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

General Information of Drug (ID: DM1EGC3)

• Drug Name: H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2 Drug Info
• Synonyms: CHEMBL262017; H-D-Phe-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH2

Indication

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

• Cross-matching ID:
  PubChem CID: 44403230
  TTD Drug ID: DM1EGC3

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	[2]
Octreotide	DMHIDCJ	Acromegaly	5A60.0	Approved	[3]
Lanreotide acetate	DMG6ZU4	Acromegaly	5A60.0	Approved	[4]
Ga-68-DOTATOC	DMZ0P95	Diagnostic imaging	N.A.	Approved	[5]
Copper dotatate Cu-64	DM26KR1	Diagnostic imaging	N.A.	Approved	[6]
ODT-8	DMBWO5T	N. A.	N. A.	Phase 3	[7]
Paltusotine	DM97IN2	Acromegaly	5A60.0	Phase 3	[8]
TBR-760	DMM5BVG	Pituitary adenoma	2F37.0	Phase 2	[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]

Drug(s) Targeting Somatostatin receptor type 5 (SSTR5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pasireotide	DMHM7JS	Cushing disease	5A70	Approved	[12]
ODT-8	DMBWO5T	N. A.	N. A.	Phase 3	[7]
FR-121196	DMNRUGA	Alzheimer disease	8A20	Terminated	[13]
SOMATOSTATIN	DMIOFQE	Acromegaly	5A60.0	Investigative	[1]
Des-AA1,2,5-[D-Trp8,Tyr11]SRIF	DM7MZ2V	Discovery agent	N.A.	Investigative	[14]
Des-AA1,2,5,12,13-[D-Trp8]SRIF	DM1KJAE	Discovery agent	N.A.	Investigative	[7]
SRIF-28	DM0OM9L	Discovery agent	N.A.	Investigative	[15]
99mTc-MIP-1407	DMYPD5L	Neuroendocrine cancer	2B72.1	Investigative	[12]
Des-AA1,2,4,12,13-[D-Trp8]SRIF	DMMWDC5	Discovery agent	N.A.	Investigative	[7]
Cytotoxin Peptide Conjugate	DM7SVLZ	Discovery agent	N.A.	Investigative	[16]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Somatostatin receptor type 2 (SSTR2)	TTZ6T9E	SSR2_HUMAN	Inhibitor	[1]
Somatostatin receptor type 5 (SSTR5)	TT2BC4G	SSR5_HUMAN	Inhibitor	[1]

References

• [1] Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from ... J Med Chem. 2005 Oct 20;48(21):6643-52.
• [2] 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).
• [3] 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.
• [4] Treatment strategies for acromegaly. Expert Opin Emerg Drugs. 2005 Nov;10(4):875-90.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [7] Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides. J Med Chem. 2005 Jan 27;48(2):515-22.
• [8] 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.
• [9] TBR-760, a Dopamine-Somatostatin Compound, Arrests Growth of Aggressive Nonfunctioning Pituitary Adenomas in Mice. Endocrinology. 2020 Aug 1;161(8):bqaa101.
• [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] 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: 359).
• [13] 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.
• [14] Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. J Med Chem. 2005 Jan 27;48(2):507-14.
• [15] Novel octreotide dicarba-analogues with high affinity and different selectivity for somatostatin receptors. J Med Chem. 2010 Aug 26;53(16):6188-97.
• [16] An adjustable release rate linking strategy for cytotoxin-peptide conjugates. Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803.