Is PT-141 (bremelanotide) FDA-approved?

Yes. Bremelanotide was FDA-approved in June 2019 under the brand name Vyleesi for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women not caused by a medical or psychiatric condition. This is currently its only approved indication. Use in men or for other purposes is off-label.

How is PT-141 different from Viagra or Cialis?

PDE5 inhibitors (sildenafil, tadalafil) work peripherally by increasing genital blood flow; they require sexual stimulation and do not act on desire itself. PT-141 works centrally in the brain — targeting MC3R and MC4R in the hypothalamus and limbic system — to enhance sexual desire and arousal at the neurological level, independently of vascular mechanisms. The two approaches are pharmacologically complementary; early trials combined them for men with PDE5-inhibitor non-response.

What is the approved dose and how is it taken?

The FDA-approved Vyleesi dose is 1.75 mg injected subcutaneously (into the abdomen or thigh) at least 45 minutes before anticipated sexual activity, using the supplied single-use autoinjector. It should not be used more than once in 24 hours or more than approximately eight times per month. This is the only dose and route that has regulatory approval; community protocols using compounded material are anecdotal.

What are the main side effects?

In Phase 3 clinical trials, nausea was the most common side effect (approximately 40% of treated patients), followed by flushing (20%), injection-site reactions (13%), and headache (11%). A transient increase in blood pressure and decrease in heart rate occurs after each dose, typically resolving within 12 hours. Repeated monthly use above eight doses can cause focal hyperpigmentation of the face, gums, or breasts. It is contraindicated in patients with uncontrolled hypertension or cardiovascular disease.

Does PT-141 cause tanning like Melanotan II?

PT-141 was specifically derived from Melanotan II with reduced MC1R (melanocyte) activity, so it does not produce significant skin darkening at clinical doses. Some community sources report mild and transient pigmentation changes, but this is not a primary or intended effect, unlike MT-II which was developed partly as a tanning agent.

Men are not an approved indication. Early-phase human trials and off-label use in men have explored PT-141 for erectile dysfunction, particularly in PDE5-inhibitor non-responders, with modest preliminary signals of benefit. However, no Phase 3 male trial has been completed and there is no approved male indication. Off-label male use relies on anecdotal and small-trial data only.

Aesthetic

PT-141

Also known as: Bremelanotide, Vyleesi, PT141

PT-141 (bremelanotide) is an FDA-approved melanocortin receptor agonist — marketed as Vyleesi — indicated for hypoactive sexual desire disorder (HSDD) in premenopausal...

Last updated July 11, 2026

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Overview

PT-141, the research designation for bremelanotide, is a synthetic cyclic heptapeptide (Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-OH; C₅₀H₆₈N₁₄O₁₀; MW ≈ 1025.2 Da) derived by structural modification of Melanotan II (MT-II), itself a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH). Where MT-II retains strong agonism at MC1R and produces prominent skin-tanning effects, PT-141 was re-engineered for preferential activity at MC3R and MC4R while reducing MC1R tanning activity — giving it a CNS-mediated pro-sexual profile without significant melanogenesis. In June 2019 the FDA approved bremelanotide under the brand name Vyleesi (Palatin Technologies / AMAG Pharmaceuticals) for acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women, making it the first melanocortin receptor agonist approved for any indication in the United States. Approval was based on two identical Phase 3 randomized, double-blind, placebo-controlled trials (RECONNECT Studies 301 and 302), in which 1,247 premenopausal women received bremelanotide 1.75 mg SC as needed or placebo for 24 weeks. Both co-primary endpoints — change in FSFI desire domain score and change in FSDS-DAO item 13 (distress) — reached statistical significance. Outside its approved indication, PT-141 has been studied in early-phase trials for male erectile dysfunction, including patients with inadequate response to PDE5 inhibitors, and is used off-label by men in research and compounding contexts. These uses lack an approved indication and rely on smaller or earlier-phase evidence. Research-use material sold outside the pharmaceutical supply chain is not subject to FDA manufacturing oversight and may vary in identity, purity, and sterility. The approved Vyleesi autoinjector is the only form of bremelanotide with confirmed pharmaceutical-grade quality. This entry is for research reference only and does not constitute medical advice.

How it works

Bremelanotide is a non-selective agonist at melanocortin receptors (MC1R, MC3R, MC4R, and MC5R; it does not bind MC2R). Its pro-sexual effects are attributed primarily to agonism at MC4R — and to a lesser extent MC3R — in hypothalamic and limbic nuclei, particularly the medial preoptic area and paraventricular nucleus. Activation of these receptors enhances dopaminergic and nitric oxide signaling within CNS circuits governing sexual motivation and arousal, a mechanism entirely distinct from the peripheral vasodilatory approach of PDE5 inhibitors (sildenafil, tadalafil). The compound therefore acts on desire and arousal at the level of the brain rather than on genital blood flow, which theoretically allows activity even when nitric oxide-dependent vascular pathways are impaired. MC1R agonism is present but lower than in MT-II, resulting in minimal tanning. Pharmacokinetics after SC injection: absolute bioavailability ≈ 100%; Tmax ≈ 1 hour; terminal half-life ≈ 2.7 hours (range 1.9–4.0 h); protein binding 21%; excretion predominantly renal (≈ 65%) with fecal component (≈ 23%).

