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

General Information of Drug (ID: DMH1PQ0)

• Drug Name: CEP-2563 Drug Info
• Synonyms: KT-8391; L-Lysyl-beta-alanine 9(S),12(R)-Epoxy-10(S)-methoxy-9-methyl-1-oxo-2,3,9,10,11,12-hexahydro-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-10-ylmethyl ester dihydrochloride

Indication

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

• Cross-matching ID:
  PubChem CID: 9831755
  TTD Drug ID: DMH1PQ0

Molecule-Related Drug Atlas

Drug(s) Targeting NT-3 growth factor receptor (TrkC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Entrectinib	DMMPTLH	Non-small-cell lung cancer	2C25	Approved	[4]
Larotrectinib	DM26CQR	Solid tumour/cancer	2A00-2F9Z	Approved	[5]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[6]
Altiratinib	DMUJCBT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
PMID28270021-Compound-WO2016054807Example1	DMD5QEL	Chronic pain	MG30	Patented	[8]
PMID28270010-Compound-Figure24-b	DM0QHLK	N. A.	N. A.	Patented	[7]
Pyrrolo[2,3-d]pyrimidine derivative 4	DME0WSR	Chronic pain	MG30	Patented	[8]
3-amino-5-benzyl-substituted indazole derivative 1	DMFDURZ	Chronic pain	MG30	Patented	[8]
PMID28270010-Compound-Figure5-1	DM2YAPJ	N. A.	N. A.	Patented	[7]
PMID28270021-Compound-WO2015042088Example4	DM6KXOQ	Chronic pain	MG30	Patented	[8]

Drug(s) Targeting Platelet-derived growth factor receptor alpha (PDGFRA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[9]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[10]
Olaratumab	DMNYOIX	Soft tissue sarcoma	2B57	Approved	[11]
Avapritinib	DMK2GZX	Gastrointestinal stromal tumour	2B5B	Approved	[12]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[13]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[14]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[15]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[16]
MP470	DMELUAK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[17]
MEDI-575	DMI9WVM	Glioblastoma multiforme	2A00.0	Phase 2	[18]

Drug(s) Targeting Platelet-derived growth factor receptor beta (PDGFRB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[19]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[9]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[20]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[13]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[15]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[16]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[6]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[21]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[22]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[23]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
NT-3 growth factor receptor (TrkC)	TTXABCW	NTRK3_HUMAN	Modulator	[2]
Platelet-derived growth factor receptor alpha (PDGFRA)	TT8FYO9	PGFRA_HUMAN	Inhibitor	[2]
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Inhibitor	[3]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007988)
• [2] Phase I clinical trial of CEP-2563 dihydrochloride, a receptor tyrosine kinase inhibitor, in patients with refractory solid tumors. Invest New Drugs. 2004 Nov;22(4):449-58.
• [3] Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [5] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [6] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [7] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
• [8] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part II.Expert Opin Ther Pat. 2017 Jul;27(7):831-849.
• [9] Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
• [10] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [11] A phase I study of olaratumab, an anti-platelet-derived growth factor receptor alpha (PDGFRalpha) monoclonal antibody, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Mar;73(3):595-604.
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [13] E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
• [14] The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.
• [15] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [16] National Cancer Institute Drug Dictionary (drug id 452042).
• [17] Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
• [18] Clinical pipeline report, company report or official report of MedImmune (2011).
• [19] Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
• [20] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [21] Company report (Neuronova)
• [22] Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
• [23] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.