PT-141
Bremelanotide, a melanocortin receptor agonist specialized for sexual response
In 2019, the FDA approved bremelanotide (PT-141) for low sexual desire disorder in women, after two phase 3 trials in 1,267 women.
It activates the MC4R receptor in the hypothalamus and modulates dopamine in the motivation circuits: it acts on desire in the brain, not on blood flow like sildenafil.
Designed for sexual response, it has also been studied in men in phase 2 for erection and desire (Diamond, 2004).
- Half-life
- About three hours; the effect appears within the hour and lasts several hours.
- Route
- Subcutaneous injection, on demand, ahead of a chosen moment.
Technical sheet
- Family
- Bremelanotide, a melanocortin receptor agonist specialized for sexual response
- Half-life
- About three hours; the effect appears within the hour and lasts several hours.
- Route
- Subcutaneous injection, on demand, ahead of a chosen moment.
- Time to effect
- Thirty minutes to two hours after injection, depending on the person.
- Level of evidence
- Documented in humans
Chemical identity
- Chemical name
- Brémélanotide
- Form
- Synthetic peptide, values for the base form
- CAS No.
- 189691-06-3
Salt form: as stated on the lot's certificate of analysis.
MC4R, a hypothalamic receptor
PT-141 activates, in the hypothalamus, the MC4R (and MC3R) melanocortin receptors. It thus modulates dopamine in the motivation and pleasure circuits, and lowers the threshold for arousal, independent of direct stimulation.
In women as in men
It was the first molecule successfully studied for hypoactive sexual desire disorder in premenopausal women. In men, it has also been studied where the vascular route isn't enough.
Desire, without the tan
Designed to act mainly on the brain, it is not made for tanning, but frequent use can darken the skin in patches. It keeps part of the effect on appetite and the same tendency toward nausea at the start.
Effects and realistic timelines
Sexual desire: a significant increase versus placebo in the RECONNECT trials
Thirty minutes to two hours
Sexual response, in women as in men: greater erectile response in phase 2
Hours
Pleasure and sensitivity: greater sensitivity and pleasure, according to user reports
Hours
What you may feel
- Nausea within the hour that follows, the most frequent effect, which lessens with continued use.
- Flushing, facial redness, headaches.
- A slight, temporary rise in blood pressure.
- With frequent use, darkening of the skin in places, which may persist.
Stop and consult if
- An erection that lasts more than four hours.
- Palpitations, chest pain, a sharp rise in blood pressure.
- Vomiting that prevents you from keeping fluids down.
When to abstain
- Uncontrolled hypertension or known cardiovascular disease.
- Pregnancy or breastfeeding.
- Blood pressure treatment, without your prescriber's advice.
- Minors.
The effects to watch for, and how to reduce them
This sheet is educational. It replaces neither a diagnosis nor follow-up: for any medical condition, pregnancy, breastfeeding or current medication, talk to a health professional.
To avoid
- A second melanocortin agonist on the same day (Melanotan II): same receptors, effects and nausea that add up.
- Alcohol in quantity: amplified nausea and drop in blood pressure.
PT-141 has passed phase 3 (the RECONNECT program) in more than 1,200 premenopausal women with desire disorder: a significant increase in desire and less distress compared with placebo.
It has been approved in the United States since 2019. In men, phase 2 trials showed an effect on erection and desire.
2019 · Kingsberg et al., Obstetrics and Gynecology (RECONNECT trials)
Two randomized, placebo-controlled phase 3 trials, premenopausal women with hypoactive sexual desire disorder
Significant increase in desire and decreased distress related to its decline compared with placebo; nausea was the main adverse effect, especially at the start.
2004 · Diamond et al., Urology
Double-blind, placebo-controlled trial in men with erectile dysfunction
Increased erectile response and desire on bremelanotide, including without visual stimulation: the central effect is confirmed.
2008 · Safarinejad and Hosseini, Journal of Urology
Randomized, placebo-controlled trial in men who did not respond adequately to sildenafil
Improved erectile function in a substantial share of participants, showing the value of a central mechanism where the vascular pathway isn't enough.
Is it like sildenafil?
No. Sildenafil acts on blood flow to the genitals. PT-141 activates the MC4R receptor in the brain, which is involved in desire.
How long before it works?
The effect usually appears thirty minutes to two hours after injection and lasts several hours. The protocol provided with the product specifies the timing.
Does it tan?
No. With frequent use, some areas of the skin can darken: that's why your protocol limits the number of doses.
Glossary (5)
- Bremelanotide
- The generic name for PT-141, approved as a drug in the United States in 2019.
- MC4R
- A brain melanocortin receptor involved in appetite and sexual response.
- Hypoactive sexual desire disorder
- A persistent decline in desire that causes distress, without a medical or relational cause that explains it.
- Hypothalamus
- A brain region that regulates appetite, temperature, hormones, and part of sexual behaviour.
- Phase 3
- The last stage of clinical trials before approval, involving a large number of participants.