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

General Information of Drug (ID: DMBGA35)

• Drug Name: AP-1030 Drug Info
• Synonyms: AP-1102; AP-1130; MS-05; Combined MC1/MC4 receptor agonists, Action Pharma; Melanocortin-1/-4 receptor agonists, ActionPharma; Melanocortin-1/melanocortin-4 receptor agonists, Action Pharma

Indication

Disease Entry	ICD 11	Status	REF
Metabolic disorder	5C50-5D2Z	Phase 1/2	[1]

• Cross-matching ID: TTD Drug ID: DMBGA35

Molecule-Related Drug Atlas

Drug(s) Targeting Melanocortin receptor 1 (MC1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bremelanotide	DM20LIM	Hypoactive sexual desire dysfunction	HA00	Approved	[3]
Afamelanotide	DMVWHTG	Erythropoietic porphyrias	5C58.12	Approved	[4]
Dersimelagon	DMMO0SU	Erythropoietic protoporphyria	5C58.12	Phase 3	[5]
PL8177	DML5V22	Ulcerative colitis	DD71	Phase 2	[6]
MT-II	DMKT1DA	Female sexual arousal dysfunction	HA01.1	Investigative	[7]
C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2	DMX7IVO	Discovery agent	N.A.	Investigative	[8]
Ac-YRMEHdFRWG-NH2	DMN2UKC	Discovery agent	N.A.	Investigative	[9]
C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2	DMM19SJ	Discovery agent	N.A.	Investigative	[8]
C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2	DMSIGJW	Discovery agent	N.A.	Investigative	[8]
C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2	DMUESCH	Discovery agent	N.A.	Investigative	[8]

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	[10]
Bremelanotide	DM20LIM	Hypoactive sexual desire dysfunction	HA00	Approved	[3]
Setmelanotide	DMPVRN9	Obesity	5B81	Approved	[11]
Amylin	DMWDEN0	N. A.	N. A.	Phase 4	[12]
AMG 386	DMQJXL4	Breast cancer	2C60-2C65	Phase 3	[10]
PMX-53	DMZUAJ4	Atopic dermatitis	EA80	Phase 2	[13]
PF-446687	DML38VU	Female sexual arousal dysfunction	HA01.1	Phase 2	[14]
PF-07258669	DM3CJ5N	Malnutrition	5B50-5B71	Phase 1	[15]
PT-14	DMYM9JL	Erectile dysfunction	HA01.1	Discontinued in Phase 2	[16]
Melanotetan II	DMYK8MV	Obesity	5B81	Preclinical	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Melanocortin receptor 1 (MC1R)	TT0MV2T	MSHR_HUMAN	Modulator	[2]
Melanocortin receptor 4 (MC4R)	TTD0CIQ	MC4R_HUMAN	Modulator	[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: 1322).
• [2] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [5] Dersimelagon, a novel oral melanocortin 1 receptor agonist, demonstrates disease-modifying effects in preclinical models of systemic sclerosis. Arthritis Res Ther. 2022 Sep 1;24(1):210.
• [6] Pharmacokinetics of the Melanocortin Type 1 Receptor Agonist PL8177 After Subcutaneous Administration. Drugs R D. 2021 Dec;21(4):431-443.
• [7] Design of potent linear alpha-melanotropin 4-10 analogues modified in positions 5 and 10. J Med Chem. 1989 Jan;32(1):174-9.
• [8] Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. J Med Chem. 2006 Mar 23;49(6):1946-52.
• [9] Discovery of a beta-MSH-derived MC-4R selective agonist. J Med Chem. 2005 May 5;48(9):3095-8.
• [10] Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
• [11] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [12] Novel anti-obesity drugs. Expert Opin Investig Drugs. 2000 Jun;9(6):1317-26.
• [13] 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.
• [14] Melanocortin Receptor Agonists Facilitate Oxytocin-Dependent Partner Preference Formation in the Prairie Vole. Neuropsychopharmacology. 2015 Jul;40(8):1856-65.
• [15] 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.
• [16] 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.