Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMPVRN9)

Drug Name

Setmelanotide Drug Info

Synonyms

RM-493; UNII-N7T15V1FUY; BIM-22493; N7T15V1FUY; 920014-72-8; Setmelanotide [USAN:INN]; GTPL9272; CHEMBL3301624; CS-6399; DB11700; HY-19870; L-Cysteinamide, N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-, cyclic (2-> 8)-disulfide; (4R,7S,10S,13R,16S,19R,22R)-22-[[(2S)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-13-benzyl-10-[3-(diaminomethylideneamino)propyl]-16-(1H-imidazol-5-ylmethyl)-7-(1H-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21-hexaoxo-1,2-d

Indication

Disease Entry	ICD 11	Status	REF
Obesity	5B81	Approved	[1]
Bardet biedl syndrome	5A61.0	Phase 3	[2]
Prader-Willi syndrome	LD90.3	Phase 2	[3]
Diabetic complication	5A2Y	Preclinical	[4]

Cross-matching ID

PubChem CID: 11993702
CAS Number: CAS 920014-72-8
TTD Drug ID: DMPVRN9
ACDINA Drug ID: D01425

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Preclinical Drug(s)

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Drug(s) Targeting Melanocortin receptor 4 (MC4R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methylnaltrexone bromide	DMZTGN2	Opioid-induced constipation	DB32.1	Approved	[5]
Bremelanotide	DM20LIM	Hypoactive sexual desire dysfunction	HA00	Approved	[6]
Amylin	DMWDEN0	N. A.	N. A.	Phase 4	[7]
AMG 386	DMQJXL4	Breast cancer	2C60-2C65	Phase 3	[5]
PMX-53	DMZUAJ4	Atopic dermatitis	EA80	Phase 2	[8]
PF-446687	DML38VU	Female sexual arousal dysfunction	HA01.1	Phase 2	[9]
AP-1030	DMBGA35	Metabolic disorder	5C50-5D2Z	Phase 1/2	[10]
PF-07258669	DM3CJ5N	Malnutrition	5B50-5B71	Phase 1	[11]
PT-14	DMYM9JL	Erectile dysfunction	HA01.1	Discontinued in Phase 2	[12]
Melanotetan II	DMYK8MV	Obesity	5B81	Preclinical	[5]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Melanocortin receptor 4 (MC4R)	TTD0CIQ	MC4R_HUMAN	Agonist	[1]

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References

1	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
2	ClinicalTrials.gov (NCT03746522) Setmelanotide (RM-493), Melanocortin-4 Receptor (MC4R) Agonist, in Bardet-Biedl Syndrome (BBS) and Alstrom Syndrome (AS) Patients With Moderate to Severe Obesity. U.S. National Institutes of Health.
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	2011 Pipeline of Ipsen.
5	Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
6	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
7	Novel anti-obesity drugs. Expert Opin Investig Drugs. 2000 Jun;9(6):1317-26.
8	Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
9	Melanocortin Receptor Agonists Facilitate Oxytocin-Dependent Partner Preference Formation in the Prairie Vole. Neuropsychopharmacology. 2015 Jul;40(8):1856-65.
10	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
11	Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss. J Med Chem. 2023 Mar 9;66(5):3195-3211.
12	The protective effects of the melanocortin receptor (MCR) agonist, melanotan-II (MTII), against binge-like ethanol drinking are facilitated by deletion of the MC3 receptor in mice. Neuropeptides. 2014 Feb;48(1):47-51.