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

General Information of Drug (ID: DMRKE9G)

• Drug Name: SRI-62-834 Drug Info
• Synonyms: CRC-8605; Rac-2-[Hydroxy[2-(octadecyloxymethyl)tetrahydrofuran-2-ylmethoxy]phosphinyloxy]-N,N,N-trimethylethylamminium hydroxyde,inner salt P-oxide

Indication

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

• Cross-matching ID:
  PubChem CID: 130724
  CAS Number: CAS 113201-37-9
  TTD Drug ID: DMRKE9G

Molecule-Related Drug Atlas

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	[4]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[5]
Olaratumab	DMNYOIX	Soft tissue sarcoma	2B57	Approved	[6]
Avapritinib	DMK2GZX	Gastrointestinal stromal tumour	2B5B	Approved	[7]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[8]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[9]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
MP470	DMELUAK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]
MEDI-575	DMI9WVM	Glioblastoma multiforme	2A00.0	Phase 2	[13]

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	[14]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[4]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[15]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[8]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[16]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[17]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[18]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
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 800000818)
• [2] Antitumor activity of SRI 62-834, a cyclic ether analog of ET-18-OCH3. Lipids. 1987 Nov;22(11):884-90.
• [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] 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.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [6] 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.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [8] 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.
• [9] 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.
• [10] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [11] National Cancer Institute Drug Dictionary (drug id 452042).
• [12] 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.
• [13] Clinical pipeline report, company report or official report of MedImmune (2011).
• [14] 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.
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [16] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [17] Company report (Neuronova)
• [18] 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.
• [19] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.