Bremelanotide

Bremelanotide is a melanocortin receptor (MCR) agonist that nonselectively activates several receptor subtypes with the following order of potency: MC1R, MC4R, MC3R, MC5R, MC2R. At therapeutic dose levels, binding to MC1R and MC4R is most relevant.

• VYLEESI is indicated for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), as characterized by low sexual desire that causes marked distress or interpersonal difficulty and is NOT due to: A co-existing medical or psychiatric condition, Problems with the relationship, or The effects of a medication or drug substance. Acquired HSDD refers to HSDD that develops in a patient who previously had no problems with sexual desire.

• VYLEESI is contraindicated in patients who have uncontrolled hypertension or known cardiovascular disease [see Warnings and Precautions ( 5.1 )]. Uncontrolled hypertension or known cardiovascular disease.contraindicated

Inject 1.75 mg subcutaneously via the autoinjector to the abdomen or thigh, as needed, at least 45 minutes before anticipated sexual activity. ( 2.1 ) Do not administer more than one dose within 24 hours. ( 2.1 ) More than 8 doses per month is not recommended. ( 2.1 ) 2.1 Recommended Dosage The recommended dosage of VYLEESI is 1.75 mg administered subcutaneously in the abdomen or thigh, as needed, at least 45 minutes before anticipated sexual activity. The duration of efficacy after each dose is unknown and the optimal window for VYLEESI administration has not been fully characterized. Patients may decide the optimal time for VYLEESI administration based on how they experience the duration of effect on desire and any adverse reactions such as nausea [ see Warnings and Precautions ( 5.3 )]. Patients should not administer more than one dose within 24 hours. The efficacy of consecutive doses within 24 hours has not been established and administering doses close together may increase the risk of additive effects on blood pressure [see Warnings and Precautions ( 5.1 )]. Administering more than 8 doses per month is not recommended. Few patients in the phase 3 program received more than 8 doses per month. Also, more frequent dosing increases the risk for focal hyperpigmentation and the length of time per month when blood pressure is increased [see Warnings and Precautions ( 5.1 , 5.2 )]. VYLEESI is self-administered via a prefilled autoinjector pen.

Transient increase in blood pressure and decrease in heart rate: Occurs after each dose and usually resolves within 12 hours. Consider the patient's cardiovascular risk before initiating VYLEESI and periodically during treatment and ensure blood pressure is well-controlled. VYLEESI is not recommended in patients at high risk for cardiovascular disease. ( 5.1 ) Focal hyperpigmentation: Reported by 1% of patients who received up to 8 doses per month, including involvement of the face, gingiva and breasts. Higher risk in patients with darker skin and with daily dosing. Resolution was not confirmed in some patients. Consider discontinuing VYLEESI if hyperpigmentation develops. ( 5.2 ) Nausea: Reported by 40% of patients who received up to 8 monthly doses, requiring anti-emetic therapy in 13% of patients and leading to premature discontinuation for 8% of patients. Improved for most patients with the second dose. Consider discontinuing VYLEESI or initiating anti-emetic therapy for persistent or severe nausea. ( 5.3 ) 5.1 Transient Increase in Blood Pressure and Reduction in Heart Rate VYLEESI transiently increases blood pressure and reduces heart rate after each dose. In clinical studies, VYLEESI induced maximal increases of 6 mmHg in systolic blood pressure (SBP) and 3 mmHg in diastolic blood pressure (DBP) that peaked between 2 to 4 hours post dose. There was a corresponding reduction in heart rate up to 5 beats per minute. Blood pressure and heart rate returned to baseline usually within 12 hours post-dose.

The following adverse reactions are discussed in greater detail elsewhere in labeling: Transient increases in blood pressure and reductions in heart rate [ see Warnings and Precautions ( 5.1 ) and Clinical Pharmacology ( 12.2 ) ] Focal hyperpigmentation [ see Warnings and Precautions ( 5.2 )] Nausea [ see Warnings and Precautions ( 5.3 ) ] Most common adverse reactions (incidence > 4%) are nausea, flushing, injection site reactions, headache, and vomiting. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Palatin Technologies at 1-800-972-5220 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to the rates in the clinical trials of another drug and may not reflect the rates observed in practice. The efficacy and safety of VYLEESI was studied in two identical, 24-week, randomized, double-blind, placebo-controlled trials in 1247 premenopausal women with acquired, generalized HSDD. The age range was 19-56 years old with a mean age of 39 years old; 86% were White and 12% were Black. Both trials also included a 52-week open-label, uncontrolled extension phase during which 684 patients received VYLEESI [ see Clinical Studies ( 14 )]. Most patients used VYLEESI two to three times per month and no more than once a week. Serious adverse reactions were reported in 1.1% of VYLEESI-treated patients and 0.5% of placebo-treated patients.

Pregnancy: Advise patients to discontinue VYLEESI if pregnancy is suspected. ( 8.1 ) Females of Reproductive Potential: Advise patients to use effective contraception while taking VYLEESI. ( 8.3 ) 8.1 Pregnancy Pregnancy Exposure Registry There will be a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to VYLEESI during pregnancy. Pregnant women exposed to VYLEESI and healthcare providers are encouraged to call the VYLEESI Pregnancy Exposure Registry at (800) 972-5220. Risk Summary The few pregnancies in women exposed to VYLEESI in clinical trials are insufficient for determining whether there is a drug-associated risk for major birth defects, miscarriage or adverse maternal or fetal outcomes. Based on findings in animal studies, the use of VYLEESI in pregnant women may be associated with the potential for fetal harm. In animal reproduction and development studies, daily subcutaneous administration of bremelanotide to pregnant dogs during the period of organogenesis at exposures greater than or equal to 16 times the maximum recommended dose (based on area under the concentration-time curve or AUC) produced fetal harm. In mice subcutaneously dosed with bremelanotide during pregnancy and lactation, developmental effects were observed in the offspring at greater than or equal to 125-times the maximum recommended dose (based on AUC) [ see Data ].

