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Bremelanotide

Bremelanotide, also known as PT-141, is a powerful peptide (a compound consisting of two or more amino acids) that activates internal pathways in the brain involved in normal sexual responses. This FDA-approved drug is also a melanocortin receptor agonist, which helps activate a type of protein known as melanocortin receptor. It is given by subcutaneous injection (under the skin) using a single use autoinjector pen. Scientific studies report that administration of this peptide has shown promise in various aspects of health.

Overall Health Benefits of Bremelanotide

  • Improves Sexual Health [1-15]
  • Reverses Steroid-Induced Weight Gain [16]
  • Improves Mood [17]
  • Improves Blood Sugar Levels [18-20]
  • Improves Lipid Profile [21]
  • Increases Energy Levels [22-24]
  • Improves Eye Health [25-27]
  • Promotes Weight Loss [28-30]
  • Fights Alcohol Addiction [31-33]
  • Boosts Immune Function [34-39]
  • Improves Cognitive Health [40-48]

Sexual Health

Sexual dysfunction often affects one’s self-confidence and relationship with partner. Fortunately, this condition is very treatable with bremelanotide. In fact, the FDA approved bremelanotide in June 2019 as a therapeutic option for women with low libido after it showed an increase in sexual desire and reduction in distress in two replicate phase 3 trials involving women with hypoactive sexual desire disorder (HSDD). [1-2] It now joins flibanserin, the only other drug approved by the FDA for the treatment of HSDD in premenopausal women.

Numerous human studies have also shown promising results with regards to the therapeutic benefits of bremelanotide on sexual health:

  • In premenopausal women with sexual dysfunctions, bremelanotide self-administration at various does (0.75, 1.25 or 1.75 mg) as desired over 12 weeks, resulted in significant improvements in female sexual function index total score and female sexual distress scale-desire/arousal/orgasm total score compared to placebo. [3]
  • In female subjects with arousal disorder, administration of 20-mg bremelanotide given as an intranasal spray on “as required” basis 45–60 minutes before attempting sexual intercourse, was associated with significantly greater intercourse satisfaction compared to placebo. [4]
  • In premenopausal women with sexual arousal disorder, administration of a single intranasal dose of 20 mg bremelanotide was associated with moderate or high sexual desire and improved satisfaction with their level of sexual arousal compared to placebo treatment. [5]
  • In clinical trials, administration of bremelanotide in healthy women showed increased vaginal blood flow as well as increased sexual desire and arousal. [6-8]
  • Administration of bremelanotide to normal men and to patients with erectile dysfunction (ED) resulted in a rapid dose-dependent increase in erectile activity. [9]
  • In healthy male subjects and in patients with an inadequate response to Viagra, bremelanotide administration at doses greater than 1 mg resulted in a statistically significant erectile response. [10-11]
  • In a first Phase IIB at home study, administration of bremelanotide resulted in significant improvements in erectile function as assessed by the International Index of Erectile Function (IIEF). [12]
  • Co-administration of sildenafil and 7.5 mg intranasal bremelanotide has been shown to induce significantly prolonged time of penile erections compared with sildenafil alone. [13]
  • In a 12-week phase IIb trial recruiting 726 non-diabetic men suffering from ED, bremelanotide administration at a dose of 5 mg was associated with significantly higher scores in the International Index of Erectile Function (IIEF-5) Questionnaire. [14]
  • A study found that bremelanotide’s effect on penile erection can be compared to standard drugs for ED. [15]

Steroid Induced Weight Gain

Steroids are often extremely effective in alleviating pain and inflammation. However, this drug can affect fat metabolism, which ultimately leads to weight gain. Studies show that bremelanotide counteracts steroid induced weight gain in patients who are on chronic steroid therapy. [16]

Mood

In men and women with sexual dysfunction, low mood and depression are very common. Because of the therapeutic benefit of bremelanotide on libido and sexual performance, this powerful peptide has been studied for its mood-enhancing effect. Studies show that bremelanotide exerts its antidepressant and anti-anxiety effects by improving the function of the central nervous system, resulting in improved overall mood. [17]

Blood Sugar

Studies show that melanocortin receptor agonists help protect against diabetes and the negative effects of high blood sugar through the following mechanisms:

  • By improving the body’s response to the effects of insulin (insulin sensitivity). [18-19]
  • In murine models of obesity and type 2 diabetes, melanocortin receptor agonists significantly improve blood sugar tolerance and reduce blood levels of insulin. [20]

