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
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
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.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL259 |
0.27 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | IMCIVREE Approved UseObesity 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 Date2020 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20.9% |
SETMELANOTIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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%) Other AEs:Upper respiratory tract infection (25.9%) Asthenia (18.5%) Injection site reaction (4, 14.8%) Eosinophilia Spontaneous penile erection (23.1%) Sources: Suicidal ideation (grade 5, 11.1%) Pneumonia Adrenal insufficiency Panic attack (1) Hyperhidrosis Pleuritis |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213793Orig1s000PharmR.pdf#page=25 Page: 25.0 |
PubMed
Title | Date | PubMed |
---|---|---|
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30048591
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
Edited
Wed Apr 02 07:11:38 GMT 2025
by
admin
on
Wed Apr 02 07:11:38 GMT 2025
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Record UNII |
9L64H0UE5Y
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Record Status |
Validated (UNII)
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Record Version |
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admin on Wed Apr 02 07:11:38 GMT 2025 , Edited by admin on Wed Apr 02 07:11:38 GMT 2025
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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
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |