PT-141 | Reviews, Dosage, and Clinical Trials

PT-141 (bremelanotide) is an FDA-approved treatment of low sexual desire in women, and is also known to treat sexual arousal disorder in men.

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    Compound Overview

    Class of Compound:

    Peptide

    Mechanism of Action:

    PT-141 is an agonist of the melanocortin receptors, with high affinity for MC4R, the stimulation of which increases sexual desire and causes sexual arousal in both men and women

    Notable Studies:

    Also Known As:

    Bremelanotide, bremelanotide acetate, Rekynda, Vyleesi, CID9941379

    Research Applications:

    • Sexual funtion
    • Male sexual arousal
    • Anti-inflammatory action

    Risks:

    • Injection-related side effects
    • Temporarily increases blood pressure
    • Not FDA approved to treat men.

    Chemical Structure

    Bremelanotide-structure

    What is PT-141?

    PT-141, also known as bremelanotide, is an FDA-approved treatment of hypoactive sexual desire disorder (HSDD) in women [1]. It is a modified synthetic derivative of alpha-melanocyte-stimulating hormone (α-MSH), a peptide of the melanocortin family that regulates skin pigmentation, feeding behavior, and sexual activity, among its other functions.

    Back in the 1960s, researchers found that α-MSH caused caused sexual arousal when administered to rats, which eventually led to the development of α-MSH analogues like PT-141, melanotan I, and melanotan II.

    In 2019, bremelanotide (PT-141) was approved in the United States as a therapy for premenopausal women with HSDD [2], and it is currently available under the brand name Vyleesi in auto-injection pens [3]. The manufacture and commercialization of Vyleesi in the United States are conducted by Palatin Technologies, the company that originally developed the drug [4, 5].

    In addition to its role in treating HSDD in women, PT-141 has been extensively studied in a variety of contexts, including for its roles in treating erectile dysfunction (ED) and other forms of sexual dysfunction.

    PT-141

    What Does PT-141 Do?

    As an analogue of α-MSH, PT-141 acts on the melanocortin receptors (MCRs), which are found predominantly in the skin and central nervous system and cause an increase in pigmentation by activating melanocytes. However, MCRs are also associated with effects on sexual desire and appetite. PT-141 strongly engages MC1R, MC3R, and MC4R, the latter of which plays a role in modulating sexual desire [2].

    Following a subcutaneous injection of PT-141, maximal levels occur after about one hour, with a range of 30 minutes to one hour [6]. In the realm of male sexual desire, this translates to a virtually on-demand erection.

    PT-141 Benefits | Clinical Trials

    PT-141 that is sold online is generally available only to qualified researchers and is not intended for human testing. However, since PT-141 is another name for the FDA-approved drug bremelanotide, the documented benefits and applications of bremelanotide are identical to those of PT-141:

    Potential treatment of erectile dysfunction: While PT-141 is not indicated to treat erectile dysfunction (ED), several small-scale studies have found that it may be beneficial to male patients with ED who do not respond to sildenafil (Viagra).

    A 2003 phase 1 randomized double-blind placebo-controlled trial involving 24 healthy male subjects without erectile dysfunction found that test subjects who received intranasal doses of PT-141 (4 to 20 mg) experienced “significantly increased duration of rigid erections of 140 minutes compared to 22 minutes in the placebo group” [6].

    A 2004 study involving fewer than 400 patients found that doses of 1mg of PT-141 (bremelanotide) could produce a statistically significant “erectile response” [7].

    Based on the above results, the safety and efficacy of PT-141 in test subjects with mild to moderate ED were investigated in a phase II study. Results showed a 3-fold increase in erectile activity following 20mg intranasal administration of PT-141 [8].

    A 2008 study involving intranasal bremelanotide spray found that it could help men achieve an erection suitable for penetrative sex when administered 45 minutes prior to intercourse [9].

    These findings suggest that PT-141 may act as an alternative ED treatment for subjects who do not respond to sildenafil, a potentiality that merits further research.


    Treatment of HSDD in premenopausal women: As we have mentioned, bremelanotide is an FDA-approved treatment of low sexual desire in premenopausal women [4, 5].

    While female sexual desire is not yet fully understood, evidence suggests that estradiol, testosterone, dopamine, norepinephrine, and serotonin all play a role.

