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

General Information of Drug (ID: DMS7C6R)

• Drug Name: MK-5046 Drug Info
• Synonyms: MK 5046; MK5046

Indication

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

• Cross-matching ID:
  PubChem CID: 49871766
  TTD Drug ID: DMS7C6R

Molecule-Related Drug Atlas

Drug(s) Targeting Bombesin receptor (BS)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Demobesin	DMPXLMB	Breast cancer	2C60-2C65	Phase 1	[4]
BAY-86-7548	DM195JA	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]
kuwanon H	DMVQDNR	Discovery agent	N.A.	Investigative	[6]
bombesin	DMDFQ0Y	Discovery agent	N.A.	Investigative	[7]
PD 168368	DMFNQEA	Discovery agent	N.A.	Investigative	[8]
bantag-1	DM4OT8M	Discovery agent	N.A.	Investigative	[3]
ranatensin	DMI7NAF	Discovery agent	N.A.	Investigative	[9]
PD 176252	DM7AY6K	Discovery agent	N.A.	Investigative	[8]
[(N4-Bzdig)0]BB(7-14)	DMD4BSJ	Discovery agent	N.A.	Investigative	[10]
neuromedin B	DMCXJLH	Discovery agent	N.A.	Investigative	[11]

Drug(s) Targeting Gastrin-releasing peptide receptor (GRPR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ASP-7147	DMGDF2X	Irritable bowel syndrome	DD91.0	Phase 2	[12]
RC-3095	DMIG98L	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
177Lu-labelled NeoBOMB1	DM2TSMD	Solid tumour/cancer	2A00-2F9Z	Phase 2	[14]
177-Lu-NeoB	DM6JLNT	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[14]
177Lu-AMBA	DMFG1YA	Breast cancer	2C60-2C65	Phase 1	[15]
BIM-26226	DM9F4LP	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[16]
kuwanon H	DMVQDNR	Discovery agent	N.A.	Investigative	[6]
bombesin	DMDFQ0Y	Discovery agent	N.A.	Investigative	[7]
PD 168368	DMFNQEA	Discovery agent	N.A.	Investigative	[17]
bantag-1	DM4OT8M	Discovery agent	N.A.	Investigative	[3]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Bombesin receptor (BS)	TTHYDUM	NMBR_HUMAN; GRPR_HUMAN; BRS3_HUMAN	Agonist	[2]
Gastrin-releasing peptide receptor (GRPR)	TTC1MVT	GRPR_HUMAN	Agonist	[3]

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: 6170).
• [2] Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. J Pharmacol Exp Ther. 2011 Feb;336(2):356-64.
• [3] Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors. J Pharmacol Exp Ther. 2013 Oct;347(1):100-16.
• [4] 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. (Target id: 38).
• [5] Plasma pharmacokinetics, whole-body distribution, metabolism, and radiation dosimetry of 68Ga bombesin antagonist BAY 86-7548 in healthy men. J Nucl Med. 2013 Jun;54(6):867-72.
• [6] Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry. Biochem Biophys Res Commun. 1995 Aug 15;213(2):594-9.
• [7] Expression and characterization of cloned human bombesin receptors. Mol Pharmacol. 1995 Jan;47(1):10-20.
• [8] Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. Peptides. 2009 Aug;30(8):1473-86.
• [9] Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R). Biochemistry. 1999 Jun 1;38(22):7307-20.
• [10] Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study. J Med Chem. 2005 Jan 13;48(1):100-10.
• [11] Insights into bombesin receptors and ligands: Highlighting recent advances. Peptides. 2015 Oct;72:128-44.
• [12] Astellas and Drais Partner To Develop Third Astellas Compound through Tacurion
• [13] Lipid modification of GRN163, an N3'-->P5' thio-phosphoramidate oligonucleotide, enhances the potency of telomerase inhibition. Oncogene. 2005 Aug 4;24(33):5262-8.
• [14] 68Ga/177Lu-NeoBOMB1, a Novel Radiolabeled GRPR Antagonist for Theranostic Use in Oncology. J Nucl Med. 2017 Feb;58(2):293-299.
• [15] Multimodality imaging and preclinical evaluation of 177Lu-AMBA for human prostate tumours in a murine model. Anticancer Res. 2010 Oct;30(10):4039-48.
• [16] Effect of the gastrin-releasing peptide antagonist BIM 26226 and lanreotide on an acinar pancreatic carcinoma. Eur J Pharmacol. 1998 Apr 17;347(1):77-86.
• [17] Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. J Pharmacol Exp Ther. 1999 Sep;290(3):1202-11.