Metabolism

Following subcutaneous administration of VYLEESI, the mean plasma C max and AUC of bremelanotide are 72.8 ng/mL and 276 hr*ng/mL, respectively. Mean plasma concentrations of bremelanotide increase in a less than dose proportional manner in the dose range of 0.3 to 10 mg, with mean C max levels reaching a plateau at the 7.5 mg subcutaneous dose level (approximately 4.3 times the maximum recommended dose).

No reports of overdosage with VYLEESI have been reported. Nausea, focal hyperpigmentation and more pronounced blood pressure increases are more likely with higher doses. In the event of overdosage, treatment should address the symptoms with supportive measures, as needed.

• Jun 21, 2019NDANDA210557Cosette

1. 1Nausea37543%
2. 2Drug Ineffective17120%
3. 3Headache13015%
4. 4Vomiting10712%
5. 5Off Label Use708.0%
6. 6Flushing657.4%
7. 7Illness637.2%
8. 8Adverse Drug Reaction434.9%
9. 9Dizziness384.3%
10. 10Fatigue343.9%
11. 11Feeling Abnormal333.8%
12. 12Cough323.7%
13. 13Malaise273.1%
14. 14Pain252.9%
15. 15Erythema242.7%

The 10 most recently updated of 10 ClinicalTrials.gov registrations naming Bremelanotide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Single Dose of Vyleesi in Lactating Female Subjects to Measure the Concentration of Bremelanotide in Breast Milk
  Completed · Phase 4 · Interventional · 10 enrolled · Cosette Pharmaceuticals, Inc.
  NCT06867835updated 2026-01-13
• A Phase 2 Study Evaluating the Co-Administration of Bremelanotide With Tirzepatide for the Treatment of Obesity
  Active not recruiting · Phase 2 · Interventional · 108 enrolled · Palatin Technologies, Inc
  NCT06565611updated 2025-03-06
• A Phase 3, Bridging, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group Trial to Evaluate the Efficacy and Safety of Subcutaneously Administered Bremelanotide in Premenopausal Women With Hypoactive Sexual Desire Disorder (With or Without Decreased Arousal)
  Completed · Phase 3 · Interventional · 193 enrolled · Kwang Dong Pharmaceutical co., ltd.
  NCT04943068updated 2024-11-13
• A Phase IIb, Multicenter, Open-Label, Prospective Study of Bremelanotide in Diabetic Kidney Disease
  Completed · Phase 2 · Interventional · 16 enrolled · Palatin Technologies, Inc
  NCT05709444updated 2024-10-17
• Role of the Melanocortin-4 Receptor in Hypoactive Sexual Desire Disorder
  Completed · Phase 4 · Interventional · 40 enrolled · Imperial College Healthcare NHS Trust
  NCT04179734updated 2024-08-09
• Study to Evaluate Rate of Nausea in Healthy Premenopausal Female Subjects Treated With Single Dose of Bremelanotide Alone or With Zofran
  Completed · Phase 1 · Interventional · 228 enrolled · AMAG Pharmaceuticals, Inc.
  NCT03973047updated 2022-04-04
• 1. Study to Evaluate the Efficacy/Safety of Bremelanotide in Premenopausal Women With Hypoactive Sexual Desire Disorder
  Completed · Phase 3 · Interventional · 723 enrolled · Palatin Technologies, Inc
  NCT02333071updated 2021-04-09
• 2. Study to Evaluate the Efficacy/Safety of Bremelanotide in Premenopausal Women With Hypoactive Sexual Desire Disorder
  Completed · Phase 3 · Interventional · 714 enrolled · Palatin Technologies, Inc
  NCT02338960updated 2021-01-28
• Bremelanotide in Premenopausal Women With Female Sexual Arousal Disorder and/or Hypoactive Sexual Desire Disorder
  Completed · Phase 2 · Interventional · 612 enrolled · Palatin Technologies, Inc
  NCT01382719updated 2014-12-18
• Evaluate the Safety and Efficacy of Bremelanotide in Women With Female Sexual Arousal Disorder (FSAD)
  Completed · Phase 2 · Interventional · Palatin Technologies, Inc
  NCT00425256updated 2011-02-23

Frequently asked questions

How does Bremelanotide work?

Bremelanotide is a melanocortin receptor (MCR) agonist that nonselectively activates several receptor subtypes with the following order of potency: MC1R, MC4R, MC3R, MC5R, MC2R. At therapeutic dose levels, binding to MC1R and MC4R is most relevant.

What is Bremelanotide used for?

According to FDA labeling, Bremelanotide carries indications including: VYLEESI is indicated for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), as characterized by low sexual desire that causes marked distress or interpersonal difficulty and is NOT due to: A co-existing medical or psychiatric condition, Problems with the relationship, or The effects of a medication or drug substance. Acquired HSDD refers to HSDD that develops in a patient who previously had no problems with sexual desire.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Bremelanotide?

Bremelanotide is classified as Other gynecologicals, Melanocortin Receptor Agonist, Melanocortin Receptor Agonists, Unknown Cellular or Molecular Interaction, Increased Dopamine Activity.

What are the brand names for Bremelanotide?

Bremelanotide is marketed under brand names including Vyleesi.

What are the contraindications for Bremelanotide?

Bremelanotide labeling lists contraindications including: VYLEESI is contraindicated in patients who have uncontrolled hypertension or known cardiovascular disease [see Warnings and Precautions ( 5.1 )]. Uncontrolled hypertension or known cardiovascular disease.. Always consult the full prescribing information and a clinician.