    PT-141 activates presynaptic MC4Rs on neurons and increases the amount of dopamine released [10]. Leading up to its approval, research on bremelanotide showed that premenopausal women with sexual dysfunction who were administered the peptide experienced more sexually satisfying events [11] and had less intercourse-related distress compared to placebo [12, 13].


    General sexual dysfunction treatment: According to King et al., melanocortin agonists like PT-141 have “possible applications to the unmet medical needs of decreased sexual motivation and loss of libido” [14]. The authors cited the Molinoff (2003) study, where PT-141 was found to increase the rigidity of erections in test subjects with and without ED [6]. PT-141’s ability to trigger sexual desire in both men and women, independent of sexual stimulation, suggests that it holds potential as a treatment for a variety of sexual desire disorders.

    Order PT-141 online from one of the best vendors in the world...

    PT-141 Side Effects

    At the recommended dose of 1.75 mg, bremelanotide may produce the following common side effects [2]:

    • Nausea (40% particularly with the first injection)
    • Flushing (20%)
    • Injection site reactions (13%)
    • Headaches (11%)

    Uncommon adverse reactions include [2]:

    • Increases in blood pressure
    • Severe nausea
    • Vomiting
    • Arthralgia
    • Restless leg syndrome
    • Local hyperpigmentation

    Due to the risk of the peptide causing an increase in blood pressure and reduction in heart rate, it should not be administered to subjects who are [16]:

    • Pregnant or suspected of being pregnant
    • Suffering from cardiovascular disease
    • Diagnosed with uncontrolled hypertension

    In rare instances, PT-141 may lead to elevated serum enzyme levels, and in even rarer cases, cause acute liver damage [2].

    Is PT-141 Safe?

    When administered as a treatment of low sexual desire in women, bremelanotide has a favorable safety profile, having completed phase 3 clinical trials prior its being approved for use in the United States in 2019 [15].

    In the field of male sexual desire, preliminary trials have established both the safety and efficacy of PT-141, showing that it is a potent initiator of erection with minimal side effects [14]. It must be reiterated that PT-141 is not approved to treat male sexual dysfunction at this time, and that PT-141 sold online is generally available for educational or scientific research only.

    PT-141 Dosage Calculator

    As a treatment of low sexual desire in women, bremelanotide is typically administered subcutaneously via self-injection. The most common dosage is 1.75 mg, roughly 45 minutes prior to anticipated sexual activity [2]. Patients with HSDD who are prescribed bremelanotide are advised to self-administer it no more than once per day, for a maximum of 8 times per month [13]. Those who experience adverse reactions to bremelanotide can reduce the dosage. Research has shown that doses of just 1.25 mg can still produce an effective response [11].

    Studies involving male subjects with or without ED have tested subcutaneous injections of PT-141 ranging from 1 to 10 mg, showing that PT-141 can produce statistically significant results at doses exceeding 1 mg [7] and dose-dependent improvements in erectile function at doses up to 20 mg [14]. Research suggests a starting dose of 1 mg as a treatment of erectile dysfunction.

    Where To Buy PT-141 Online

    Researchers interested in studying PT-141 may be curious about where to buy this peptide online. Having tested multiple vendors, our preferred PT-141 source is Peptide Sciences. They consistently supply research-grade PT-141 at reasonable prices with decent shipping times.

    Here are a few of the reasons why we rate them so highly.

    • Rigorous Independent Testing: When our team made test purchases from Peptide Sciences, we were impressed that they provided lab reports showing the quality of the PT-141 they offered. This level of transparency helps foster trust and sets Peptide Sciences apart from other vendors.
    • Affordable Prices: The costs of running a study involving PT-141 can quickly spiral, so Peptide Sciences’ price of just $47.50 for a 10 mg vial of PT-141 is impressive. They also offer a further 14% off on all bulk purchases (10 vials or more).
    • Impressive Customer Service: Our team was impressed by the customer service offered by Peptide Sciences. They were highly responsive to our emails and kept us in the loop at every stage of the buying process.
    • Secure Website: Peptide Sciences offers a secure, fast, website that protects customer data. We didn’t have any worries about our personal data being exposed or compromised when we ordered from this vendor.
    • Solid Shipping Policy: All U.S. orders over $200 are free, and worldwide shipping costs just $15. You won’t have any shipping headaches when you order from this vendor. As a bonus incentive, all orders exceeding $400 earn a gift of one 30ml vial of bacteriostatic water, which you’ll need to reconstitute PT-141 in powder form.

