The Sex Drug - PT-141

_{By kblaw on pixabay.com}

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A few days ago, I encountered a Quora answer by Franklin Veaux. The question was “What is the most interesting aphrodisiac you have heard of?”.

Now, I’m personally less than convinced by aphrodisiacs, most are a scam. But Franklin introduced me to something new: PT-141 (or Bremelanotide)

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_{Bremelanotide, © Public Domain}

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To quote the effects of this complicated looking peptide:

Its effects are interesting. I’ve tried it. It takes a loooong time to work (as a subcutaneous injection, 4–6 hours; as a nasal spray, about an hour), but when it arrives, it arrives like a freight train. There’s nothing subtle about it. (Franklin Veaux)

Other user experiences reach from happy about finally being able to have sex again, after taking dosages of 2.5 to 4 mg (in combination with 25 mg Viagra)¹, to someone in his late 50s having not really the best experience upon taking a dosage of 20 mg. ²_{Hive account@suesa}

_{(Maybe it's important to make sure you're taking the correct amount? I don't know. Seems like it.)}

But … what’s really behind this drug?

The History

As it’s often the case with new drugs (Viagra was supposed to be used against high blood pressure), the original goal was not to create a powerful aphrodisiac - who would have thought?

Bremelanotide is a derivative of MT-II (Melanotan-I).³ The name might sound familiar, ever heard of melanin? That’s what makes your skin dark(er).

Melanotan-II was created to serve as a tanning agent, which would remove the need for sun exposure. Just that it didn’t work out as intended.

During initial testing of a novel synthetic agent intended for artificial tanning, Melanotan-II, a self-described “human pincushion/ guinea pig” inadvertently self-administered a dose twice the expected concentration. To his surprise, he experienced an 8 hour-long erection, along with some nausea and vomiting. ³

You’re trying to get a nice tan and end up having an 8 hour-long erection. Talk about unexpected side effects. Of course, a discovery like that couldn’t go unexplored, this could be the new Viagra after all!

A double-blind placebo-controlled crossover study by Wessells et al. tested 10 men with erectile dysfunction. They received injections of the drug (0.025 - 0.157 mg/kg body weight) and successfully achieved erections. Just as with the “human guinea pig”, side effects like nausea were reported.³.

As previously mentioned, PT-141 is a derivative of MT-II, and in phase 1 trials, it showed similar desired effects with no significant side effects. Phase II trials soon followed, with the main problem being side effects like nausea. ³

What about Women?

Do we really need another drug to give men erections? Isn’t there already enough on the market? What about women, Viagra doesn’t really help here.

Luckily, there’s a study for that!

A placebo-controlled, randomized, parallel group, dose-finding trial with 612 premenopausal female participants, to be correct. Palatin Technologies did this study in 2011/2012. Subcutaneous injections proved to have the desired effect of increasing libido, with only side effects like nausea, flushing, and headache. ^{4, 5}

But wait, how did we get from a nasal spray to subcutaneous injections? These are certainly a lot more uncomfortable, why switch?

Because in 2008, there had been concerns that the drug might raise blood pressure, which can be dangerous (especially if you already have elevated blood pressure). They switched to a different method, and in 2014, Palatin conducted a human phase 3 study using only subcutaneous delivery, with no real effect on blood pressure detectable.⁶. Good news for people with high blood pressure, bad news for those with a fear of needles.

Outlook

As of right now, bremelanotide is not FDA-approved, even though it’s being used in research to treat hypoactive sexual desire disorder⁷ (what a name …).

In June 2018, the FDA issued an acceptance letter to continue testing the drug for possible future approval. At that point, there had been 30 clinical trials with over 2,500 women. ⁸

While not intended for human consumption, bremelanotide can be ordered for relatively cheap through peptide-producing companies. ^8,9

What do you think? Would you try this peptide as medication, once it’s approved? Would you want to try it before it’s approved? Do you see ethical problems with it? After all, it might be used as a date-rape drug. Then again, the delivery options are not exactly ideal for that to happen …

I’m looking forward to hearing your opinions!

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Sources:

¹ PT-141: A Seemingly Fast and Effective Solution to the Flatline, Dead Dick, Lost Libido, and Trouble Rewiring.

²World of Peptides.com - My experience with PT-141 (Bremelanotide)

³King et al. (2009), “Melanocortin Receptors, Melanotropic Peptides and Penile Erection, Curr Top Med Chem

⁴Palatin Technologies (2014), “Bremelanotide in Premenopausal Women With Female Sexual Arousal Disorder and/or Hypoactive Sexual Desire Disorder”, ClinicalTrials.gov

⁵Claytin et al. (2016), “Bremelanotide for Female Sexual Dysfunctions in Premenopausal Women: A Randomized, Placebo-Controlled Dose-Finding Trial”, Sage journals

⁶New Drug Approvals.org - Female Libido Enhancer - Bremelanotide (2015)

⁷Bremelanotide Approval Status

⁸ Peptide Sciences

⁹UK-Peptides.com

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_{Signature by Hive account@atopy}