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

General Information of DTT (ID: TTC1MVT)

• DTT Name: Gastrin-releasing peptide receptor (GRPR) DTT Info
• Gene Name: GRPR

Molecule-Related Drug & Molecule List

5 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
177Lu-labelled NeoBOMB1	DM2TSMD	Solid tumour/cancer	2A00-2F9Z	Phase 2	[1]
ASP-7147	DMGDF2X	Irritable bowel syndrome	DD91.0	Phase 2	[2]
RC-3095	DMIG98L	Solid tumour/cancer	2A00-2F9Z	Phase 2	[3]
177-Lu-NeoB	DM6JLNT	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[1]
177Lu-AMBA	DMFG1YA	Breast cancer	2C60-2C65	Phase 1	[4]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BIM-26226	DM9F4LP	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[5]

27 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(CH3)CCO-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2	DMD0P4G	Discovery agent	N.A.	Investigative	[6]
(D)Phe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH2	DMQN14X	Discovery agent	N.A.	Investigative	[7]
177Lu-labelled RM2	DMLC2VE	Solid tumour/cancer	2A00-2F9Z	Investigative	[8]
Ac-His-Trp-Ala-Val-Ala-His-Leu-Met-NH2	DMCA4QR	Discovery agent	N.A.	Investigative	[6]
Ac-His-Trp-Ala-Val-D-Ala-His-Leu-Met-NH2	DMUINVT	Discovery agent	N.A.	Investigative	[6]
Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2	DMUGO9M	Discovery agent	N.A.	Investigative	[6]
bantag-1	DM4OT8M	Discovery agent	N.A.	Investigative	[9]
bombesin	DMDFQ0Y	Discovery agent	N.A.	Investigative	[10]
JMV 1535	DMP1B9D	Discovery agent	N.A.	Investigative	[7]
JMV 1693	DMARTN3	Discovery agent	N.A.	Investigative	[7]
JMV 1719	DM82HW9	Discovery agent	N.A.	Investigative	[7]
JMV 1799	DMX3P68	Discovery agent	N.A.	Investigative	[7]
JMV 1801	DMTX694	Discovery agent	N.A.	Investigative	[7]
JMV 1802	DMGT6DN	Discovery agent	N.A.	Investigative	[7]
JMV 1803	DM248HC	Discovery agent	N.A.	Investigative	[7]
JMV 1813	DMSICYK	Discovery agent	N.A.	Investigative	[7]
kuwanon H	DMVQDNR	Discovery agent	N.A.	Investigative	[11]
MK-5046	DMS7C6R	Discovery agent	N.A.	Investigative	[9]
neuromedin B	DMCXJLH	Discovery agent	N.A.	Investigative	[10]
PD 168368	DMFNQEA	Discovery agent	N.A.	Investigative	[12]
PD 176252	DM7AY6K	Discovery agent	N.A.	Investigative	[13]
ranatensin	DMI7NAF	Discovery agent	N.A.	Investigative	[14]
[(N4-Bzdig)0,Nle14]BB(7-14)	DMVWCTL	Discovery agent	N.A.	Investigative	[15]
[(N4-Bzdig)0]BB(7-14)	DMD4BSJ	Discovery agent	N.A.	Investigative	[15]
[N40,Pro1,Tyr4,Nle 14]BB	DM6EAHF	Discovery agent	N.A.	Investigative	[15]
[N40,Pro1,Tyr4]BB	DMVFHNM	Discovery agent	N.A.	Investigative	[15]
[Tyr4]Bombesin	DMA6VNI	Discovery agent	N.A.	Investigative	[15]

References

• [1] 68Ga/177Lu-NeoBOMB1, a Novel Radiolabeled GRPR Antagonist for Theranostic Use in Oncology. J Nucl Med. 2017 Feb;58(2):293-299.
• [2] Astellas and Drais Partner To Develop Third Astellas Compound through Tacurion
• [3] Lipid modification of GRN163, an N3'-->P5' thio-phosphoramidate oligonucleotide, enhances the potency of telomerase inhibition. Oncogene. 2005 Aug 4;24(33):5262-8.
• [4] Multimodality imaging and preclinical evaluation of 177Lu-AMBA for human prostate tumours in a murine model. Anticancer Res. 2010 Oct;30(10):4039-48.
• [5] 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.
• [6] Gastrin releasing peptide antagonists with improved potency and stability. J Med Chem. 1991 Jul;34(7):2102-7.
• [7] Synthesis and biological evaluation of bombesin constrained analogues. J Med Chem. 2000 Jun 15;43(12):2356-61.
• [8] Radiopharmaceutical therapy in cancer: clinical advances and challenges. Nat Rev Drug Discov. 2020 Sep;19(9):589-608.
• [9] 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.
• [10] Expression and characterization of cloned human bombesin receptors. Mol Pharmacol. 1995 Jan;47(1):10-20.
• [11] Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry. Biochem Biophys Res Commun. 1995 Aug 15;213(2):594-9.
• [12] Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. J Pharmacol Exp Ther. 1999 Sep;290(3):1202-11.
• [13] PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94.
• [14] Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R). Biochemistry. 1999 Jun 1;38(22):7307-20.
• [15] 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.