide continues to date to determine the full scope and potential of the peptide in terms of long term use as well as to potentially treat (or manage) other skin disorders.
1. Rare Disease Database. National Organization for Rare Disorders. https://rarediseases.org/rare-diseases/erythropoietic-protoporphyria/
2. Lecha, M., Puy, H., & Deybach, J. C. (2009). Erythropoietic protoporphyria. Orphanet journal of rare diseases, 4, 19. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2747912/
3. National Center for Biotechnology Information. “PubChem Compound Summary for CID 16197727, Afamelanotide” https://pubchem.ncbi.nlm.nih.gov/compound/Afamelanotide
4. The Role of Melanin-Concentrating Hormone in Color Change. B. Baker. Annals of the New York Academy of Sciences. Vol 680, Issue 1. p.279-289. May 1993. https://doi.org/10.1111/j.1749-6632.1993.tb19690.x
5. EpiTan focuses on Melanotan, a potential blockbuster. 2004 newsletter. https://www.thepharmaletter.com/article/epitan-focuses-on-melanotan-a-potential-blockbuster
6. Drug Trials Snapshots: Scenesse. https://www.fda.gov/drugs/drug-approvals-and-databases/drug-trials-snapshots-scenesse
7. Dorr RT, Ertl G, Levine N, Brooks C, Bangert JL, Powell MB, Humphrey S, Alberts DS. Effects of a superpotent melanotropic peptide in combination with solar UV radiation on tanning of the skin in human volunteers. Arch Dermatol. 2004 Jul. https://pubmed.ncbi.nlm.nih.gov/15262693/
8. Van Hout MC, Brennan R. An in-depth case examination of an exotic dancer’s experience of melanotan. Int J Drug Policy. 2014 May;25(3):444-50. https://pubmed.ncbi.nlm.nih.gov/24280586/
9. Hooda, J., Shah, A., & Zhang, L. (2014). Heme, an essential nutrient from dietary proteins, critically impacts diverse physiological and pathological processes. Nutrients, 6(3), 1080–1102. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3967179/
NOTE: These products are intended for laboratory research use only. Melanotan 1 for sale is not intended for personal use. Please review and adhere to our Terms and Conditions before ordering.