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This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C49H68N18O9S2.ClH
Molecular Weight 1153.77
Optical Activity UNSPECIFIED
Defined Stereocenters 8 / 8
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SETMELANOTIDE HYDROCHLORIDE

SMILES

Cl.C[C@H]1NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC2=CNC3=C2C=CC=C3)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(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(C)=O

InChI

InChIKey=MANLVWQYYRHWLE-GZRAWZNHSA-N
InChI=1S/C49H68N18O9S2.ClH/c1-26-41(70)63-37(20-30-22-55-25-59-30)46(75)64-35(18-28-10-4-3-5-11-28)44(73)62-34(15-9-17-57-49(53)54)43(72)65-36(19-29-21-58-32-13-7-6-12-31(29)32)45(74)66-38(40(50)69)23-77-78-24-39(47(76)60-26)67-42(71)33(61-27(2)68)14-8-16-56-48(51)52;/h3-7,10-13,21-22,25-26,33-39,58H,8-9,14-20,23-24H2,1-2H3,(H2,50,69)(H,55,59)(H,60,76)(H,61,68)(H,62,73)(H,63,70)(H,64,75)(H,65,72)(H,66,74)(H,67,71)(H4,51,52,56)(H4,53,54,57);1H/t26-,33+,34+,35-,36+,37+,38+,39+;/m1./s1

HIDE SMILES / InChI

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C49H68N18O9S2
Molecular Weight 1117.309
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 8 / 8
E/Z Centers 0
Optical Activity UNSPECIFIED

Setmelanotide (IMCIVREE™) is a melanocortin-4 (MC4) receptor agonist developed by Rhythm Pharmaceuticals (Rhythm) for the treatment of ultrarare genetic disorders of obesity. Setmelanotide was approved on 27 November 2020 in the USA as a subcutaneous (SC) injectable formulation for chronic weight management in adult and pediatric patients 6 years of age and older with obesity due to proopiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), or leptin receptor (LEPR) deficiency confirmed by genetic testing demonstrating variants in POMC, PCSK1, or LEPR genes that are interpreted as pathogenic, likely pathogenic, or of uncertain significance (VUS). Rhythm are also developing the drug for the treatment of obesity associated with other rare genetic disorders including Bardet–Biedl Syndrome, Alström Syndrome, POMC and other MC4R pathway heterozygous defciency obesities, and POMC epigenetic disorders.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.27 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
IMCIVREE

Approved Use

Obesity due to proopiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), or leptin receptor (LEPR) deficiency confirmed by genetic testing demonstrating variants in POMC, PCSK1, or LEPR genes that are interpreted as pathogenic, likely pathogenic, or of uncertain significance (VUS).

