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Author Topic: PT-141 Bremelanotide  (Read 3571 times)

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LWillisjr

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Re: PT-141 Bremelanotide
« Reply #5 on: April 28, 2012, 08:14:25 PM »

subcutaneous - Lying under the skin, as tissue.

A different way of saying it is delivered by injection.
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james1947

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Re: PT-141 Bremelanotide
« Reply #4 on: April 28, 2012, 07:13:48 PM »

I would like to renew the discussion regarding PT-141 Bremelanotide.

From google search I find from Wiki:
Quote
Bremelanotide was developed from the peptide Melanotan II which underwent testing as a sunless tanning agent. In initial testing, Melanotan II did induce tanning but additionally caused sexual arousal and spontaneous erections as unexpected side effects in nine out of the ten original male volunteer test subjects.[4]
 
In studies, bremelanotide was shown to induce lordosis in an animal model[5] and was also effective in treating sexual dysfunction in both men (erectile dysfunction or impotence) and women (sexual arousal disorder). Unlike Viagra and other related medications, it does not act upon the vascular system, but directly increases sexual desire via the nervous system.[6]
 
A Phase III clinical trial was scheduled to begin in the first half of 2007, but was delayed until August 2007. On August 30, Palatin announced that the U.S. Food and Drug Administration had expressed serious concerns regarding the risk/benefit ratio of bremelanotide with regards to the side effect of increased blood pressure. The FDA stated that they would consider alternate uses for bremelanotide, including as a treatment for individuals who do not respond to more established ED treatments. However, On May 13, 2008, Palatin Technologies announced it had "discontinued development of Bremelanotide for the treatment of male and female sexual dysfunction" while concurrently announcing plans to develop it as a treatment for hemorrhagic shock instead.[7] The company additionally announced intentions to focus its attention on another compound, PL-6983, that causes lower blood pressure in animal models.[8] Palatin has since re-initiated Bremelanotide studies for ED and FSD using a subcutaneous delivery method. On August 12, 2009, the company announced that in a double-blind study of 54 volunteers bremelanotide failed to evoke the hypertensive side effects seen with the nasal delivery system used in prior studies, concluding that "variability of uptake" inherent in intranasal administration of the drug resulted in "increases in blood pressure and gastrointestinal events...primarily related to high plasma levels in [only] a subset of patients" and that subcutaneous administration of the drug circumvented the potential for this side effect.[8]
As of March, 2012, Palatin is conducting a human Phase 2B study[3] using a new subcutaneous drug delivery system that appears to have little effect on blood pressure.


Have some additional articles on the web, but this is the most concentrated and up to date.
It sounds promissing to me for ED treatment

I have a question (I am not so good in English):
What is "subcutaneous administration"?

James
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Tim468

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Re: PT-141 Bremelanotide
« Reply #3 on: July 26, 2010, 01:38:03 PM »

""In studies, bremelanotide was shown to induce lordosis ""

Hmmmm... If your partner likes it from behind, this may make it easier...

Tim
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newguy

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Re: PT-141 Bremelanotide
« Reply #2 on: June 17, 2010, 10:22:05 PM »

http://en.wikipedia.org/wiki/Bremelanotide

Quote
Bremelanotide (pronounced /ˌbrɛmɨˈlænətaɪd/ ( listen)) (formerly PT-141) is a compound under drug development by Palatin Technologies as a treatment for hemorrhagic shock and reperfusion injury. It functions by activating the melanocortin receptors MC1R and MC4R, to modulate inflammation and limiting ischemia.[1] It was originally developed for use in treating sexual dysfunction but this application was temporarily discontinued in 2008, after concerns were raised over adverse side effects of increased blood pressure. Currently, Palatin is in negotiations with the FDA to resume Human Phase 2 studies using a new subcutaneous drug delivery system that appears to have little effect on blood pressure.

The modulating inflammation part is interesting.

Quote
In studies, bremelanotide was shown to induce lordosis in an animal model[3] and was also effective in treating sexual dysfunction in both men (erectile dysfunction or impotence) and women (sexual arousal disorder). Unlike Viagra and other related medications, it does not act upon the vascular system, but directly increases sexual desire via the nervous system

As is the fact that it appear to be very different to viagra and co. In this study in was useful for some men, even when PDE5 inhibitors brought no response: http://www.ncbi.nlm.nih.gov/pubmed/18206919 For some men with peyronie's disease, ED is a significant aspect, on occasionally dictating the treatment they go on to receive. It will be interesting to see if this is of any use to those men. Perhaps it depends to some extent on to what extent their ED is mental or physical.
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MedStudent86

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PT-141 Bremelanotide
« Reply #1 on: June 17, 2010, 04:03:38 PM »

