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Bremelanotide (formerly PT-141) is the generic term for a new medication that has been tested with rats and is currently proposed as useful in treating some aspects of sexual dysfunction in some men (erectile dysfunction or impotence) as well as possible sexual dysfunctions in some women (sexual arousal disorder). The promoters think of it as a synthetic aphrodisiac, but doubt has been cast on this category in general and there is no reliable evidence for the existence of this class of chemicals. Unlike Viagra and other related medications, Bremelanotide does not act upon the vascular system, but is alleged to affect the central nervous system, raising new questions about safety and efficacy. Side effects, long term effects, and efficacy in different populations are all open to question and further study at the moment. Bremelanotide is being tested not as a pill or injection, but as a nasal spray.
The manufacturers have said that originally, the peptide Melanotan II that bremelanotide was developed from was tested as a sunless tanning agent. In initial testing, they report, Melanotan II did induce tanning but additionally caused sexual arousal and spontaneous erections as unexpected side effects in eight out of the ten original male volunteer test subjects. Further information about the subjective aspects of the response or the long term impact is missing. In unpublished clinical studies that the manufacturer reports through press releases and at non-peer-reviewed conferences, bremelanotide has been shown to be effective in treating male sexual and erectile dysfunction as well as female sexual dysfunction in highly selected participants. It is currently being tested by Palatin Technologies who have not offered any indication of how they plan to market this product and prevent its abuse.
Bremelanotide is a cyclic hepta-peptide lactam analog of alpha-melanocyte-stimulating hormone (alpha-MSH) that activates the melanocortin receptors MC3-R and MC4-R in the central nervous system. It has the amino acid sequence Ac-Nle-cyclo-OH or cyclo-alpha-MSH-(4-10). PT-141 is a metabolite of Melanotan II that lacks the C-terminal amide function. Its molecular forumla is C50H68N14O10 with a molecular weight of 1025.2.
In the United States it is currently in a Phase III clinical trial. The utlimate usefulness of this drug cannot be predicted at the moment, since it has not been approved by the U.S. or any other government, nor is approval scheduled. The drug has received widespread publicity, indicating the strength of the public relations available to the manufacturer.
External links
- Palatin Technologies The company that has developed bremelanotide.
- US 6,794,489 bremelanotide (PT-141) patent (Appl. No.:040547)
- US 6,579,968 bremelanotide (PT-141) patent (Appl. No.:066501)
- Melanotan.org
- Proc. Nat. Acad. Sci 101: 10201 (2004) A scientific study with female rats.
- Review article (in German).
- The June 2006 release of The Bremelanotide Bulletin summarized Phase IIa test results for women, which indicated significantly increased sexual desire and arousal (67% and 72% respectively) in women diagnosed with female sexual arousal disorder.
- Norman Levine, MD; researcherss on Melanotan at University of Arizona Dermatology
- PT-141 fact sheet (PDF; cached HTML version is here)