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

General Information of Drug (ID: DMM5BVG)

• Drug Name: TBR-760 Drug Info
• Synonyms: CHEMBL4594435; BIM-23A760

Indication

Disease Entry	ICD 11	Status	REF
Pituitary adenoma	2F37.0	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 139593389
  TTD Drug ID: DMM5BVG

Molecule-Related Drug Atlas

Drug(s) Targeting Somatostatin receptor type 2 (SSTR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pasireotide	DMHM7JS	Cushing disease	5A70	Approved	[3]
Octreotide	DMHIDCJ	Acromegaly	5A60.0	Approved	[4]
Lanreotide acetate	DMG6ZU4	Acromegaly	5A60.0	Approved	[5]
Ga-68-DOTATOC	DMZ0P95	Diagnostic imaging	N.A.	Approved	[6]
Copper dotatate Cu-64	DM26KR1	Diagnostic imaging	N.A.	Approved	[7]
ODT-8	DMBWO5T	N. A.	N. A.	Phase 3	[8]
Paltusotine	DM97IN2	Acromegaly	5A60.0	Phase 3	[9]
Re-188-P-2045	DM614BA	Lung cancer	2C25.0	Phase 1/2	[10]
PEN-221	DMMAUOK	Neuroendocrine cancer	2B72.1	Phase 1/2	[11]
FR-121196	DMNRUGA	Alzheimer disease	8A20	Terminated	[12]

Drug(s) Targeting Dopamine D2 receptor (D2R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dopamine	DMPGUCF	Acromegaly	5A60.0	Approved	[13]
Haloperidol	DM96SE0	Delirium		Approved	[14]
Perphenazine	DMA4MRX	Schizophrenia	6A20	Approved	[15]
Perazine	DM2AOTZ	Psychotic disorder	6A20-6A25	Approved	[16]
Domperidone	DMBDPY0	Gastrointestinal disease	DE2Z	Approved	[17]
Levodopa	DMN3E57	Parkinson disease	8A00.0	Approved	[18]
Quetiapine	DM1N62C	Anorexia nervosa cachexia	6B80	Approved	[19]
Pimozide	DMW83TP	Schizophrenia	6A20	Approved	[20]
Chlorpromazine	DMBGZI3	Acute intermittent hepatic porphyria	5C58.11	Approved	[21]
Iloperidone	DM6AUFY	Schizophrenia	6A20	Approved	[22]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dopamine D2 receptor (D2R)	TTEX248	DRD2_HUMAN	Agonist	[2]
Somatostatin receptor type 2 (SSTR2)	TTZ6T9E	SSR2_HUMAN	Agonist	[2]

References

• [1] ClinicalTrials.gov (NCT04335357) TBR-760 in Adult Patients With Non-Functioning Pituitary Adenomas. U.S. National Institutes of Health.
• [2] TBR-760, a Dopamine-Somatostatin Compound, Arrests Growth of Aggressive Nonfunctioning Pituitary Adenomas in Mice. Endocrinology. 2020 Aug 1;161(8):bqaa101.
• [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: 356).
• [4] Versatile conjugation of octreotide to dendrimers by cycloaddition ("click") chemistry to yield high-affinity multivalent cyclic Peptide dendrimers. Bioconjug Chem. 2009 Jul;20(7):1323-31.
• [5] Treatment strategies for acromegaly. Expert Opin Emerg Drugs. 2005 Nov;10(4):875-90.
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [8] Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. J Med Chem. 2005 Jan 27;48(2):515-22.
• [9] Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers. Pituitary. 2022 Apr;25(2):328-339.
• [10] The somatostatin analog 188Re-P2045 inhibits the growth of AR42J pancreatic tumor xenografts. J Nucl Med. 2014 Dec;55(12):2020-5.
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] Role of somatostatin in the augmentation of hippocampal long-term potentiation by FR121196, a putative cognitive enhancer. Eur J Pharmacol. 1993 Sep 7;241(1):27-34.
• [13] The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
• [14] Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
• [15] CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
• [16] Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
• [17] Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
• [18] 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: 3639).
• [19] Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
• [20] [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
• [21] Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
• [22] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.