I am a bodybuilder, and new to the forum. I don't personally have Erectile Dysfunction problems, however I keep abreast of various chemicals which are useful in treating temporary ED caused by the use of certain lifting supplements. There are a number of drugs that you can purchase legally for "research purposes." They will be labeled not for human consumption, but they are of course safe to use. One interesting drug, which is not a traditional PDE5 inhibitor, is PT-141 or Bremelanotide. It not only induces erections, but also increases SEXUAL DESIRE as well. It's a pretty awesome drug, and I believe its currently in Stage III clinical trials with Paladin Pharmaceuticals out of New Jersey. Below is information I took from the research chemical website, I'll also post a link to it if anyone is interested in buying some and trying it out.

http://www.ar-r.com/research-chemicals/pde5-inhibitors/ipt-141-10mg.html


PT-141 (bremelanotide) is an experimental drug used for the purpose of sexual arousal. It is a melanocortin based peptide that has shown effectiveness in clinical studies on both male and female rats. Male rats have shown erectile response with doses as low as 1-2 mgs whereas most female rats have shown positive results with higher doses around 2-3 mgs. While the dosage requirements tend to be higher for female rats, the observable results in female rats tend to be stronger. An example of findings among male rats is displayed below in an abstract from this Palatin study:

PT-141, a cyclic heptapeptide melanocortin analog, was evaluated following intranasal administration in healthy male rats and in Viagra-responsive erectile dysfunction (ED) rats. Erectile response was assessed by RigiScan in healthy subjects without visual sexual stimulation (VSS) and in Viagra((R))-responsive ED patients with VSS. In healthy subjects, mean C(max) and AUC((0-t)) increased in a dose-dependent manner. Median T(max) was 0.50 h and mean t(1/2) ranged from 1.85 to 2.09 h. In both studies, an erectile response induced by PT-141 administration was statistically significant, compared to placebo, at doses greater than 7 mg, with the onset of the first erection occurring in approximately 30 min. PT-141 was safely administered and well tolerated in both studies. A maximum-tolerated dose was not identified. Flushing and nausea were the most common adverse events reported in both studies and no clinically significant changes in vital signs, laboratory tests, ECGs, or physical exams were observed.

Female rat responses can be seen here in this research abstract:

To review the effects of bremelanotide, an analogue of the naturally occurring peptide alpha-MSH, on the preclinical indices of sexual desire in female rats, and where in the brain these actions may occur. MAIN OUTCOME MEASURES: Appetitive sexual behaviors, such as solicitations, hops and darts, and pacing, were assessed along with consummatory behaviors such as lordosis. The involvement of brain regions was assessed following direct administration to the region, by the stimulation of molecular markers of neural activation, and using microdialysis to examine extracellular fluid for different neurotransmitters. METHODS: Using a model that allows ovariectomized, hormone-primed female rats to control the timing of sexual encounters with males, tested the ability of bremelanotide to increase appetitive (proceptive) and/or consummatory sexual behaviors. RESULTS: Bremelanotide dramatically and selectively increased measures of solicitation in female rats, without altering pacing or lordosis, following both peripheral (subcutaneous) administration or infusions directly into the lateral ventricles or medial preoptic area (mPOA), but not the ventromedial hypothalamus. The mPOA is critical for the display of appetitive sexual behaviors in females and males of a variety of species. Peripheral administration of bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior, and may work by activating dopamine terminals in the mPOA. CONCLUSIONS: To the extent that solicitations indicate the desire of female rats to engage in sexual activity, bremelanotide appears to possess the behavioral, pharmacological, and neuroanatomical specificity required of a drug in the treatment of hypoactive sexual desire disorders.

All research materials are USP grade materials. All materials sold on this site are sold for research purposes only.



Other great info on this product:
http://www.ncbi.nlm.nih.gov/pubmed/17958619?ordinalpos=5&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_DefaultReportPanel.Pubmed_RVDocSum

http://www.benthamdirect.org/pages/b_viewarticle.php

http://www3.interscience.wiley.com/journal/118592979/abstract

http://www3.interscience.wiley.com/journal/118592979/abstract

http://www.sciencebase.com/science-blog/libido-nasal-spray.html

http://nymag.com/lifestyle/sex/annual/2005/15061/

http://www.guardian.co.uk/science/2006/apr/23/medicineandhealth.observermagazine

References:
Diamond LE, Earle DC, Rosen RC, Willett MS, Molinoff PB. Double-blind, placebo-controlled evaluation of the safety, pharmacokinetic properties and pharmacodynamic effects of intranasal PT-141, a melanocortin receptor agonist, in healthy males and patients with mild-to-moderate erectile dysfunction, Int J Impot Res. 2004 Jan;16(1):51-9

Safarinejad MR., Evaluation of the safety and efficacy of bremelanotide, a melanocortin receptor agonist, in female subjects with arousal disorder: a double-blind placebo-controlled, fixed dose, randomized study., J Sex Med. 2008 Apr;5(4):887-97. Epub 2007 Dec 28.
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