Melanotan II is an analog of the peptide hormone alpha-melanocyte stimulating hormone that induces skin tanning. Researchers knew that one of the best defenses against skin cancer was a natural tan which has been slowly developed over weeks. They hypothesized that an effective way to reduce skin cancer rates in people would be to induce the body’s natural tanning system to produce a protective tan prior to UV exposure. They knew the body’s naturally occurring hormone alpha-melanocyte stimulating hormone caused melanogenesis, a process by which the skin’s tanning cells (melanocytes) produce the skin’s tanning pigment (melanin). With that knowledge they tested to see if administering this hormone to the body directly could be an effective method to cause sunless tanning. What they found was that while it appeared to work, natural alpha-MSH had too short a half life in the body to be practical as a therapeutic drug. So they decided to try and find a more potent and stable alternative, one that would be more practical.

Melanotan and Melanotan II are not dyes, lotions, or other forms of fake tanning. The hormones stimulate the body’s own melanin production to give users a deep and natural tan without an orange hue or uneven color.

Melanotan is popular with athletes and fitness enthusiasts who wish to have the look of a tanned body, but would rather not expose themselves to the potentially harmful rays of the sun.

Melanotan-1 or MT-1, is a more potent version of the body’s hormone that tans the skin in response to sunlight. Results of studies in humans show that melanotan-1 safely increases the skin’s tanning response to exposure to artificial UV-B light or natural sunlight.

“If the goal of sun exposure is simply to obtain a tan, then MT-1 in combination with a minimal amount of sunlight should provide a tan, which reduces the need for substantial solar exposure,” write researcher Robert T. Dorr, PhD, of the University of Arizona, and colleagues in the July issue of the Archives of Dermatology. “This might considerably reduce the damage to skin from solar exposure.”

Researchers say the findings also show that use of the drug may help reduce the risk of skin cancer associated with use of tanning beds.

In the studies, researchers examined the safety of the drug when given at various doses for up to four weeks at a time in three different trials with human volunteers. They also studied the effects of the MT-1 on skin exposed to UV-B light or natural sunlight.

The first study showed that three out of four people who received injections of the lowest dose of the drug tanned after exposure to UV-B light on their necks. They also had 47% fewer sunburn cells compared with four volunteers who received a placebo injection.

The second study showed that a higher dose of MT-1 produces more darkening of the skin in response to exposure to UV-B light.

The third study showed that the drug significantly enhances tanning after exposure to natural sunlight. Specifically, people who did not take MT-1 needed 50% more sun exposure to achieve the same level of tanning. In addition, people who used the drug had tans that lasted at least three weeks longer than those achieved through sunlight alone.

The results also showed that the drug was safe to use and side effects were minor, such as nausea and temporary facial flushing.

Three 2004 Phase I clinical trials sought to establish the safety of therapy combined with UV-B light or sunlight exposure. The researchers determined, “Melanotan-1 can be safely combined with UV-B light or sunlight and appears to act synergistically in the tanning response to light.” This trial was funded by the National Cancer Institute.

A 1999 clinical dose ranging study in “eight male volunteers with ‘tannable’ skin types III-IV” given Melanotan determined that an optimal dose for ten daily subcutaneous injections is 0.16 mg/kg per day.

Clinical trials to determine efficacy of the drugs have typically used dosages up to 0.21mg/kg daily for Melanotan (16mg for a 75kg (165lb) individual), and up to 0.03mg/kg daily for Melanotan II (2.25mg for a 75kg (165lb) individual). More typically however, trials have used the dosages of 0.16mg/kg (12mg) and 0.025mg/kg (1.875mg) respectively.

Melanotan]
Melanotan II: Start with a dose of 0.25mg. If side effects (primarily nausea) are not proving troublesome, attempt to increase daily dosage by 0.25mg where possible, until you reach 1-1.5mg daily. Most have found that this level will yield a very pleasing result there is no* point in increasing too much further unless a very deep tan was desired. As with Melanotan, once the desired level of tanning is reached, a maintenance phase is used.