Setmelanotide

Melanocortin 4 Receptor Agonist — ALIMENTARY TRACT AND METABOLISM

Key facts

Setmelanotide is an onp drug in the Melanocortin 4 Receptor Agonist class catalogued in DrugCentral. It was first approved by the EMA in 2018. Its mechanism of action is classified as Melanocortin 4 Receptor Agonists. DrugCentral lists 5 molecular targets, including MC4R, Mc4r and MC1R. Recorded indications include BardetBiedl syndrome, Leptin receptor (LEPR) deficiency, Obesity and Pro-opiomelanocortin (POMC) deficiency.

• Approval status: onp (first approved 2018 by the EMA).
• Drug class: Melanocortin 4 Receptor Agonist.
• Mechanism of action: Melanocortin 4 Receptor Agonists.
• Molecular targets: MC4R, Mc4r, MC1R and MC3R (5 listed in DrugCentral).
• Indications: BardetBiedl syndrome, Leptin receptor (LEPR) deficiency, Obesity and Pro-opiomelanocortin (POMC) deficiency.
• ATC code: A08AA12 (Centrally acting antiobesity products).
• Molecular formula: C49H68N18O9S2; molecular weight 1117.33 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (4)

• BardetBiedl syndrome
• Leptin receptor (LEPR) deficiency
• Obesity
• Pro-opiomelanocortin (POMC) deficiency

Mechanism & targets

• Mechanism of action (MoA): Melanocortin 4 Receptor Agonists
• Established pharmacologic class: Melanocortin 4 Receptor Agonist

Molecular targets (5)

Target	Gene	Action	Activity
Melanocortin receptor 4	MC4R	agonist	Kd 8.68
Melanocortin receptor 4	Mc4r	agonist	Ki 8.57
Melanocyte-stimulating hormone receptor	MC1R	agonist	Ki 8.41
Melanocortin receptor 3	MC3R	agonist	Ki 8.00
Melanocortin receptor 5	MC5R	agonist	Ki 6.37

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2020-11-25	FDA	—	RHYTHM PHARMACEUTICALS INC	Yes
2018-11-19	EMA	—	Rhythm Pharmaceuticals Limited	Yes

ATC classification

ATC code	Therapeutic hierarchy
A08AA12	ALIMENTARY TRACT AND METABOLISM › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › Centrally acting antiobesity products

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: LEPR, PCSK1, POMC · Testing Required
• FDA label: LEPR, PCSK1, POMC · Testing Required
• HCSC label: LEPR, PCSK1, POMC · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Skin hyperpigmentation	215.3
Melanocytic naevus	51.8

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Setmelanotide is on its molecule page.

• Molecular formula: C₄₉H₆₈N₁₈O₉S₂
• Molecular weight: 1117.33 g/mol
• CAS number: —
• InChIKey: HDHDTKMUACZDAA-PHNIDTBTSA-N
• PubChem CID: 11993702

C[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)C)C(=O)N)CC2=CNC3=CC=CC=C32)CCCN=C(N)N)CC4=CC=CC=C4)CC5=CN=CN5

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Setmelanotide used for?

DrugCentral lists the following indications for Setmelanotide: BardetBiedl syndrome, Leptin receptor (LEPR) deficiency, Obesity and Pro-opiomelanocortin (POMC) deficiency.

How does Setmelanotide work?

Setmelanotide is classified as Melanocortin 4 Receptor Agonists; its molecular targets in DrugCentral include MC4R (agonist), Mc4r (agonist), MC1R (agonist) and MC3R (agonist).

When was Setmelanotide first approved?

Setmelanotide was first approved by the EMA in 2018.

What drug class does Setmelanotide belong to?

Setmelanotide is in the Melanocortin 4 Receptor Agonist class.

What is the chemical formula of Setmelanotide?

Setmelanotide has the molecular formula C49H68N18O9S2 and a molecular weight of 1117.33 g/mol.

Sources

• DrugCentral drug card 5416 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3301624 — compound record and bioactivity
• PubChem CID 11993702 — chemical identifiers
• DrugBank DB11700 — drug record
• FDA UNII N7T15V1FUY — substance identity
• DailyMed: FDA labels for Setmelanotide — current prescribing information (label search)
• UniProt P32245 (MC4R) — target protein
• UniProt Q01726 (MC1R) — target protein
• UniProt P41968 (MC3R) — target protein
• UniProt P33032 (MC5R) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.