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

General Information of Drug (ID: DM958QB)

• Drug Name: Ripretinib Drug Info
• Synonyms: 1442472-39-0; Ripretinib [USAN]; UNII-9XW757O13D; GTPL9175; SCHEMBL14999718; 9XW757O13D; HY-112306; CS-0044835; N-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-N'-phenylurea; 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea; Urea, N-(4-bromo-5-(1-ethyl-1,2-dihydro-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl)-2-fluorophenyl)-N'-phenyl-

Indication

Disease Entry	ICD 11	Status	REF
Gastrointestinal stromal tumour	2B5B	Approved	[1]
Glioma	2A00.0	Phase 1	[2]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]
Systemic mastocytosis	2A21.0	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 71584930
  CAS Number: CAS 1442472-39-0
  TTD Drug ID: DM958QB
  ACDINA Drug ID: D01395

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	[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]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[12]

Drug(s) Targeting Tyrosine-protein kinase Kit (KIT)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[13]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[14]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[15]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[16]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[16]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[17]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[18]
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]

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]
Tyrosine-protein kinase Kit (KIT)	TTX41N9	KIT_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] 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.
• [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] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [13] A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
• [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] New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
• [16] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [17] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [18] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019