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

General Information of Drug (ID: DM195JA)

• Drug Name: BAY-86-7548 Drug Info
• Synonyms: Bombesin-68Ga-labeled tracer (PET/CT cancer imaging), Bayer

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 72722205
  TTD Drug ID: DM195JA

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	[3]
kuwanon H	DMVQDNR	Discovery agent	N.A.	Investigative	[4]
bombesin	DMDFQ0Y	Discovery agent	N.A.	Investigative	[5]
PD 168368	DMFNQEA	Discovery agent	N.A.	Investigative	[6]
MK-5046	DMS7C6R	Discovery agent	N.A.	Investigative	[7]
bantag-1	DM4OT8M	Discovery agent	N.A.	Investigative	[8]
ranatensin	DMI7NAF	Discovery agent	N.A.	Investigative	[9]
PD 176252	DM7AY6K	Discovery agent	N.A.	Investigative	[6]
[(N4-Bzdig)0]BB(7-14)	DMD4BSJ	Discovery agent	N.A.	Investigative	[10]
neuromedin B	DMCXJLH	Discovery agent	N.A.	Investigative	[11]

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	Enhancer	[2]

References

• [1] ClinicalTrials.gov (NCT01205321) PET/CT Imaging for Radiation Dosimetry, Plasma Pharmacokinetics, Biodistribution, Safety and Tolerability and Diagnostic Performance of BAY86-7548 in Patients With Prostate Cancer and Healthy Volunteers. U.S. National Institutes of Health.
• [2] 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.
• [3] 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).
• [4] Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry. Biochem Biophys Res Commun. 1995 Aug 15;213(2):594-9.
• [5] Expression and characterization of cloned human bombesin receptors. Mol Pharmacol. 1995 Jan;47(1):10-20.
• [6] Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. Peptides. 2009 Aug;30(8):1473-86.
• [7] Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. J Pharmacol Exp Ther. 2011 Feb;336(2):356-64.
• [8] 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.
• [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.