Researched effects

Clinical Significantly increases sexual desire and reduces distress related to low sexual desire in premenopausal women with HSDD
Clinical Sustained improvement in desire and distress maintained over 52 weeks of open-label extension without new safety signals
Preclinical Improves erectile function in men who are inadequate responders to PDE5 inhibitors (intranasal formulation, early-phase data)
Preclinical Enhanced erectile response when co-administered with sildenafil compared to sildenafil monotherapy in early-phase trial
Preclinical Acts via central (CNS) mechanisms, potentially effective when peripheral vasodilatory pathways are insufficient
Anecdotal Increased sexual desire, arousal, and satisfaction in both men and women as reported by off-label users

Evidence levels: Clinical (human trials) · Preclinical (animal/lab) · Anecdotal (community-reported).

Dosing reference

For research reference only — not a recommendation.

Clinical / studied dosing

The FDA-approved dose of Vyleesi (bremelanotide) is 1.75 mg administered as a single subcutaneous injection into the abdomen or thigh, at least 45 minutes before anticipated sexual activity. No more than one dose should be taken per 24 hours, and the manufacturer advises against using more than one dose per month on average (no more than eight doses per month) to reduce the risk of hyperpigmentation. Vyleesi is supplied as a single-use autoinjector. It should not be used in patients with uncontrolled hypertension or known cardiovascular disease due to transient blood-pressure effects. Earlier intranasal formulations (10–20 mg) were investigated in Phase 1–2 trials for male erectile dysfunction but the intranasal route was halted by the FDA in 2007 because of more pronounced blood-pressure concerns at those doses; the approved subcutaneous route at 1.75 mg produces more modest and manageable cardiovascular effects.

Community-reported dosing (anecdotal)

Anecdotal and research-reference only; not medical advice. Community and compounding sources typically describe bremelanotide at 1–2 mg administered subcutaneously 30–60 minutes before sexual activity, mirroring the Vyleesi clinical dose. Some off-label male users report doses of 1 mg to reduce nausea while still achieving effect. These figures reflect unverified self-reported practice outside any clinical trial, and material obtained outside the pharmaceutical supply chain is unregulated and of unknown purity. The only evidence-supported dose and route is the FDA-approved 1.75 mg SC protocol.

Half-life: Approximately 2.7 hours (range 1.9–4.0 hours) following subcutaneous administration. Peak plasma concentration is reached in approximately 1 hour. Blood pressure effects peak at 2–4 hours post-dose and return to baseline within approximately 12 hours.
Routes: subcutaneous

Safety & side effects

Bremelanotide (Vyleesi) is FDA-approved (June 2019) for HSDD in premenopausal women; this is the only approved indication. The most common adverse reactions in RECONNECT Phase 3 trials were nausea (40.0%), flushing (20.3%), headache (11.3%), and injection-site reactions. Nausea was severe enough for 13% of treated patients to use an antiemetic. VYLEESI transiently increases blood pressure and decreases heart rate after each dose; in trials, mean peak systolic blood pressure increased by up to 6 mmHg and mean peak diastolic by up to 3 mmHg, peaking at 2–4 hours and resolving within 12 hours. It is contraindicated in patients with uncontrolled hypertension or cardiovascular disease. Repeated use above eight doses per month may cause focal hyperpigmentation of the face, gums, and breasts, particularly in patients with darker skin tones. A single case of clinically apparent hepatotoxicity has been reported (possible, not established causal). Serious adverse events occurred in 1.1% of bremelanotide-treated patients versus 0.5% placebo in Phase 3. WADA status: bremelanotide is not explicitly named on the 2025 WADA Prohibited List as a specific compound, but WADA Section S2 (Peptide Hormones, Growth Factors, Related Substances and Mimetics) contains broad catch-all language that may encompass melanocortin receptor agonists; competitive athletes should seek guidance from their governing body or a qualified anti-doping advisor before use. Research-use material sold outside the pharmaceutical supply chain is unregulated; purity, identity, and sterility are not guaranteed. This information is for research reference only and is not a recommendation for human use outside a licensed medical context.

