Melanotan 1 10mg

▎Melanotan-1 Structure

▎Melanotan-1 Research

What is the research background of Melanotan-1?

Melanotan-1 is a synthetic analog of α-melanocyte-stimulating hormone (α-MSH). α-MSH is produced by specific cells in the human body and plays an important role in physiological processes such as pigmentation. In order to explore its applications in different fields, researchers developed Melanotan-1. In-depth research on α-MSH led to the birth of Melanotan-1. α-MSH is known to play a key role in stimulating the production of melanin, and Melanotan-1 was designed to have stronger activity and specific functions, such as in skin tanning and potential photoprotective effects^[1] .

What is Melanotan-1?

Melanotan-1 is a synthetic analog of α-melanocyte-stimulating hormone. By binding to the MC1R on melanocytes, it stimulates melanocytes to produce melanin. It has shown significant efficacy in the treatment of erythropoietic protoporphyria and also has potential application prospects in the treatment of other skin diseases.

Melanotan-1 has the characteristic of a long-lasting effect. It can continuously stimulate melanocytes in the body to produce melanin, thus providing long-term therapeutic effects. Compared with some other treatment methods, Melanotan-1 does not require frequent administration, reducing the treatment burden on patients. In clinical studies, Melanotan-1 has shown good safety. Common adverse reactions include headache, nausea, vomiting, etc., but they are generally mild and can be relieved through appropriate treatment. In addition, Melanotan-1 has little toxicity to important organs such as the liver and kidneys, providing a certain safety guarantee for its clinical application.

What is the specific mechanism by which Melanotan-1 prevents sun damage?

Melanin in the skin plays a role in absorbing ultraviolet rays and free radicals, thus protecting the skin from ultraviolet damage. Ultraviolet radiation can cause mutations in the genes of skin cells and is the main cause of various skin cancers. The presence of melanin can reduce the direct exposure of ultraviolet rays to skin cells and lower the risk of gene mutations. After the skin is exposed to ultraviolet rays, it will cause an increase in the activity of melanocyte-stimulating hormone receptors, resulting in an increase in eumelanin in epidermal melanocytes. As an analog of α-melanocyte-stimulating hormone, Melanotan-1 can mimic this process and promote the production of melanin^[2] . By increasing the melanin content in the skin, Melanotan-1 can reduce the direct damage of ultraviolet rays to skin cells. Studies have shown that after using Melanotan-1, the skin's tolerance to ultraviolet rays is enhanced, and the occurrence of sunburn is reduced. Compared with traditional tanning methods such as sun tanning and the use of tanning products, Melanotan-1 has some unique advantages. Sun tanning requires long-term exposure to the sun, which is likely to cause skin sunburn, aging, and an increased risk of skin cancer. The use of tanning products may have problems such as skin irritation and allergies caused by chemical components. Melanotan-1, through subcutaneous injection, can more precisely control the production of melanin and reduce the adverse effects on the skin.

What is the specific mechanism of action of Melanotan-1 in the treatment of vitiligo?

Stimulating melanin production: Melanotan-1 can stimulate melanocytes to produce melanin. Melanin is an important substance that determines skin color. In patients with vitiligo, due to damaged or abnormal melanocytes, white patches appear on the skin. Melanotan-1 promotes the proliferation and differentiation of melanocytes and increases the synthesis of melanin by activating specific signaling pathways ^[3].

Regulating the immune system: Vitiligo is considered an autoimmune disease, in which the immune system abnormally attacks melanocytes. Melanotan-1 may play a role in regulating the immune system and reducing the attack on melanocytes. It may regulate the immune response by influencing the activity and function of immune cells, thus relieving the symptoms of vitiligo.

Antioxidant effect: Oxidative stress also plays an important role in the pathogenesis of vitiligo. Melanotan-1 may have certain antioxidant capacity and reduce the damage of oxidative stress to melanocytes. It can neutralize free radicals, protect melanocytes from oxidative damage, and help maintain the normal function of melanocytes.

What research data support the specific effects of Melanotan-1 in the treatment of erythropoietic protoporphyria?

Erythropoietic protoporphyria (EPP) is a hereditary porphyrin metabolic disorder in which patients experience acute phototoxic reactions, severely affecting their quality of life. As a synthetic analog of α-melanocyte-stimulating hormone, Melanotan-1 has the following research data to support its specific effects in the treatment of EPP:

Improving light tolerance: In multiple clinical studies, Melanotan-1 has been proven to improve the light tolerance of EPP patients. For example, in the Phase III trial CUV039, treatment with Melanotan-1 improved the light tolerance of EPP patients. Compared with the placebo, treatment with Melanotan-1 enabled patients to spend more time in direct sunlight without pain and increased the time until the initial symptoms of phototoxicity caused by a standardized light source appeared^[4] .

Improving quality of life: Multiple studies have shown that treatment with Melanotan-1 can improve the quality of life of EPP patients. In different clinical trials, after receiving Melanotan-1 treatment, patients' quality of life was evaluated using validated questionnaires, and the results showed an improvement in quality of life ^[4].

