U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C50H68N14O10
Molecular Weight 1025.1627
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BREMELANOTIDE

SMILES

CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@H](CC2=CNC3=CC=CC=C23)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](CC4=CC=CC=C4)NC(=O)[C@H](CC5=CN=CN5)NC1=O)C(O)=O

InChI

InChIKey=FFHBJDQSGDNCIV-MFVUMRCOSA-N
InChI=1S/C50H68N14O10/c1-3-4-16-35(58-29(2)65)43(67)64-41-25-42(66)54-20-11-10-18-37(49(73)74)60-46(70)39(23-31-26-56-34-17-9-8-15-33(31)34)62-44(68)36(19-12-21-55-50(51)52)59-45(69)38(22-30-13-6-5-7-14-30)61-47(71)40(63-48(41)72)24-32-27-53-28-57-32/h5-9,13-15,17,26-28,35-41,56H,3-4,10-12,16,18-25H2,1-2H3,(H,53,57)(H,54,66)(H,58,65)(H,59,69)(H,60,70)(H,61,71)(H,62,68)(H,63,72)(H,64,67)(H,73,74)(H4,51,52,55)/t35-,36-,37-,38+,39-,40-,41-/m0/s1

HIDE SMILES / InChI
Molecular Formula C50H68N14O10
Molecular Weight 1025.1627
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 7 / 7
E/Z Centers 1
Optical Activity UNSPECIFIED

Description

Bremelanotide (formerly PT-141) was developed for the treatment of female sexual dysfunction, hemorrhagic shock, and reperfusion injury. Bremelanotide, a synthetic peptide analog of α-melanocyte-stimulating hormone (α-MSH) is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system. Bremelanotide originally was tested for intranasal administration in treating female sexual dysfunction but this application was temporarily discontinued in 2008 after concerns were raised over adverse side effects of increased blood pressure. It appears that development for hemorrhagic shock and reperfusion injury has been discontinued. Palatin Technologies licensed North American development and commercialization rights of bremelanotide to Amag in January 2017. In June 2018, the US Food and Drug Administration (FDA) accepted AMAG Pharmaceuticals’ new drug application for bremelanotide for treatment of hypoactive sexual desire disorder in premenopausal women. If approved, bremelanotide will be available as a self-administered, disposable subcutaneous auto-injector used in anticipation of a sexual encounter.