Research summary

Bremelanotide has a more robust clinical evidence base than almost any research peptide, owing to its FDA-approval pathway. The pivotal evidence consists of two identical Phase 3 RECONNECT trials (Kingsberg et al., Obstet Gynecol, 2019; PMID 31599840): 1,247 premenopausal women with HSDD were randomised 1:1 to bremelanotide 1.75 mg SC as needed or placebo for 24 weeks. Both studies met both co-primary endpoints — FSFI desire domain (pooled improvement +0.35 over placebo, p<0.001) and FSDS-DAO item 13 distress score (pooled improvement −0.33 over placebo, p<0.001). Effect sizes were statistically significant but modest in absolute terms, and the clinical meaningfulness of these changes has been debated. A 52-week open-label extension (Simon et al., Obstet Gynecol, 2019; PMID 31599847) enrolling 684 completers found no new safety signals and sustained improvement in desire and distress, with FSFI desire changes exceeding the minimal clinically important difference threshold (+0.6) for most of the extension. Nausea (40.4%), flushing (20.6%), and headache (12.0%) were the dominant drug-related adverse events; nausea was the principal reason for discontinuation. For men, earlier-phase evidence includes a Phase 2A dose-response study (Diamond et al., 2004) via intranasal route in men with erectile dysfunction, a non-responder study (Safarinejad & Hosseini, 2008) reporting meaningful improvement in approximately 34% of sildenafil non-responders versus 9% placebo, and a combination study suggesting additive benefit when co-administered with sildenafil. No male-specific Phase 3 trial has been completed and there is no approved male indication. A Phase 2 study of bremelanotide plus a PDE5 inhibitor for men who are non-responders to PDE5 inhibitor monotherapy was announced by Palatin Technologies but results have not been published at the time of this writing. The honest assessment: bremelanotide is the best-evidenced pro-sexual peptide available, with robust FDA-level clinical data supporting a specific and modest benefit for HSDD in premenopausal women. Male use remains preliminary and off-label. The compound's transient cardiovascular effects, high nausea incidence, and hyperpigmentation risk with frequent use are well-characterised real concerns.

FAQ

Is PT-141 (bremelanotide) FDA-approved?: Yes. Bremelanotide was FDA-approved in June 2019 under the brand name Vyleesi for the treatment of acquired, generalized hypoactive sexual desire disorder (HSDD) in premenopausal women not caused by a medical or psychiatric condition. This is currently its only approved indication. Use in men or for other purposes is off-label.
How is PT-141 different from Viagra or Cialis?: PDE5 inhibitors (sildenafil, tadalafil) work peripherally by increasing genital blood flow; they require sexual stimulation and do not act on desire itself. PT-141 works centrally in the brain — targeting MC3R and MC4R in the hypothalamus and limbic system — to enhance sexual desire and arousal at the neurological level, independently of vascular mechanisms. The two approaches are pharmacologically complementary; early trials combined them for men with PDE5-inhibitor non-response.
What is the approved dose and how is it taken?: The FDA-approved Vyleesi dose is 1.75 mg injected subcutaneously (into the abdomen or thigh) at least 45 minutes before anticipated sexual activity, using the supplied single-use autoinjector. It should not be used more than once in 24 hours or more than approximately eight times per month. This is the only dose and route that has regulatory approval; community protocols using compounded material are anecdotal.
What are the main side effects?: In Phase 3 clinical trials, nausea was the most common side effect (approximately 40% of treated patients), followed by flushing (20%), injection-site reactions (13%), and headache (11%). A transient increase in blood pressure and decrease in heart rate occurs after each dose, typically resolving within 12 hours. Repeated monthly use above eight doses can cause focal hyperpigmentation of the face, gums, or breasts. It is contraindicated in patients with uncontrolled hypertension or cardiovascular disease.
Does PT-141 cause tanning like Melanotan II?: PT-141 was specifically derived from Melanotan II with reduced MC1R (melanocyte) activity, so it does not produce significant skin darkening at clinical doses. Some community sources report mild and transient pigmentation changes, but this is not a primary or intended effect, unlike MT-II which was developed partly as a tanning agent.
Can men use PT-141?: Men are not an approved indication. Early-phase human trials and off-label use in men have explored PT-141 for erectile dysfunction, particularly in PDE5-inhibitor non-responders, with modest preliminary signals of benefit. However, no Phase 3 male trial has been completed and there is no approved male indication. Off-label male use relies on anecdotal and small-trial data only.
Is PT-141 on the WADA prohibited list?: Bremelanotide is not listed by name on the 2025 WADA Prohibited List, but WADA Section S2 (Peptide Hormones, Growth Factors, Related Substances and Mimetics) contains broad language that may encompass melanocortin receptor agonists. Competitive athletes subject to anti-doping rules should consult their sport's governing body or a qualified anti-doping advisor before using bremelanotide in any form.

References

All content is for research and educational use only and is not medical advice. Products are sold for laboratory research only and are not for human consumption.

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