Protective effect on liver function: Studies have found that Melanotan-1 may have a protective effect on the liver function of EPP patients. In a retrospective observational study, 2933 liver function tests, 1186 protoporphyrin concentration tests, and 1659 Melanotan-1 implant applications of 70 EPP patients were included. The results showed that as the number of days since the last Melanotan-1 implant increased, the protoporphyrin (PPIX) concentration increased significantly (p < 0.0001); while in the past 365 days, as the Melanotan-1 dose increased, alanine aminotransferase (ALAT) and bilirubin decreased significantly (p = 0.012, p = 0.0299). This indicates that Melanotan-1 has a dose-dependent protective effect on the liver function of EPP patients^[5] .

Correlation of PPIX and liver parameters. Diagram (A): Histograms (green) show the distribution of the laboratory data. The pairwise comparisons for all laboratory data are displayed. Diagram (B): The statistical data for each test, including mean, SD, median, minimum, and maximum, are displayed.

Source:PubMed^[5]

The Australian company EpiTan has conducted research on a new topical formulation of Melanotan (Ⅰ): 

Melanotan (Ⅰ) is an analog of α-melanocyte-stimulating hormone, used to prevent sun damage. It stimulates the production of melanin, darkens the skin, and thus protects the skin from ultraviolet radiation.

There are three clinical studies that have verified the safety of Melanotan-1. In the first study, 4 subjects were randomly assigned to receive Melanotan-1 (0.08mg/kg subcutaneous injection per day), and another 4 subjects received isotonic sodium chloride (9%) solution injection for 10 days, followed by UV-B light irradiation at 3 times the minimum erythema dose (MED) on the neck.

The results showed that 3 out of 4 subjects who received Melanotan-1 achieved tanning, and the number of sunburned cells in the irradiated neck area of these subjects decreased by 47% (Dorr RT).

In the second study, the dose of MT-1 was increased to 0.16mg/kg per day for 10 days.

During (n = 7) or after (n = 5) the MT-1 administration period, the buttock area was exposed to UV-B radiation (0.25 - 0.75 MED). The results showed that the higher dose of MT-1 darkened more skin areas (Dorr RT).In the third study, 8 subjects were randomly assigned to receive half-back sunlight exposure for 3 - 5 days or sunlight exposure plus 0.16mg/kg of MT-1, 5 days a week for 4 weeks. The results showed that the back tanning in the MT-1 group was significantly enhanced, and this tanning effect lasted at least 3 weeks longer than that of the control group that only received sunlight exposure, while the control group needed 50% more sunlight exposure time to achieve the same degree of tanning ^[6].

The application of Melanotan-1 in melanoma research: 

Melanoma is a highly malignant skin tumor, and current treatment methods include surgery, radiotherapy, chemotherapy, and immunotherapy. As an MCR agonist, Melanotan-1 may play a potential therapeutic role by regulating the growth, differentiation, and apoptosis of melanoma cells. Some studies have shown that Melanotan-1 can inhibit the proliferation and invasion of melanoma cells and induce the apoptosis of melanoma cells ^[7].

Which diseases can Melanotan-1 be used to treat?

Erythropoietic protoporphyria (EPP): 

Erythropoietic protoporphyria is a hereditary porphyria caused by low ferrochelatase activity, leading to the accumulation of protoporphyrin in red blood cells, plasma, liver, and skin. Patients are usually sensitive to sunlight, and when exposed to the sun, they will experience symptoms such as skin pain, itching, erythema, and blisters. Melanotan-1 reduces the symptoms of EPP patients by stimulating the production of melanin in the skin and increasing the skin's protection against ultraviolet rays. Studies have shown that Melanotan-1 can significantly reduce the frequency and severity of phototoxic reactions in EPP patients and improve their quality of life ^[8].

Congenital erythropoietic porphyria (CIPA): 

Congenital erythropoietic porphyria is a rare autosomal recessive genetic disease, mainly caused by mutations in the hydroxymethylbilane synthase (HMBS) gene, leading to abnormal porphyrin metabolism. Patients are extremely sensitive to light, and their skin and eyes are easily damaged. Melanotan-1 can also provide certain protection against ultraviolet rays for CIPA patients by increasing the production of skin melanin and reducing their symptoms^[9] .

Solar urticaria: 

For patients with solar urticaria, Melanotan-1 can also enhance the skin's protection against ultraviolet rays and reduce the frequency and severity of urticaria symptoms ^[10].

Polymorphous light eruption (PMLE): 

Studies have shown that Melanotan-1 also has a certain therapeutic effect on PMLE patients, which can reduce the occurrence of rashes and improve the quality of life of patients^[10].

Vitiligo: 

Melanotan-1 may play a certain role in promoting the repigmentation of vitiligo patients by promoting the proliferation and differentiation of melanocytes. Although there are relatively few studies on its application in the treatment of vitiligo at present, the preliminary results show certain potential^[10].

Acne: 

The therapeutic effect of Melanotan-1 on acne may be related to its regulation of the immune system and reduction of the inflammatory response. Some studies have found that Melanotan-1 can relieve the inflammatory symptoms of acne and promote the healing of skin lesions^[10].