Abnormal Lipid Profile

There is also evidence that melanocortin receptor agonists such as bremelanotide may help correct abnormal lipid levels. In streptozotocin-induced diabetic mice, injection of melanocortin receptor agonist reduces fat formation in the liver, thereby improving abnormal lipid metabolism associated with insulin-deficiency. [21]

Energy Levels

Melanocortin receptor agonists such as bremelanotide may help increase energy levels as well as productivity. Studies show that melanocortin receptor agonists play a critical role in the regulation of food intake and energy expenditure, primarily through regulation of the activity of the sympathetic nervous system. [22-24]

Eye Health

Photoreceptor cell, a specialized type of neuron found in the retina, is particularly vulnerable to high blood sugar levels. Studies show that melanocortin receptor agonists helps preserve eye health by:

  • In mice, it counteracts the harmful effects of high blood sugar levels on the eyes. [25]
  • In murine models, it protects retinal vascular network by inhibiting local inflammatory and immune responses. [26-27]

Weight Loss

Studies show that the melanocortin receptor agonist bremelanotide may also help improve body composition by inducing weight loss:

  • In obese nonhuman primate model, treatment with melanocortin receptor agonist decreased food intake by 35%, with persistent weight loss over 8 weeks of treatment (13.5%). [28]
  • In rodent models, melanocortin receptor agonists have been shown by several investigators to decrease food intake and body weight. [29-30]

Alcohol Addiction

Recent data have implicated that melanocortin receptor agonists such as bremelanotide may play a role in modulating voluntary ethanol (alcohol) consumption, thereby treating alcohol addiction. In mice, melanocortin receptor agonist administration effectively reduces ethanol drinking, suggesting that it can be a potential therapeutic option for alcohol abuse disorders. [31-33]

Immune Function

Melanocortin receptor agonists such as bremelanotide play a crucial role in strengthening the immune system. Studies show that melanocortin receptor agonists exert its immune boosting effects through the following important mechanisms:

  • It enhances the activities of the cells of the immune system, including neutrophils, monocytes, dendritic cells, B-lymphocytes, and white blood cells. [34-36]
  • It has potent anti-inflammatory effect. [37-39]

Cognitive Health

There is increasing evidence that bremelanotide along with other melanocortin receptor agonists may help improve cognitive health. Studies show that they exert this effect through the following mechanisms:

  • Melanocortin receptor agonists interact with brain chemicals that regulate socioemotional behaviors and cognitive skills, including oxytocin, dopamine, serotonin, and corticotropin-releasing factor. [40-43]
  • In rodents, melanocortin receptor agonists improve general cognitive processes, including social information processing and social reinforcement. [44-48]
  • Available from https://www.wptv.com/news/national/fda-approves-new-drug-for-women-with-low-sexual-desire-disorder.
  • Available from https://www.medscape.com/viewarticle/914779.
  • Clayton AH, Althof SE, Kingsberg S, et al. Bremelanotide for Female Sexual Dysfunctions in Premenopausal Women: A Randomized, Placebo-Controlled Dose-Finding Trial. Women’s Health. 2016;12(3):325-337. doi:10.2217/whe-2016-0018. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5384512/.
  • 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. The journal of sexual medicine. 2008; 5(4):887-97. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/18179455,
  • Diamond LE, Earle DC, Heiman JR, Rosen RC, Perelman MA, Harning R. An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist. The journal of sexual medicine. 2006; 3(4):628-638. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/16839319.
  • Allahdadi KJ, Tostes RCA, Webb RC. Female Sexual Dysfunction: Therapeutic Options and Experimental Challenges. Cardiovascular & hematological agents in medicinal chemistry. 2009;7(4):260-269. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3008577/#!po=60.4167.
  • Brown AD, Blagg J, Reynolds DS. Designing drugs for the treatment of female sexual dysfunction. Drug discovery today. 2007; 12(17-18):757-66. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/17826689.
  • Retrieved from https://www.palatin.com/research-focus/female-sexual-dysfunction/phase-3-reconnect-studies/.
  • Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Annals of the New York Academy of Sciences. 2003; 994:96-102. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/12851303.
  • 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. International journal of impotence research. 2004; 16(2):135-42. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/14999221.
  • Safarinejad MR, Hosseini SY. Salvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study. The Journal of urology. 2008; 179(3):1066-71. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/18206919.
  • King SH, Mayorov AV, Balse-Srinivasan P, Hruby VJ, Vanderah TW, Wessells H. Melanocortin Receptors, Melanotropic Peptides and Penile Erection. Current topics in medicinal chemistry. 2007;7(11):1098-1106. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2694735/.
  • Shadiack AM, Sharma SD, Earle DC, Spana C, Hallam TJ. Melanocortins in the treatment of male and female sexual dysfunction. Curr Top Med Chem. 2007;7(11):1137-44. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/17584134.
  • Diamond LE, et al. Co-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response. Urology. 2005;65(4):755–9. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/15833522.
  • Albersen M, Shindel A, Mwamukonda K, Lue T. The future is today: emerging drugs for the treatment of erectile dysfunction. Expert opinion on emerging drugs. 2010;15(3):467-480.
  • doi:10.1517/14728214.2010.480973. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3163612/.</li>

