Bremelanotide
Also known as: Bremelanotide, Bremelanotide acetate, PT-141, PT141, Vyleesi
Source Bremelanotide at Peptiology
Save 10% with code PEPTI-BOSSRABBIT-10
Affiliate link: we earn a commission on purchases made through this link, at no extra cost to you.
Tapping Shop Now & Save 10% copies your 10% off code PEPTI-BOSSRABBIT-10 to your clipboard. Paste it at the Peptiology checkout to claim the discount.
Summary
Bremelanotide (Vyleesi™) is a synthetic cyclic heptapeptide that acts as a melanocortin receptor agonist. It is FDA‑approved for on‑demand subcutaneous use in premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), a condition marked by persistent low sexual desire that causes distress.
Mechanism of Action
Bremelanotide mimics the neuropeptide α‑MSH and binds with high affinity to the melanocortin‑4 receptor (MC4R) in the central nervous system. Activation of MC4R is thought to influence neural circuits that regulate sexual arousal and desire, thereby enhancing the motivational component of sexual response without directly affecting peripheral sexual organs.
What the Research Shows
The drug’s development culminated in two phase‑3, double‑blind, placebo‑controlled trials involving over 1,200 women, which demonstrated sufficient improvement in sexual desire to support FDA approval in 2019. Across the broader clinical program (≈3,500 participants in 43 studies), the safety profile was characterized, with most adverse events being mild to moderate. Additional reviews note that bremelanotide is one of two melanocortin‑targeting peptides approved for HSDD, underscoring the therapeutic relevance of this receptor system. Preclinical work on related melanocortin agonists has spurred interest in metabolic indications, but no efficacy data for bremelanotide in those areas are reported.
Reported Benefits
Clinical trials showed that on‑demand subcutaneous bremelanotide can increase sexual desire and reduce distress in women with HSDD, leading to its regulatory approval. The drug’s rapid onset and self‑administration allow flexible use around anticipated sexual activity, offering an alternative to daily‑dose agents.
Limitations of the Evidence
Evidence is limited to premenopausal women with acquired, generalized HSDD; efficacy in other populations or for other sexual dysfunctions has not been demonstrated. Long‑term data beyond 18 months are sparse, and the need for subcutaneous injection may affect adherence. The precise neurobiological mechanisms remain incompletely understood.
Safety Considerations
The most common adverse events were nausea (≈40 % of treated participants) and flushing (≈20 %). Headache and injection‑site reactions occurred in roughly 10 % and 5 % of users, respectively. Blood pressure showed small, transient increases, prompting caution in patients with cardiovascular risk. Hyperpigmentation was rare with label‑dose schedules but more frequent after daily dosing for many consecutive days. No deaths were reported, and serious adverse events were infrequent.
How It Is Administered
Bremelanotide is supplied as an acetate formulation for subcutaneous injection. It is intended for self‑administration on an as‑needed basis, typically 45 minutes before anticipated sexual activity, following the dosing schedule outlined in the prescribing information.
