NAV

Bremelanotide

Identification

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.5 Bremelanotide does not interact with alcohol.2 The mechanism by which bremelanotide's action on receptors translates to a clinical effect is still unknown.5

Bremelanotide was first described in the literature in 2003 when it was known by the investigational code PT-141.1 Since then it was investigated for its place in treating sexual dysfunction in men and women but is now only indicated for women.1,2,5 Other drugs used to treat female sexual dysfunction include flibanserin, estrogen, ospemifene, and prasterone.3

Bremelanotide was granted FDA approval on 21 June 2019.5

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Peptides
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • Bremelanotida
  • Bremelanotide
  • Brémelanotide
  • Bremelanotidum
External IDs
  • PT 141
  • PT-141

Pharmacology

Indication

Bremelanotide is indicated to treat premenopausal women with hypoactive sexual desire disorder that is not due to a medical or psychiatric condition, problems with the relationship, or the effects of a medication or drug.5

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Bremelanotide is a melanocortin receptor agonist injected 45 minutes before anticipated sexual activity.5 Agonism of the melanocortin receptor MC1R also leads to increased melanin expression.5 Patients taking bremelanotide may also experience nausea, headache, and vomiting.5

Mechanism of action

Bremelanotide is an agonist of many melanocortin receptors which in order of potency are MC1R, MC4R, MC3R, MC5R, and MC2R.5 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.5 MC3R and MC4R are found in the hypothalamus and are involved in food intake and energy homeostasis.1

One theory is that bremelanotide stimulates dopamine in the medial preoptic area, which is involved in the sexual behaviour of a number of organisms.4

TargetActionsOrganism
UMelanocyte-stimulating hormone receptor
agonist
Humans
UMelanocortin receptor 4
agonist
Humans
UMelanocortin receptor 3
agonist
Humans
UMelanocortin receptor 5
agonist
Humans
UAdrenocorticotropic hormone receptor
agonist
Humans
Absorption

Bremelanotide has a Tmax or 1.0 hour (0.5-1.0 hours) and is 100% bioavailable.5 The Cmax is 72.8ng/mL and the AUC is 276hr*ng/mL.5

Volume of distribution

The mean volume of distribution of bremelanotide is 25.0±5.8L.5

Protein binding

Bremelanotide is 21% protein bound in serum.5

Metabolism

Bremelanotide is a 7 amino acid and so its metabolism consists of multiple hydrolysis reactions.5

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.5

Half-life

The half life of bremelanotide is 2.7 hours (1.9-4.0 hours).5

Clearance

The mean clearance of bremelanotide is 6.5±1.0L/hr.5

Adverse Effects
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Toxicity

Currently there are no reports of overdoses of bremelanotide.5 Patients taking higher doses are more likely to experience nausea, focal hyperpigmentation, and increases in blood pressure.5 In the event of an overdose, supportive measures should be used to address the associated symptoms.5

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

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.
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NaltrexoneThe serum concentration of Naltrexone can be decreased when it is combined with Bremelanotide.
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Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Bremelanotide acetatePV2WI7495P1607799-13-2MAYUSRUHXFWITM-GBRHMYBBSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
VyleesiInjection1.75 mg/0.3mLSubcutaneousAMAG Pharmaceuticals, Inc.2019-06-21Not applicableUS flag
VyleesiInjection1.75 mg/0.3mLSubcutaneousPalatin Technologies2019-06-21Not applicableUS flag

Categories

ATC Codes
G02CX05 — Bremelanotide
Drug Categories
Chemical TaxonomyProvided 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

Chemical Identifiers

UNII
6Y24O4F92S
CAS number
189691-06-3

References

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  5. FDA Approved Drug Products: Bremelanotide Injection [Link]
PubChem Compound
9941379
PubChem Substance
347828024
ChemSpider
8116997
BindingDB
50389769
RxNav
2176312
ChEBI
177849
ChEMBL
CHEMBL2070241
Wikipedia
Bremelanotide
MSDS
Download (526 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4RecruitingTreatmentHypoactive Sexual Desire Disorder (HSDD)1
3CompletedTreatmentHypoactive Sexual Desire Disorder (HSDD)2
3RecruitingTreatmentHypoactive Sexual Desire Disorder (HSDD)1
2CompletedNot AvailableArousal Disorders, Sexual1
2CompletedTreatmentHypoactive Sexual Desire Disorder (HSDD) / Sexual; Disorder, Arousal, Female1
2RecruitingTreatmentKidney Diseases1
1CompletedTreatmentNausea1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionSubcutaneous1.75 mg/0.3mL
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9700592No2017-07-112033-11-05US flag
US9352013No2016-05-312033-11-05US flag
US10286034No2019-05-142033-11-05US flag
US6794489No2004-09-212020-06-28US flag
US6579968No2003-06-172020-06-28US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
boiling point (°C)230MSDS

Targets

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Details1. Melanocyte-stimulating hormone receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Ubiquitin protein ligase binding
Specific Function
Receptor for MSH (alpha, beta and gamma) and ACTH. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
Gene Name
MC1R
Uniprot ID
Q01726
Uniprot Name
Melanocyte-stimulating hormone receptor
Molecular Weight
34705.04 Da
Details2. Melanocortin receptor 4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Receptor specific to the heptapeptide core common to adrenocorticotropic hormone and alpha-, beta-, and gamma-MSH. Plays a central role in energy homeostasis and somatic growth. This receptor is mediated by G proteins that stimulate adenylate cyclase (cAMP).
Specific Function
Melanocortin receptor activity
Gene Name
MC4R
Uniprot ID
P32245
Uniprot Name
Melanocortin receptor 4
Molecular Weight
36942.325 Da
Details3. Melanocortin receptor 3
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Receptor for MSH (alpha, beta and gamma) and ACTH. This receptor is mediated by G proteins which activate adenylate cyclase. Required for expression of anticipatory patterns of activity and wakefulness during periods of limited nutrient availability and for the normal regulation of circadian clock activity in the brain.
Specific Function
Melanocortin receptor activity
Gene Name
MC3R
Uniprot ID
P41968
Uniprot Name
Melanocortin receptor 3
Molecular Weight
36042.75 Da
Details4. Melanocortin receptor 5
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Receptor for MSH (alpha, beta and gamma) and ACTH. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. This receptor is a possible mediator of the immunomodulation properties of melanocortins.
Specific Function
Hormone binding
Gene Name
MC5R
Uniprot ID
P33032
Uniprot Name
Melanocortin receptor 5
Molecular Weight
36600.21 Da
Details5. Adrenocorticotropic hormone receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Melanocortin receptor activity
Specific Function
Receptor for corticotropin (ACTH). This receptor is mediated by G proteins (G(s)) which activate adenylate cyclase (cAMP).
Gene Name
MC2R
Uniprot ID
Q01718
Uniprot Name
Adrenocorticotropic hormone receptor
Molecular Weight
33926.28 Da

Drug created at October 20, 2016 20:37 / Updated at September 05, 2022 12:50