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

General Information of Drug (ID: DMK2GZX)

• Drug Name: Avapritinib Drug Info
• Synonyms: 1703793-34-3; UNII-513P80B4YJ; 513P80B4YJ; (1S)-1-(4-fluorophenyl)-1-[2-[4-[6-(1-methylpyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]piperazin-1-yl]pyrimidin-5-yl]ethanamine; Avapritinib [INN]; BLU-285 (Avapritinib); SCHEMBL16652297; EX-A1366; BCP20175; CS-7577; ACN-051245; HY-101561; (S)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazin-1-yl)pyrimidin-5-yl)ethanamine

Indication

Disease Entry	ICD 11	Status	REF
Gastrointestinal stromal tumour	2B5B	Approved	[1]
Mast cell leukaemia	2A21.00	Phase 1	[2]
Systemic mastocytosis	2A21.0	Phase 1	[3]

• Cross-matching ID:
  PubChem CID: 118023034
  CAS Number: CAS 1703793-34-3
  TTD Drug ID: DMK2GZX
  ACDINA Drug ID: D01518

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]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[7]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[8]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]
MP470	DMELUAK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
MEDI-575	DMI9WVM	Glioblastoma multiforme	2A00.0	Phase 2	[12]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[13]

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]

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [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] 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.
• [8] 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.
• [9] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [10] National Cancer Institute Drug Dictionary (drug id 452042).
• [11] 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.
• [12] Clinical pipeline report, company report or official report of MedImmune (2011).
• [13] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.