Routes of Administration
Goals & Uses
- Melanocortin-related skin tanningDermatology / CosmeticLow
- Male sexual dysfunction / erectile dysfunctionSexual HealthLow
- Erectile dysfunctionSexual HealthModerate
- Female sexual arousal disorderSexual DysfunctionModerate
- Hypoactive sexual desire disorderFemale Sexual DysfunctionHigh
- Hypoactive Sexual Desire Disorder (HSDD) treatmentSexual DysfunctionHigh
- Increased sexual desire/libidoSexual HealthHigh
Contraindications
- Known cardiovascular diseaseCardiovascularHigh
- Hypersensitivity to bremelanotide or excipientsAllergic/immunologicHigh
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Hypersensitivity to bremelanotide or any excipientsAllergyHigh
- Use in postmenopausal womenEndocrine/hormonalModerate
- Uncontrolled hypertensionCardiovascularModerate
Adverse Effects
- HypertensionCardiovascularUncommonHigh blood pressure
- Injection site reactionsLocalCommon
- HeadacheNeurologicCommonPain in the head or upper neck
- Transient hypertensionCardiovascularCommon
- FlushingVascularCommonWarmth and redness of the skin
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Injection site erythemaLocalCommonRedness at the injection site
- Hyperpigmentation (focal)DermatologicUncommon
Drug Interactions
- Antihypertensive agentsModerate
- Other sexual dysfunction agents (e.g., sildenafil)Low
- Indomethacin and NSAIDsLow
- NaltrexoneModerate
Population Constraints
- Severe renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeAbsolute
- MenSexRelative
- Lactating womenReproductiveAbsolute
- Premenopausal women onlyAge/reproductive StatusAbsolute
- Severe hepatic impairmentOrgan ImpairmentRelative
Regulatory Status
- European UnionUnapprovedSubmitted but not authorized
- United StatesApprovedApproved: Hypoactive sexual desire disorder in premenopausal womenMarketed as Vyleesi
- United KingdomUnapprovedNot licensed
Approved by FDA in 2019 (Vyleesi) for HSDD in premenopausal women; not approved in EU or UK.
Evidence & Sources
- Journal ArticleModerateDhillon S, Keam SJ2019-01-01T00:00:00.000000Z
- Journal ArticleModeratePettigrew JA, Novick AM2021-01-01T00:00:00.000000Z
- Journal ArticleModerateClayton AH, et al.2022-01-01T00:00:00.000000Z
- Journal ArticleModerateSweeney P, et al.2023-01-01T00:00:00.000000Z
Frequently Asked Questions
Who is eligible to receive bremelanotide?
The drug is approved for premenopausal women who have acquired, generalized hypoactive sexual desire disorder that causes personal distress. It is not indicated for men, post‑menopausal women, or for other forms of sexual dysfunction.
How quickly does bremelanotide work?
Clinical data support an on‑demand approach, with dosing recommended about 45 minutes before sexual activity. Users typically report an increase in desire within the same evening, although individual response times can vary.
What are the most common side effects?
Nausea and flushing are the most frequently reported, affecting roughly two‑thirds of users. Headache, mild injection‑site reactions, and modest blood‑pressure elevations have also been observed.
Can bremelanotide be taken daily?
Label instructions advise intermittent, on‑demand use. Daily dosing has been associated with a higher incidence of skin hyperpigmentation and is not recommended outside of a clinical trial setting.
Is bremelanotide safe for people with heart disease?
Because small, transient increases in blood pressure have been noted, clinicians advise caution in patients with uncontrolled hypertension or significant cardiovascular disease, and recommend monitoring blood pressure during treatment.
What is Bremelanotide?
Bremelanotide (Vyleesi™) is a synthetic cyclic heptapeptide that acts as a melanocortin receptor agonist. It is FDA‑approved for on‑demand subcutaneous use in premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), a condition marked by persistent low sexual desire that causes distress.
What is Bremelanotide used for?
Bremelanotide is educationally associated with: Melanocortin-related skin tanning, Male sexual dysfunction / erectile dysfunction, Erectile dysfunction, Female sexual arousal disorder, Hypoactive sexual desire disorder, Hypoactive Sexual Desire Disorder (HSDD) treatment, Increased sexual desire/libido. Educational only — not medical advice.
How is Bremelanotide administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Bremelanotide?
Reported adverse effects include: Hypertension, Injection site reactions, Headache, Transient hypertension, Flushing, Nausea, Injection site erythema, Hyperpigmentation (focal). This list is not exhaustive — consult a qualified clinician.
Who should avoid Bremelanotide?
Recorded contraindications: Known cardiovascular disease, Hypersensitivity to bremelanotide or excipients, Pregnancy, Hypersensitivity to bremelanotide or any excipients, Use in postmenopausal women, Uncontrolled hypertension. Consult a qualified clinician before use.