Launch Date

2020
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
6.65 ng/mL
0.5 mg 1 times / day steady-state, subcutaneous
dose: 0.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
10.4 ng/mL
1 mg 1 times / day steady-state, subcutaneous
dose: 1 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
17.5 ng/mL
1.5 mg 1 times / day steady-state, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
25.1 ng/mL
2 mg 1 times / day steady-state, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
32.8 ng/mL
2.5 mg 1 times / day steady-state, subcutaneous
dose: 2.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
38 ng/mL
2.5 mg 1 times / day steady-state, subcutaneous
dose: 2.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
25.4 ng/mL
0.0215 mg/kg single, subcutaneous
dose: 0.0215 mg/kg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
14.2 ng/mL
0.75 mg 2 times / day steady-state, subcutaneous
dose: 0.75 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
23 ng/mL
1.5 mg 1 times / day steady-state, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
27.5 ng/mL
2 mg 1 times / day steady-state, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
19.7 ng/mL
2 mg single, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
24.8 ng/mL
1.5 mg single, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
17.5 ng/mL
2 mg single, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
6.47 ng/mL
0.5 mg 1 times / day unknown, subcutaneous
dose: 0.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
11.5 ng/mL
1 mg 1 times / day unknown, subcutaneous
dose: 1 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
22.4 ng/mL
1.5 mg 1 times / day unknown, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
24.5 ng/mL
2 mg 1 times / day unknown, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
24.4 ng/mL
2.5 mg 1 times / day unknown, subcutaneous
dose: 2.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
7.21 ng/mL
0.5 mg 1 times / day unknown, subcutaneous
dose: 0.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
10.4 ng/mL
1 mg 1 times / day unknown, subcutaneous
dose: 1 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
17 ng/mL
1.5 mg 1 times / day unknown, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
23.9 ng/mL
2 mg 1 times / day unknown, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
31.1 ng/mL
2.5 mg 1 times / day unknown, subcutaneous
dose: 2.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
38.9 ng/mL
3 mg 1 times / day unknown, subcutaneous
dose: 3 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
35.8 ng × h/mL
0.5 mg 1 times / day steady-state, subcutaneous
dose: 0.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
59.3 ng × h/mL
1 mg 1 times / day steady-state, subcutaneous
dose: 1 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
106 ng × h/mL
1.5 mg 1 times / day steady-state, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
146 ng × h/mL
2 mg 1 times / day steady-state, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
188 ng × h/mL
2.5 mg 1 times / day steady-state, subcutaneous
dose: 2.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
207 ng × h/mL
2.5 mg 1 times / day steady-state, subcutaneous
dose: 2.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
243 ng × h/mL
0.75 mg 2 times / day steady-state, subcutaneous
dose: 0.75 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
271 ng × h/mL
1.5 mg 1 times / day steady-state, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
347 ng × h/mL
2 mg 1 times / day steady-state, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
253 ng × h/mL
2 mg single, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
111 ng × h/mL
1.5 mg single, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
36.2 ng × h/mL
2 mg single, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
38.3 ng × h/mL
0.5 mg 1 times / day unknown, subcutaneous
dose: 0.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
74.2 ng × h/mL
1 mg 1 times / day unknown, subcutaneous
dose: 1 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
147 ng × h/mL
1.5 mg 1 times / day unknown, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
159 ng × h/mL
2 mg 1 times / day unknown, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
180 ng × h/mL
2.5 mg 1 times / day unknown, subcutaneous
dose: 2.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
56.2 ng × h/mL
0.5 mg 1 times / day unknown, subcutaneous
dose: 0.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
79.1 ng × h/mL
1 mg 1 times / day unknown, subcutaneous
dose: 1 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
130 ng × h/mL
1.5 mg 1 times / day unknown, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
178 ng × h/mL
2 mg 1 times / day unknown, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
260 ng × h/mL
2.5 mg 1 times / day unknown, subcutaneous
dose: 2.5 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
383 ng × h/mL
3 mg 1 times / day unknown, subcutaneous
dose: 3 mg
route of administration: Subcutaneous
experiment type: UNKNOWN
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
8.98 h
0.0215 mg/kg single, subcutaneous
dose: 0.0215 mg/kg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.91 h
0.75 mg 2 times / day steady-state, subcutaneous
dose: 0.75 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.55 h
1.5 mg 1 times / day steady-state, subcutaneous
dose: 1.5 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.73 h
2 mg 1 times / day steady-state, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: STEADY-STATE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.18 h
2 mg single, subcutaneous
dose: 2 mg
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
SETMELANOTIDE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
20.9%
SETMELANOTIDE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Disc. AE: Depression, Upper respiratory tract infection...
Other AEs: Spontaneous penile erection, Suicidal ideation...
AEs leading to
discontinuation/dose reduction:
Depression (4, 29.6%)
Upper respiratory tract infection (25.9%)
Asthenia (18.5%)
Injection site reaction (4, 14.8%)
Eosinophilia
Other AEs:
Spontaneous penile erection (23.1%)
Suicidal ideation (grade 5, 11.1%)
Pneumonia
Adrenal insufficiency
Panic attack (1)
Hyperhidrosis
Pleuritis
Sources:
AEs