Originator

Approval Year

2019
334
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2678
Agonist
2678
Agonist
2678
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
72.8 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
1.75 mg single, subcutaneous
dose: 1.75 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
BREMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
276 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
1.75 mg single, subcutaneous
dose: 1.75 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
BREMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.7 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
1.75 mg single, subcutaneous
dose: 1.75 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
BREMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
79%
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
1.75 mg single, subcutaneous
dose: 1.75 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
BREMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Disc. AE: Nausea, Headache...
Other AEs: Nausea, Flushing...
AEs leading to
discontinuation/dose reduction:
Nausea (8%)
Headache (2%)
Vomiting (1%)
Flushing (1%)
Injection site reactions (1%)
Flu-like symptoms (grade 1-2, <1%)
Increased blood pressure (grade 1-2, <1%)
Other AEs:
Nausea (grade 1-2, 40%)
Flushing (grade 1-2, 20.3%)
Injection site reactions (grade 1-2, 13.2%)
Headache (grade 1-2, 11.3%)
Vomiting (grade 1-2, 4.8%)
Cough (grade 1-2, 3.3%)
Fatigue (grade 1-2, 3.2%)
Hot flush (grade 1-2, 2.7%)
Paraesthesia (grade 1-2, 2.6%)
Dizziness (grade 1-2, 2.2%)
Nasal congestion (grade 1-2, 2.1%)
Upper abdominal pain (grade 1-2, <2%)
Diarrhea (grade 1-2, <2%)
Myalgia (grade 1-2, <2%)
Arthralgia (grade 1-2, <2%)
Pain (grade 1-2, <2%)
Restless leg syndrome (grade 1-2, <2%)
Rhinorrhea (grade 1-2, <2%)
Creatine phosphokinase increased (grade 1-2, <2%)
Blood pressure increased (grade 1-2, <2%)
Pain in extremity (grade 1-2, <2%)
Hyperpigmentation skin (grade 1-2, <2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
20 mg 1 times / day single, intranasal
Highest studied dose
Dose: 20 mg, 1 times / day
Route: intranasal
Route: single
Dose: 20 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
healthy, mean age 32.7
n = 24
Health Status: healthy
Age Group: mean age 32.7
Sex: M
Population Size: 24
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
Other AEs: Flushing...
Other AEs:
Flushing (mild, 16.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
20 mg 1 times / day single, intranasal
Highest studied dose
Dose: 20 mg, 1 times / day
Route: intranasal
Route: single
Dose: 20 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
healthy, mean age 32.7
n = 6
Health Status: healthy
Age Group: mean age 32.7
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
Other AEs: Vomiting, Feeling hot...
Other AEs:
Vomiting (mild, 16.7%)
Feeling hot (mild, 33.3%)
Somnolence (mild, 16.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
1.75 mg 3 times / week multiple, subcutaneous
Dose: 1.75 mg, 3 times / week
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 3 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
unhealthy, mean age 38.5
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: mean age 38.5
Sex: F
Population Size: 627
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
Other AEs: Paresthesia, Injection site erythema...
Other AEs:
Paresthesia (grade 1-2, 2.6%)
Injection site erythema (grade 1-2, 2.9%)
Injection site pruritus (grade 1-2, 2.1%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
10 mg 1 times / day single, subcutaneous
MTD
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: single
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
healthy
n = 6
Health Status: healthy
Sex: M
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
Other AEs: Vomiting...
Other AEs:
Vomiting (grade 1-2, 50%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
AEs

AEs

AESignificanceDosePopulation
Flushing 1%
Disc. AE
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Injection site reactions 1%
Disc. AE
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Vomiting 1%
Disc. AE
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Headache 2%
Disc. AE
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Nausea 8%
Disc. AE
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Headache grade 1-2, 11.3%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Injection site reactions grade 1-2, 13.2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Nasal congestion grade 1-2, 2.1%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Dizziness grade 1-2, 2.2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Paraesthesia grade 1-2, 2.6%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Hot flush grade 1-2, 2.7%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Flushing grade 1-2, 20.3%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Fatigue grade 1-2, 3.2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Cough grade 1-2, 3.3%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Vomiting grade 1-2, 4.8%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Nausea grade 1-2, 40%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Flu-like symptoms grade 1-2, <1%
Disc. AE
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Increased blood pressure grade 1-2, <1%
Disc. AE
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Arthralgia grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Blood pressure increased grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Creatine phosphokinase increased grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Diarrhea grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Hyperpigmentation skin grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Myalgia grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Pain in extremity grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Pain grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Restless leg syndrome grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Rhinorrhea grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Upper abdominal pain grade 1-2, <2%
1.75 mg 10 times / 24 weeks multiple, subcutaneous
Recommended
Dose: 1.75 mg, 10 times / 24 weeks
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 10 times / 24 weeks
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
unhealthy, 19-56 years old
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: 19-56 years old
Sex: F
Population Size: 627
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/210557s000lbl.pdf
Flushing mild, 16.7%
20 mg 1 times / day single, intranasal
Highest studied dose
Dose: 20 mg, 1 times / day
Route: intranasal
Route: single
Dose: 20 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
healthy, mean age 32.7
n = 24
Health Status: healthy
Age Group: mean age 32.7
Sex: M
Population Size: 24
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
Somnolence mild, 16.7%
20 mg 1 times / day single, intranasal
Highest studied dose
Dose: 20 mg, 1 times / day
Route: intranasal
Route: single
Dose: 20 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
healthy, mean age 32.7
n = 6
Health Status: healthy
Age Group: mean age 32.7
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
Vomiting mild, 16.7%
20 mg 1 times / day single, intranasal
Highest studied dose
Dose: 20 mg, 1 times / day
Route: intranasal
Route: single
Dose: 20 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
healthy, mean age 32.7
n = 6
Health Status: healthy
Age Group: mean age 32.7
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
Feeling hot mild, 33.3%
20 mg 1 times / day single, intranasal
Highest studied dose
Dose: 20 mg, 1 times / day
Route: intranasal
Route: single
Dose: 20 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
healthy, mean age 32.7
n = 6
Health Status: healthy
Age Group: mean age 32.7
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/14963471/
Injection site pruritus grade 1-2, 2.1%
1.75 mg 3 times / week multiple, subcutaneous
Dose: 1.75 mg, 3 times / week
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 3 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
unhealthy, mean age 38.5
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: mean age 38.5
Sex: F
Population Size: 627
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
Paresthesia grade 1-2, 2.6%
1.75 mg 3 times / week multiple, subcutaneous
Dose: 1.75 mg, 3 times / week
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 3 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
unhealthy, mean age 38.5
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: mean age 38.5
Sex: F
Population Size: 627
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
Injection site erythema grade 1-2, 2.9%
1.75 mg 3 times / week multiple, subcutaneous
Dose: 1.75 mg, 3 times / week
Route: subcutaneous
Route: multiple
Dose: 1.75 mg, 3 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
unhealthy, mean age 38.5
n = 627
Health Status: unhealthy
Condition: hypoactive sexual desire disorder
Age Group: mean age 38.5
Sex: F
Population Size: 627
Sources:
https://pubmed.ncbi.nlm.nih.gov/31599840/
Vomiting grade 1-2, 50%
10 mg 1 times / day single, subcutaneous
MTD
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: single
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
healthy
n = 6
Health Status: healthy
Sex: M
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210557Orig1s000MultidisciplineR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587