    Overall, our team rates Peptide Sciences as the top PT-141 vendor in the market today. They can supply research-grade PT-141 at reasonable prices and you won’t have to wait long for your order to arrive.

    Highly recommended!

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    FAQ

    PT-141. Just. Works.

    PT-141 is a research peptide that has been clinically proven to increase sexual desire in both animal and human studies. With a favorable safety profile, bremelanotide (PT-141) is indicated to treat low sexual desire in women in the United States. PT-141 has also been extensively tested, with promising results, as a potential treatment of erectile dysfunction.

    Researchers looking to further study PT-141 are strongly encouraged to consider Peptide Sciences — a reliable, trustworthy vendor that ships research-grade PT-141 worldwide.

    PT-141

    References

    1. National Center for Biotechnology Information (2021). PubChem Substance Record for SID 319341034, 189691-06-3, Source: ToxPlanet. Retrieved October 21, 2021 from https://pubchem.ncbi.nlm.nih.gov/substance/319341034.
    2. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Bremelanotide. 2021 Aug 20. PMID: 34436837.
    3. Dhillon S, Keam SJ. Bremelanotide: First Approval. Drugs. 2019 Sep;79(14):1599-1606. doi: 10.1007/s40265-019-01187-w. PMID: 31429064.
    4. Mayer D, Lynch SE. Bremelanotide: New Drug Approved for Treating Hypoactive Sexual Desire Disorder. Ann Pharmacother. 2020 Jul;54(7):684-690. doi: 10.1177/1060028019899152. Epub 2020 Jan 1. PMID: 31893927.
    5. Bremelanotide (Vyleesi) for hypoactive sexual desire disorder. Med Lett Drugs Ther. 2019 Jul 29;61(1577):114-116. PMID: 31381550.
    6. Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003 Jun;994:96-102. doi: 10.1111/j.1749-6632.2003.tb03167.x. PMID: 12851303.
    7. Rosen RC, Diamond LE, Earle DC, Shadiack AM, Molinoff PB. Evaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra. Int J Impot Res. 2004 Apr;16(2):135-42. doi: 10.1038/sj.ijir.3901200. PMID: 14999221.
    8. 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 Feb;16(1):51-9. doi: 10.1038/sj.ijir.3901139. PMID: 14963471.
    9. Safarinejad MR, Hosseini SY. Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study. J Urol. 2008 Mar;179(3):1066-71. doi: 10.1016/j.juro.2007.10.063. Epub 2008 Jan 18. PMID: 18206919.
    10. Pfaus JG, Sadiq A, Spana C, Clayton AH. The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women. CNS Spectr. 2021 Jan 18:1-9. doi: 10.1017/S109285292100002X. Epub ahead of print. PMID: 33455598.
    11. Clayton, A. H., Althof, S. E., Kingsberg, S., DeRogatis, L. R., Kroll, R., Goldstein, I., Kaminetsky, J., Spana, C., Lucas, J., Jordan, R., & Portman, D. J. (2016). Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial. Women's health (London, England), 12(3), 325–337. https://doi.org/10.2217/whe-2016-0018
    12. Kingsberg SA, Clayton AH, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Simon JA. Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. Obstet Gynecol. 2019 Nov;134(5):899-908. doi: 10.1097/AOG.0000000000003500. PMID: 31599840; PMCID: PMC6819021.
    13. (2021). Retrieved 10 October 2021, from https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
    14. King SH, Mayorov AV, Balse-Srinivasan P, Hruby VJ, Vanderah TW, Wessells H. Melanocortin receptors, melanotropic peptides and penile erection. Curr Top Med Chem. 2007;7(11):1098-1106. PMID: 17584130; PMCID: PMC2694735.
    15. Simon JA, Kingsberg SA, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Clayton AH. Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder. Obstet Gynecol. 2019 Nov;134(5):909-917. doi: 10.1097/AOG.0000000000003514. PMID: 31599847; PMCID: PMC6819023.
    16. Althof S, Derogatis LR, Greenberg S, Clayton AH, Jordan R, Lucas J, Spana C. Responder Analyses from a Phase 2b Dose-Ranging Study of Bremelanotide. J Sex Med. 2019 Aug;16(8):1226-1235. doi: 10.1016/j.jsxm.2019.05.012. Epub 2019 Jul 2. PMID: 31277966.