Hailey-Hailey disease: 

Melanotan-1 has also shown certain therapeutic effects in the treatment of Hailey-Hailey disease. This rare skin disease is characterized by repeated blisters and erosions on the skin. Melanotan-1 may improve the symptoms of patients by regulating the function of skin cells^[10].

In conclusion, as a synthetic analog of α-melanocyte-stimulating hormone (α-MSH), Melanotan-1 (melanotan I) is of great significance in the field of skin health. It can increase the melanin content in the skin, helping the skin better resist the damage of ultraviolet rays, thus preventing sunburn, reducing skin aging, and lowering the risk of skin cancer. By activating the melanocortin receptor, Melanotan-1 promotes the production and distribution of melanin, forming a natural "sunscreen" to protect skin cells from DNA damage induced by ultraviolet rays and the damage of free radicals.

In the treatment of skin diseases, Melanotan-1 also shows potential application value. For pigmentation disorders such as vitiligo, it can stimulate the activity of melanocytes and promote the synthesis of melanin, helping to restore the normal pigmentation of the skin. In addition, it also has certain potential in the treatment of diseases with uneven pigmentation such as melasma. By regulating the distribution and metabolism of melanin, it can improve the skin color and uniformity.

As a polypeptide substance, Melanotan-1 is gradually receiving more attention and research in the fields of dermatology and cosmetology, providing people with a new option to deal with skin pigment-related problems. It should be noted that the medical application of Melanotan-1 still requires rigorous evaluation. Currently, most studies have a small sample size and limited long-term safety data. However, with the development of new sustained-release formulations and local drug delivery systems, its prospects for clinical translation are promising.

About The Author

The above-mentioned materials are all researched, edited and compiled by Cocer Peptides.

Scientific Journal Author

Elizabeth A. Langan is a renowned UK dermatologist and medical researcher. She holds academic positions at multiple institutions, including Professorships at the University of Lubeck and the University of Manchester, as well as roles at Heidelberg University and Queen Mary University of London. Langan works at prestigious medical institutions such as the Schleswig-Holstein University Hospital and the Salford Royal NHS Foundation Trust. She has published many papers in professional journals like Dermatological Science. Her research areas cover dermatology, general and internal medicine, surgery, oncology, and research & experimental medicine. Her work is widely recognized and has significantly contributed to these medical fields. Elizabeth A. Langan is listed in the reference of citation [1].

▎Relevant Citations

[1] Langan E A, Nie Z, Rhodes L E. Melanotropic peptides: more than just 'Barbie drugs' and 'sun-tan jabs'?[J]. British Journal of Dermatology, 2010,163(3):451-455.DOI:10.1111/j.1365-2133.2010.09891.x.

[2] Humphrey S M, Oo T, Barnetson S C. Clinical potential of Melanota® (NDP-α-MSH) in skin protection -: current status and future perspective[J]. Experimental Dermatology, 2004,13(9):578.

[3] Perez-Bootello J, Cova-Martin R, Naharro-Rodriguez J, et al. Vitiligo: Pathogenesis and New and Emerging Treatments[J]. International Journal of Molecular Sciences, 2023,24(24).DOI:10.3390/ijms242417306.

[4] Kim E S, Garnock-Jones K P. Afamelanotide: A Review in Erythropoietic Protoporphyria[J]. American Journal of Clinical Dermatology, 2016,17(2):179-185.DOI:10.1007/s40257-016-0184-6.

[5] Minder A, Schneider-Yin X, Zulewski H, et al. Afamelanotide Is Associated with Dose-Dependent Protective Effect from Liver Damage Related to Erythropoietic Protoporphyria[J]. Life-Basel, 2023,13(4).DOI:10.3390/life13041066.

[6] Dorr R T, Ertl G, Levine N, et al. Effects of a superpotent melanotropic peptide in combination with solar UV radiation on tanning of the skin in human volunteers[J]. Archives of Dermatology, 2004,140(7):827-835.DOI:10.1001/archderm.140.7.827.

[7] Reid C, Fitzgerald T, Fabre A, et al. Atypical melanocytic naevi following melanotan injection.[J]. Irish Medical Journal, 2013,106(5):148-149. https://pubmed.ncbi.nlm.nih.gov/23914578/

[8] Dominguez-Mozo M I, Toledano-Martinez E, Rodriguez-Rodriguez L, et al. JC virus reactivation in patients with autoimmune rheumatic diseases treated with rituximab[J]. Scandinavian Journal of Rheumatology, 2016,45(6):507-511.DOI:10.3109/03009742.2015.1135980.

[9] Wu V, Sykes E A, Beyea M M, et al. Approche à adopter pour la prise en charge de la maladie de Ménière. Canadian Family Physician Medecin De Famille Canadien, 2019,65(7):468-472. https://pubmed.ncbi.nlm.nih.gov/31300427/

[10] McNeil M M, Nahhas A F, Braunberger T L, et al. Afamelanotide in the Treatment of Dermatologic Disease[J]. Skin Therapy Letter, 2018,23(6):6-10. https://pubmed.ncbi.nlm.nih.gov/30517779/

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