inducer
781
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2C19
1478

CYP2E1
882

CYP2B6
810

CYP2C8
911

OATP1B3
706

P-gp
1461

OAT3
642

BCRP
699

OAT1
599

OATP1B1
788

OCT2
647
CYP1A2
701

CYP2B6
547

CYP2C19
293
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OAT3
644
 low [Inhibition 1 uM]
OATP1B3
715
 low [Inhibition 1 uM]
P-gp
1650
 low [Inhibition 1 uM]
BCRP
773
 low
OAT1
603
 low
OATP1B1
803
 low
OCT2
648
 low
CYP2A6
739
 no [Inhibition 200 uM]
CYP3A4
1925
 no [Ki 16 uM]
CYP2C19
1553
 no [Ki 35 uM]
CYP1A2
1692
 no
CYP1A2
1692
 no
CYP2B6
1001
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2C8
965
 no
CYP2C9
1819
 no
CYP2D6
1891
 no
CYP2E1
970
 no
CYP3A4
1925
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
Acorn PharmaTech
ACN-057294
http://www.acornpharmatech.com/
BOC Sciences
189691-06-3
https://www.bocsci.com/bremelanotide-cas-189691-06-3-item-61871.html
BioSynth
Q-200747
https://www.biosynth.com/en/products/life-science/other-biochemicals/products/Q-200747.html
Chemenu
CM101686
http://www.chemenu.com/products/CM101686
Chemspace
CSSB02125551071
https://chem-space.com/CSSB02125551071
Hairui
BRCQ032
http://www.hairuichem.com/en/product/189691-06-3.html
MolPort
MolPort-009-194-183
https://www.molport.com/shop/molecule-link/MolPort-009-194-183
MuseChem
M043676
https://www.musechem.com/product/M043676.html
Smolecule
S522013
http://www.smolecule.com/products/s522013
THE BioTek
bt-261470
https://www.thebiotek.com/product/inhibitors/bt-261470
THE BioTek
bt-242583
https://www.thebiotek.com/product/peptides/bt-242583
eNovation Chemicals
D679352
https://www.enovationchem.com/ProductDetails.asp?ProductID=D679352
iChemical
EBD19124
http://www.ichemical.com/products/189691-06-3.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
PubMed

