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

General Information of Drug (ID: DM5DZEL)

• Drug Name: PLX9486 Drug Info
• Synonyms: CGT9486

Indication

Disease Entry	ICD 11	Status	REF
Gastrointestinal stromal tumour	2B5B	Phase 1/2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 75593308
  TTD Drug ID: DM5DZEL

Molecule-Related Drug Atlas

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	[3]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[4]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[5]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[6]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[6]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[7]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[8]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[9]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tyrosine-protein kinase Kit (KIT)	TTX41N9	KIT_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT02401815) CGT9486 (Formerly Known as PLX9486) as a Single Agent and in Combination With PLX3397 (Pexidartinib) or Sunitinib in Participants With Advanced Solid Tumors. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] 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.
• [4] 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.
• [5] 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.
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [7] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [8] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [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).