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

General Information of Drug (ID: DM37I92)

• Drug Name: RPR-108514A Drug Info
• Synonyms: CHEMBL543669; RPR-108514A

Indication

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

• Cross-matching ID:
  PubChem CID: 18770833
  TTD Drug ID: DM37I92

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

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	[12]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[2]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[13]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[14]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[15]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[16]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[17]

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	[1]
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Inhibitor	[1]

References

• [1] The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-d]pyrimidines, inhibitors of CSF-1R tyrosine kinase activity, Bioorg. Med. Chem. Lett. 7(4):421-424 (1997).
• [2] 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.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [4] 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.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [6] 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.
• [7] 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.
• [8] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [9] National Cancer Institute Drug Dictionary (drug id 452042).
• [10] 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.
• [11] Clinical pipeline report, company report or official report of MedImmune (2011).
• [12] 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.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [14] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [15] Company report (Neuronova)
• [16] 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.
• [17] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.