General
Preferred name
BREMELANOTIDE
Synonyms
PT-141 Acetate ()
Bremelanotide (Acetate) ()
PT-141 ()
BREMELANOTIDE ACETATE ()
Vyleesi (autoinjector) ()
Vyleesi ()
PT 141 ()
Bremelanotida ()
PT-141 FREE BASE ()
PT-141 (acetate) ()
P&D ID
PD059044
CAS
189691-06-3
1607799-13-2
Tags
available
drug
Approved by
FDA
First approval
2019
Drug indication
mental or behavioural disorder
Sexual dysfunction
Hypoactive sexual desire dysfunction
Erectile dysfunction
Drug Status
approved
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
HALF-LIFE
The half life of bremelanotide is 2.7 hours (1.9-4.0 hours).[L4894]
PHARMACODYNAMICS
Bremelanotide is a melanocortin receptor agonist injected 45 minutes before anticipated sexual activity.[L4894] Agonism of the melanocortin receptor MC1R also leads to increased melanin expression.[L4894] Patients taking bremelanotide may also experience nausea, headache, and vomiting.[L4894]
MOA
Bremelanotide is an agonist of many melanocortin receptors which in order of potency are MC1R, MC4R, MC3R, MC5R, and MC2R.[L4894] 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.[L4894] MC3R and MC4R are found in the hypothalamus and are involved in food intake and energy homeostasis.[A179683]; ; One theory is that bremelanotide stimulates dopamine in the medial preoptic area, which is involved in the sexual behaviour of a number of organisms.[A179692]
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.[L4894]
ROE
64.8% of a radiolabelled dose is excreted in the urine and 22.8% of the dose is recovered in the feces.[L4894]
TOXICITY
Currently there are no reports of overdoses of bremelanotide.[L4894] Patients taking higher doses are more likely to experience nausea, focal hyperpigmentation, and increases in blood pressure.[L4894] In the event of an overdose, supportive measures should be used to address the associated symptoms.[L4894]
METABOLISM
Bremelanotide is a 7 amino acid and so its metabolism consists of multiple hydrolysis reactions.[L4894]
ABSORPTION
Bremelanotide has a Tmax or 1.0 hour (0.5-1.0 hours) and is 100% bioavailable.[L4894] The Cmax is 72.8ng/mL and the AUC is 276hr\*ng/mL.[L4894]
DESCRIPTION
Bremelanotide is a stabilised, cyclic derivative of αMSH. Although it exhibits little selectivity across the melanocortin receptor family (with the exception of MC2, the ACTH receptor), bremelanotide's ability to increase female sexual arousal/desire is attributed primarily to agonist activity at the MC3 and MC4 receptors .
(GtoPdb)
DESCRIPTION
Bremelanotide Acetate (PT-141 Acetate) is an agonist of melanocortin receptor (MCR) .
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
15
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
ReFrame library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
41
Molecular Weight
1024.52
Hydrogen Bond Acceptors
11
Hydrogen Bond Donors
14
Rotatable Bonds
17
Ring Count
5
Aromatic Ring Count
4
cLogP
-0.44
TPSA
376.47
Fraction CSP3
0.46
Chiral centers
7.0
Largest ring
23.0
QED
0.04
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Melanocortin Receptor
MC1R, MC2R, MC3R, MC4R, MC5R
Indication
hypoactive sexual desire disorder
MOA
melanocortin receptor agonist
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Source data
