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

General Information of Drug (ID: DMM3FD2)

• Drug Name: HS014 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 24868239
  TTD Drug ID: DMM3FD2

Molecule-Related Drug Atlas

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	[3]
Bremelanotide	DM20LIM	Hypoactive sexual desire dysfunction	HA00	Approved	[4]
Setmelanotide	DMPVRN9	Obesity	5B81	Approved	[5]
Amylin	DMWDEN0	N. A.	N. A.	Phase 4	[6]
AMG 386	DMQJXL4	Breast cancer	2C60-2C65	Phase 3	[3]
PMX-53	DMZUAJ4	Atopic dermatitis	EA80	Phase 2	[7]
PF-446687	DML38VU	Female sexual arousal dysfunction	HA01.1	Phase 2	[8]
AP-1030	DMBGA35	Metabolic disorder	5C50-5D2Z	Phase 1/2	[9]
PF-07258669	DM3CJ5N	Malnutrition	5B50-5B71	Phase 1	[10]
PT-14	DMYM9JL	Erectile dysfunction	HA01.1	Discontinued in Phase 2	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Melanocortin receptor 4 (MC4R)	TTD0CIQ	MC4R_HUMAN	Antagonist	[2]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1321).
• [2] Long-term administration of MC4 receptor antagonist HS014 causes hyperphagia and obesity in rats. Neuroreport. 1999 Mar 17;10(4):707-11.
• [3] Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [6] Novel anti-obesity drugs. Expert Opin Investig Drugs. 2000 Jun;9(6):1317-26.
• [7] 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.
• [8] Melanocortin Receptor Agonists Facilitate Oxytocin-Dependent Partner Preference Formation in the Prairie Vole. Neuropsychopharmacology. 2015 Jul;40(8):1856-65.
• [9] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [10] 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.
• [11] 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.