PubMed

TitleDatePubMed
PT-141: a melanocortin agonist for the treatment of sexual dysfunction.
2003 Jun
Bremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial.
2016 Jun
Re: Bremelanotide for Female Sexual Dysfunctions in Premenopausal Women: A Randomized, Placebo-Controlled Dose-Finding Trial.
2016 Nov
Phase I Randomized Placebo-controlled, Double-blind Study of the Safety and Tolerability of Bremelanotide Coadministered With Ethanol in Healthy Male and Female Participants.
2017 Mar

Sample Use Guides

In Vivo Use Guide
Subjects will self-administer a fixed dose of bremelanotide (BMT) subcutaneously (SC) via auto-injector on an as needed basis with no more than 1 dose taken every 24 hours.
Route of Administration: Other
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:28:06 UTC 2023
Edited
by admin
on Fri Dec 15 16:28:06 UTC 2023
Record UNII
6Y24O4F92S
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BREMELANOTIDE
INN   USAN  
INN   USAN  
Official Name English
N-ACETYL-L-2-AMINOHEXANOYL-L-.ALPHA.-ASPARTYL-L-HISTIDYL-D-PHENYLALANYL-L-ARGINYL-L-TRYPTOPHYL-L-LYSINE-(2->7)-LACTAM
Common Name English
bremelanotide [INN]
Common Name English
L-LYSINE, N-ACETYL-L-NORLEUCYL-L-.ALPHA.-ASPARTYL-L-HISTIDYL-D-PHENYLALANYL-L-ARGINYL-L-TRYPTOPHYL-, (2->7)-LACTAM
Common Name English
PT-141 FREE BASE
Code English
Bremelanotide [WHO-DD]
Common Name English
BREMELANOTIDE [USAN]
Common Name English
BREMELANOTIDE [MI]
Common Name English
Classification Tree Code System Code
WIKIPEDIA Designer-drugs-Bremelanotide
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
NCI_THESAURUS C548
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
Code System Code Type Description
CAS
189691-06-3
Created by admin on Fri Dec 15 16:28:06 UTC 2023 , Edited by admin on Fri Dec 15 16:28:06 UTC 2023
PRIMARY
MERCK INDEX
m12151
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
FDA UNII
6Y24O4F92S
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
ChEMBL
CHEMBL2070241
Created by admin on Fri Dec 15 16:28:06 UTC 2023 , Edited by admin on Fri Dec 15 16:28:06 UTC 2023
PRIMARY
MESH
C476721
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
DAILYMED
6Y24O4F92S
Created by admin on Fri Dec 15 16:28:06 UTC 2023 , Edited by admin on Fri Dec 15 16:28:06 UTC 2023
PRIMARY
NCI_THESAURUS
C77009
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
PUBCHEM
9941379
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
DRUG BANK
DB11653
Created by admin on Fri Dec 15 16:28:06 UTC 2023 , Edited by admin on Fri Dec 15 16:28:06 UTC 2023
PRIMARY
EPA CompTox
DTXSID40893711
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
INN
8737
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
WIKIPEDIA
BREMELANOTIDE
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
RXCUI
2176312
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
DRUG CENTRAL
5329
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
USAN
RR-45
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
LACTMED
Bremelanotide
Created by admin on Fri Dec 15 16:28:07 UTC 2023 , Edited by admin on Fri Dec 15 16:28:07 UTC 2023
PRIMARY
Related Record Type Details
MELANOCORTIN RECEPTOR 1
TARGET -> AGONIST
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of INTERMEDINE
PARENT -> DERIVATIVE
MELANOCORTIN RECEPTOR 5
TARGET -> AGONIST
MELANOCORTIN RECEPTOR 4
TARGET -> AGONIST
Structure of BREMELANOTIDE ACETATE
SALT/SOLVATE -> PARENT
MELANOCORTIN RECEPTOR 3
TARGET -> AGONIST
ADRENOCORTICOTROPIC HORMONE RECEPTOR
TARGET -> AGONIST
Related Record Type Details
Structure of BREMELANOTIDE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC SINGLE SUBCUTANEOUS ADMINISTRATION

Biological Half-life PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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