AEs

AESignificanceDosePopulation
Adrenal insufficiency
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Hyperhidrosis
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Pleuritis
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Pneumonia
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Panic attack 1
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Asthenia 18.5%
Disc. AE
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Spontaneous penile erection 23.1%
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Upper respiratory tract infection 25.9%
Disc. AE
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Injection site reaction 4, 14.8%
Disc. AE
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Depression 4, 29.6%
Disc. AE
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Eosinophilia Disc. AE
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Suicidal ideation grade 5, 11.1%
3 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 3 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
unhealthy, CHILD|ADOLESCENT|ADULT
Health Status: unhealthy
Age Group: CHILD|ADOLESCENT|ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >1000 uM]
no [IC50 >1000 uM]
no [IC50 >1000 uM]
no [IC50 >1000 uM]
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
week [IC50 54.1 uM]
Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Chronic treatment with a melanocortin-4 receptor agonist causes weight loss, reduces insulin resistance, and improves cardiovascular function in diet-induced obese rhesus macaques.
2013 Feb
Insights into the Allosteric Mechanism of Setmelanotide (RM-493) as a Potent and First-in-Class Melanocortin-4 Receptor (MC4R) Agonist To Treat Rare Genetic Disorders of Obesity through an in Silico Approach.
2019 Mar 20

Sample Use Guides

Obesity due to deficiency of POMC, PCSK1, or LEPR: 2 mg (0.2 mL) injected subcutaneously once daily for 2 weeks.
Route of Administration: Other
Setmelanotide (RM-493) binds human MC4R with Ki value of 0.71 nM in radioligand binding assay and activated MC4R with EC50 value of 1.5 nM in intracellular cAMP production assay.
Substance Class Chemical
Created
by admin
on Wed Apr 02 07:11:38 GMT 2025
Edited
by admin
on Wed Apr 02 07:11:38 GMT 2025
Record UNII
9L64H0UE5Y
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SETMELANOTIDE HYDROCHLORIDE [USAN]
Preferred Name English
SETMELANOTIDE HYDROCHLORIDE
USAN  
Official Name English
L-CYSTEINAMIDE, N2-ACETYL-L-ARGINYL-L-CYSTEINYL-D-ALANYL-L-HISTIDYL-D-PHENYLALANYL-L-ARGINYL-L-TRYPTOPHYL-, CYCLIC (2->8)-DISULFIDE, HYDROCHLORIDE
Systematic Name English
N2-ACETYL-L-ARGINYL-L-CYSTEINYL-D-ALANYL-L-HISTIDYL-D-PHENYLALANYL-L-ARGINYL-L-TRYPTOPHYL-L-CYSTEINAMIDE, CYCLIC (2-8)-DISULFIDE, HYDROCHLORIDE
Systematic Name English
Code System Code Type Description
USAN
HI-90
Created by admin on Wed Apr 02 07:11:38 GMT 2025 , Edited by admin on Wed Apr 02 07:11:38 GMT 2025
PRIMARY
PUBCHEM
165412040
Created by admin on Wed Apr 02 07:11:38 GMT 2025 , Edited by admin on Wed Apr 02 07:11:38 GMT 2025
PRIMARY
CAS
2324799-41-7
Created by admin on Wed Apr 02 07:11:38 GMT 2025 , Edited by admin on Wed Apr 02 07:11:38 GMT 2025
PRIMARY
SMS_ID
300000028872
Created by admin on Wed Apr 02 07:11:38 GMT 2025 , Edited by admin on Wed Apr 02 07:11:38 GMT 2025
PRIMARY
FDA UNII
9L64H0UE5Y
Created by admin on Wed Apr 02 07:11:38 GMT 2025 , Edited by admin on Wed Apr 02 07:11:38 GMT 2025
PRIMARY
NCI_THESAURUS
C174581
Created by admin on Wed Apr 02 07:11:38 GMT 2025 , Edited by admin on Wed Apr 02 07:11:38 GMT 2025
PRIMARY
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