Bremelanotide

Overall Health Benefits of Bremelanotide

• Improves sexual health [1-28]
• Promotes weight loss [29-33]
• Improves cognitive health [34-43]
• Improves blood sugar levels [44-46]
• Improves lipid profile [47]
• Improves mood and energy levels [48-50]
• Improves eye health [51-53]
• Treats alcohol addiction [54-56]
• Boosts immune function [57-62]

What is 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 receptors. It is given by subcutaneous injection (under the skin) using a single use autoinjector pen. Scientific studies report that the administration of this peptide has shown promise in various aspects of health.

How Bremelanotide Works?

As a melanocortin receptor agonist, bremelanotide helps activate a type of protein known as melanocortin receptors. These receptors are involved in wide range of brain activities such as sexual arousal, mood, appetite, and thinking.

Chemical Structure of Bremelanotide

Research on Bremelanotide

Improves Sexual Health

Sexual dysfunction often affects one’s self-confidence and relationship with a 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:

1. 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]
2. 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]
3. 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]
4. In clinical trials, administration of bremelanotide in healthy women showed increased vaginal blood flow as well as increased sexual desire and arousal. [6-8]
5. Administration of bremelanotide to normal men and patients with erectile dysfunction (ED) resulted in a rapid dose-dependent increase in erectile activity. [9]
6. In healthy male subjects and patients with an inadequate response to Viagra, bremelanotide administration at doses greater than 1 mg resulted in a statistically significant erectile response. [10-11]
7. 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]
8. Co-administration of sildenafil and 7.5mg intranasal bremelanotide has been shown to induce significantly prolonged time of penile erections compared with sildenafil alone. [13]
9. 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 on the International Index of Erectile Function (IIEF-5) Questionnaire. [14]
10. A study found that bremelanotide’s effect on penile erection can be compared to standard drugs for ED. [15]
11. In women with hypoactive sexual desire disorder who received bremelanotide, increased feelings of sexual desire, physical arousal, significant reductions in distress related to low sexual desire, and improvements in the overall quality of their sexual activities in their partner relationship were observed. [16-25]
12. In patients who self-administered bremelanotide 1.75 mg subcutaneously using an autoinjector, as needed, before sexual activity for 24 weeks, significant improvements in sexual desire and reduced distress were evident. [26]
13. In women with female sexual arousal disorder, a single intranasal dose of 20 mg bremelanotide was associated with moderate or high sexual desire compared with placebo treatment. [27]
14. In rats, the stimulation of melanocortin receptors by bremelanotide was associated with increased penile erections. [28]

Promotes Weight Loss

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

1. In the 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%). [29]
2. In rodent models, melanocortin receptor agonists have been shown by several investigators to decrease food intake and body weight. [30-31]
3. In patients who are on chronic steroid therapy, bremelanotide counteracted steroid-induced weight gain. [32]
4. In overweight premenopausal women, a significantly greater reduction of mean body weight occurred in subjects who received bremelanotide twice a day compared to subjects who received placebo treatment. [33]

Improves 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:

1. Studies show that melanocortin receptor agonists interact with brain chemicals that regulate socioemotional behaviors and cognitive skills, including oxytocin, dopamine, serotonin, and corticotropin-releasing factor. [34-37]
2. In rodents, melanocortin receptor agonists improved general cognitive processes, including social information processing and social reinforcement. [38-43]

Improves Blood Sugar Levels

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

1. Studies show that melanocortin receptor agonists improve the body’s response to the effects of insulin (insulin sensitivity), thus lowering elevated blood sugar levels. [44-45]
2. In murine models of obesity and type 2 diabetes, melanocortin receptor agonists significantly improved blood sugar tolerance and reduced blood levels of insulin. [46]

Improves Lipid Profile

There is also evidence that melanocortin receptor agonists such as bremelanotide may help correct abnormal lipid levels:

1. 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. [47]

Improves Mood and Energy Levels

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:

1. A study found that bremelanotide exerts its antidepressant and anti-anxiety effects by improving the function of the central nervous system, resulting in improved overall mood. [48]
2. Studies show that melanocortin receptor agonists play a critical role in the regulation of food intake and energy expenditure, primarily through the regulation of the activity of the sympathetic nervous system. [49-50]

Improves 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 help preserve eye health:

1. In mice, melanocortin receptor agonists counteracted the harmful effects of high blood sugar levels on the eyes. [51]
2. In murine models, melanocortin receptor agonists protected the retinal vascular network by inhibiting local inflammatory and immune responses. [52-53]

Treats 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:

1. In binge-like ethanol drinking mice, the administration of a melanocortin receptor agonist reduced voluntary ethanol drinking by signaling through the Melanocortin 4 receptor (MC4R). [54]
2. In a mouse model of binge ethanol drinking, the administration of a melanocortin receptor agonist improved the effectiveness of naltrexone, a medication that reduces alcohol consumption. [55]
3. In mice with alcohol addiction, the administration of a melanocortin receptor agonist significantly reduced ethanol drinking. [56]

Boosts Immune Function

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

1. Studies found that melanocortin receptor agonists enhance the activities of the cells of the immune system, including neutrophils, monocytes, dendritic cells, B-lymphocytes, and white blood cells. [57-59]
2. Studies also support the potent anti-inflammatory effects of melanocortin receptor agonists, making them beneficial for inflammatory conditions. [58-62]

Associated Side Effects of Bremelanotide

Bremelanotide side effects are very uncommon. There have been some side effects associated with the use of this drug wherein the patient had one of the issues listed below at some point while being on bremelanotide. However, these side effects weren’t confirmed to be associated with the treatment and could have been a coincidence and not related to the use of bremelanotide. Despite this, it was listed as a side effect associated with bremelanotide even though these associated side effects are very uncommon.

Side effects associated with bremelanotide may include the following:

• Facial flushing
• Headache
• Hyperpigmentation
• Increase in blood pressure
• Joint stiffness
• Nausea
• Vomiting

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