  • Retrieved from https://docs.google.com/viewer?url=patentimages.storage.googleapis.com/pdfs/US20050101535.pdf.
  • Retrieved from http://www.ingentaconnect.com/content/ben/ctmc/2007/00000007/00000011/art00008.
  • Toda C, Shiuchi T, Lee S, et al. Distinct Effects of Leptin and a Melanocortin Receptor Agonist Injected Into Medial Hypothalamic Nuclei on Glucose Uptake in Peripheral Tissues. Diabetes. 2009;58(12):2757-2765. doi:10.2337/db09-0638. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2780865/.
  • Kumar KG, Sutton GM, Dong JZ. Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice. Peptides. 2009; 30(10):1892-900. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/19646498.
  • Zhou L, Sutton GM, Rochford JJ, et al. Serotonin 2C Receptor Agonists Improve Type 2 Diabetes via Melanocortin-4 Receptor Signaling Pathways. Cell Metabolism. 2007;6(5):398-405. doi:10.1016/j.cmet.2007.10.008. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/17983585.
  • Leckstrom A, Lew PS, Poritsanos NJ, Mizuno TM. Central melanocortin receptor agonist reduces hepatic lipogenic gene expression in streptozotocin-induced diabetic mice. Life sciences. 2011; 88(15-16):664-9. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/21315740.
  • Hall JE, Hildebrandt DA, Kuo J. Obesity hypertension: role of leptin and sympathetic nervous system. American journal of hypertension. 2001; 14(6 Pt 2):103S-115S. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/11411745.
  • Nogueiras R, Wiedmer P, Perez-Tilve D, et al. The central melanocortin system directly controls peripheral lipid metabolism. The Journal of Clinical Investigation. 2007;117(11):3475-3488. doi:10.1172/JCI31743. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1978426/.
  • Obici S, Feng Z, Tan J, Liu L, Karkanias G, Rossetti L. Central melanocortin receptors regulate insulin action. Journal of Clinical Investigation. 2001;108(7):1079-1085. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC200952/.
  • Maisto R, Gesualdo C, Trotta MC. Melanocortin receptor agonists MCR1-5 protect photoreceptors from high-glucose damage and restore antioxidant enzymes in primary retinal cell culture. Journal of cellular and molecular medicine. 2017; 21(5):968-974. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/27998021.
  • Rossi S, Maisto R, Gesualdo C, et al. Activation of melanocortin receptors MC1 and MC5 attenuates retinal damage in experimental diabetic retinopathy. Mediators Inflamm. 2016; 7368389. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/26949291.
  • Wolf Horrell EM, Boulanger MC, D’Orazio JA. Melanocortin 1 receptor: structure, function, and regulation. Front Genet. 2016; 7: 95. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/27303435.
  • Kievit P, Halem H, Marks DL. Chronic treatment with a melanocortin-4 receptor agonist causes weight loss, reduces insulin resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013; 62(2):490-7. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/23048186.
  • Emmerson PJ, Fisher MJ, Yan LZ, Mayer JP. Melanocortin-4 receptor agonists for the treatment of obesity. Current topics in medicinal chemistry. 2007; 7(11):1121-30. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/17584132.
  • Jonsson L, Skarphedinsson JO, Skuladottir GV. Melanocortin receptor agonist transiently increases oxygen consumption in rats. Neuroreport. 2001; 12(17):3703-8. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/11726778.
  • Olney JJ, Sprow GM, Navarro M, Thiele TE. The protective effects of the melanocortin receptor (MCR) agonist, melanotan-II (MTII), against binge-like ethanol drinking are facilitated by deletion of the MC3 receptor in mice. Neuropeptides. 2014;48(1):47-51. doi:10.1016/j.npep.2013.11.001. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3946855/.
  • Navarro M, Carvajal F, Lerma-Cabrera JM, Cubero I, Picker MJ, Thiele TE. Evidence that Melanocortin Receptor Agonist Melanotan-II Synergistically Augments the Ability of Naltrexone to Blunt Binge-Like Ethanol Intake in Male C57BL/6J Mice. Alcoholism, clinical and experimental research. 2015;39(8):1425-1433. doi:10.1111/acer.12774. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4515169.
