SBS drug

Bremelanotide

DrugBank ID DB11653

Modality

Protein Based Therapies:

• Peptides

Clinical Trials Summary

Phase 0: 0

Phase 1: 1

Phase 2: 4

Phase 3: 3

Phase 4: 2

Therapeutic Categories

• Melanocortin Receptor Agonists

Brand Names

Vyleesi

Generic Name

Bremelanotide

DrugBank Accession Number

DB11653

Background

Bremelanotide is a 7 amino acid peptide used to treat hypoactive sexual desire disorder in premenopausal women. Bremelanotide does not interact with alcohol. The mechanism by which bremelanotide's action on receptors translates to a clinical effect is still unknown.

Bremelanotide was first described in the literature in 2003 when it was known by the investigational code PT-141. Since then it was investigated for its place in treating sexual dysfunction in men and women but is now only indicated for women. Other drugs used to treat female sexual dysfunction include flibanserin, estrogen, ospemifene, and prasterone.

Bremelanotide was granted FDA approval on 21 June 2019.

Modality

Protein Based Therapies

Peptides

Groups

Approved

Protein Chemical Formula

Not Available

Protein Average Weight

Not Available

Sequences

Not Available

Synonyms

• Bremelanotida
• Bremelanotide
• Brémelanotide
• Bremelanotidum

External IDs

• PT 141
• PT-141

Associated Conditions

Pharmacodynamics

Bremelanotide is a melanocortin receptor agonist injected 45 minutes before anticipated sexual activity. Agonism of the melanocortin receptor MC1R also leads to increased melanin expression. Patients taking bremelanotide may also experience nausea, headache, and vomiting.

Mechanism of action

Bremelanotide is an agonist of many melanocortin receptors which in order of potency are MC1R, MC4R, MC3R, MC5R, and MC2R. The mechanism by which agonism of these receptors translates to an improvement in hypoactive sexual desire disorder is currently unknown, however MC4R receptors are present in many areas of the central nervous system. MC3R and MC4R are found in the hypothalamus and are involved in food intake and energy homeostasis.

One theory is that bremelanotide stimulates dopamine in the medial preoptic area, which is involved in the sexual behaviour of a number of organisms.

Absorption

Bremelanotide has a T max or 1.0 hour (0.5-1.0 hours) and is 100% bioavailable. The C max is 72.8ng/mL and the AUC is 276hr*ng/mL.

Volume of distribution

The mean volume of distribution of bremelanotide is 25.0±5.8L.

Protein binding

Bremelanotide is 21% protein bound in serum.

Metabolism

Bremelanotide is a 7 amino acid and so its metabolism consists of multiple hydrolysis reactions.

Route of elimination

64.8% of a radiolabelled dose is excreted in the urine and 22.8% of the dose is recovered in the feces.

Half-life

The half life of bremelanotide is 2.7 hours (1.9-4.0 hours).

Clearance

The mean clearance of bremelanotide is 6.5±1.0L/hr.

Toxicity

Currently there are no reports of overdoses of bremelanotide. Patients taking higher doses are more likely to experience nausea, focal hyperpigmentation, and increases in blood pressure. In the event of an overdose, supportive measures should be used to address the associated symptoms.

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Food Interactions

No interactions found.

Product Ingredients

Brand Name Prescription Products

Drug Categories

• Amino Acids, Peptides, and Proteins
• Genito Urinary System and Sex Hormones
• Hormones
• Hormones, Hormone Substitutes, and Hormone Antagonists
• Hypothalamic Hormones
• Melanocortin Receptor Agonists
• Melanocortins
• Melanocyte-Stimulating Hormones
• Nerve Tissue Proteins
• Neuropeptides
• Peptide Hormones
• Peptides
• Pituitary Hormones
• Pituitary Hormones, Anterior
• Pro-Opiomelanocortin
• Protein Precursors
• Proteins
• Receptor, Melanocortin, Type 3, agonists
• Receptor, Melanocortin, Type 4, agonists

Chemical Taxonomy Provided by Classyfire

Description

Not Available

Kingdom

Organic Compounds

Super Class

Organic Acids

Class

Carboxylic Acids and Derivatives

Sub Class

Amino Acids, Peptides, and Analogues

Direct Parent

Peptides

Alternative Parents

Not Available

Substituents

Not Available

Molecular Framework

Not Available

External Descriptors

Not Available

Affected organisms

Not Available

UNII

6Y24O4F92S

CAS number

189691-06-3

General References

1. Molinoff PB, Shadiack AM, Earle D, Diamond LE, Quon CY: PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003 Jun;994:96-102. doi: 10.1111/j.1749-6632.2003.tb03167.x.
2. Clayton AH, Lucas J, DeRogatis LR, Jordan R: Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants. Clin Ther. 2017 Mar;39(3):514-526.e14. doi: 10.1016/j.clinthera.2017.01.018. Epub 2017 Feb 9.
3. Miller MK, Smith JR, Norman JJ, Clayton AH: Expert opinion on existing and developing drugs to treat female sexual dysfunction. Expert Opin Emerg Drugs. 2018 Sep;23(3):223-230. doi: 10.1080/14728214.2018.1527901. Epub 2018 Oct 11.
4. Both S: Recent Developments in Psychopharmaceutical Approaches to Treating Female Sexual Interest and Arousal Disorder. Curr Sex Health Rep. 2017;9(4):192-199. doi: 10.1007/s11930-017-0124-3. Epub 2017 Oct 19.
5. FDA Approved Drug Products: Bremelanotide Injection

Clinical Trials

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Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Prices

Not Available

Patents