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

General Information of Drug (ID: DMD965S)

• Drug Name: Quinazoline derivative 15 Drug Info
• Synonyms: PMID27646564-Compound-12-1
• Cross-matching ID: TTD Drug ID: DMD965S

Molecule-Related Drug Atlas

Drug(s) Targeting Proto-oncogene c-Ret (RET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[2]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[3]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[3]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[4]
Selpercatinib	DMZR15V	Non-small-cell lung cancer	2C25.Y	Approved	[5]
Pralsetinib	DMWU0I2	Non-small-cell lung cancer	2C25.Y	Approved	[6]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[7]
CEP-32496	DMAO04B	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[8]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[9]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[10]

Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[11]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[12]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[3]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[13]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[14]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[4]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[15]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[16]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[17]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Proto-oncogene c-Ret (RET)	TT4DXQT	RET_HUMAN	Inhibitor	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[1]

References

• [1] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [2] Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [4] 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.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [7] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2185).
• [8] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [9] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] 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.
• [12] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [13] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [14] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [15] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [16] Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
• [17] Clinical pipeline report, company report or official report of Exelixis (2011).
• [18] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services