Setmelanotide

CHEMBL3301624 Phase 4 Approved Protein

Half-Life

—

Bioavailability

—

Protein Binding

—

Molecular Weight

1117.3 g/mol

LogP

-2.5

Phase

4

Setmelanotide is a melanocortin-4 receptor (MC4R) agonist peptide used for chronic weight management in patients with obesity due to specific genetic deficiencies affecting the leptin-melanocortin pathway, including POMC, PCSK1, or LEPR deficiency. By activating MC4R in the hypothalamus, it restores impaired satiety signaling in patients with these rare monogenic obesity disorders, reducing appetite and promoting weight loss. It is the first approved therapy specifically targeting genetically defined melanocortin pathway deficiencies.

Molecular Weight

1117.3000 g/mol

LogP

-2.50

TPSA

500.00 Å²

Lipinski RO5

Fail

Therapeutic Areas

Obesity

Pharmacokinetics (PK)

Pharmacodynamics (PD)

2D Structure

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SMILES

CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)NC1=O

InChI

InChI=1S/C49H68N18O9S2/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)/t26-,33+,34+,35-,36+,37+,38+,39+/m1/s1

Molecular Formula

C49H68N18O9S2

HBD / HBA

15 / 14

Rotatable Bonds

18

Heavy Atoms

78

No targets recorded

Target interaction data is not yet available for this drug.

No interactions recorded

Drug interaction data is not yet available for this compound.

No side effects recorded

Side effect data is not yet available for this drug.

Frequently Asked Questions

Setmelanotide is a melanocortin-4 receptor (MC4R) agonist peptide used for chronic weight management in patients with obesity due to specific genetic deficiencies affecting the leptin-melanocortin pathway, including POMC, PCSK1, or LEPR deficiency. By activating MC4R in the hypothalamus, it restores impaired satiety signaling in patients with these rare monogenic obesity disorders, reducing appetite and promoting weight loss. It is the first approved therapy specifically targeting genetically defined melanocortin pathway deficiencies.

Yes, Setmelanotide is an approved drug. It has reached clinical phase 4. It is classified as a Protein.

{# References & Data Sources section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

References & Data Sources

ChEMBL — European Bioinformatics Institute (EBI). CHEMBL3301624. Open-access bioactivity database.
PubChem — National Center for Biotechnology Information (NCBI). CID 11993702. Chemical information database.

Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.

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Structure

Quick Data

Formula: C49H68N18O9S2
Synonyms: 1

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Medical Disclaimer

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.