  • Navarro M, Cubero I, Chen AS, et al. Effects of Melanocortin Receptor Activation and Blockade on Ethanol Intake: A Possible Role for the Melanocortin-4 Receptor. Alcoholism, clinical and experimental research. 2005;29(6):949-957. doi:10.1097/01.ALC.0000167740.19702.8C. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1360238/.
  • Catania A. The melanocortin system in leukocyte biology. Journal of leukocyte biology. 2007; 81(2):383-92. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/17041004.
  • Getting SJ, Flower RJ, Perretti M. Agonism at melanocortin receptor type 3 on macrophages inhibits neutrophil influx. Inflammation research : official journal of the European Histamine Research Society … [et al.]. 1999; 48 Suppl 2:S140-1. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/10667854.
  • Getting SJ, Gibbs L, Clark AJ, Flower RJ, Perretti M. POMC gene-derived peptides activate melanocortin type 3 receptor on murine macrophages, suppress cytokine release, and inhibit neutrophil migration in acute experimental inflammation. Journal of immunology (Baltimore, Md. : 1950). 1999; 162(12):7446-53. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/10358199.
  • Getting SJ, Lam CW, Leoni G, Gavins FN, Grieco P, Perretti M. [D-Trp8]-gamma-melanocyte-stimulating hormone exhibits anti-inflammatory efficacy in mice bearing a nonfunctional MC1R (recessive yellow e/e mouse). Molecular pharmacology. 2006; 70(6):1850-5. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/16959942.
  • Leoni G, Patel HB, Sampaio AL. Inflamed phenotype of the mesenteric microcirculation of melanocortin type 3 receptor-null mice after ischemia-reperfusion. FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 2008; 22(12):4228-38. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/18757499.
  • Getting SJ, Riffo-Vasquez Y, Pitchford S. A role for MC3R in modulating lung inflammation. Pulmonary pharmacology & therapeutics. 2008; 21(6):866-73. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/18992358.
  • Heisler LK, Cowley MA, Kishi T. Central serotonin and melanocortin pathways regulating energy homeostasis. Annals of the New York Academy of Sciences. 2003; 994:169-74. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/12851313.
  • Lindblom J, Opmane B, Mutulis F. The MC4 receptor mediates alpha-MSH induced release of nucleus accumbens dopamine. Neuroreport. 2001; 12(10):2155-8. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/11447325.
  • Lu XY, Barsh GS, Akil H, Watson SJ. Interaction between alpha-melanocyte-stimulating hormone and corticotropin-releasing hormone in the regulation of feeding and hypothalamo-pituitary-adrenal responses. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2003; 23(21):7863-72. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/12944516.
  • Sabatier N, Caquineau C, Dayanithi G. Alpha-melanocyte-stimulating hormone stimulates oxytocin release from the dendrites of hypothalamic neurons while inhibiting oxytocin release from their terminals in the neurohypophysis. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2003; 23(32):10351-8. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/14614094.
  • Modi ME, Inoue K, Barrett CE, et al. Melanocortin Receptor Agonists Facilitate Oxytocin-Dependent Partner Preference Formation in the Prairie Vole. Neuropsychopharmacology. 2015;40(8):1856-1865. doi:10.1038/npp.2015.35. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4839509.
  • Barrett CE, Modi ME, Zhang BC, Walum H, Inoue K, Young LJ. Neonatal melanocortin receptor agonist treatment reduces play fighting and promotes adult attachment in prairie voles in a sex-dependent manner. Neuropharmacology. 2014; 85:357-66. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/24923239.
  • Liu Y, Wang ZX. Nucleus accumbens oxytocin and dopamine interact to regulate pair bond formation in female prairie voles. Neuroscience. 2003; 121(3):537-44. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/14568015.
  • Ross HE, Young LJ. Oxytocin and the neural mechanisms regulating social cognition and affiliative behavior. Frontiers in neuroendocrinology. 2009; 30(4):534-47. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/19481567.
  • Modi ME, Young LJ. D-cycloserine facilitates socially reinforced learning in an animal model relevant to autism spectrum disorders. Biological psychiatry. 2011; 70(3):298-304. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/21481844.

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