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

General Information of Drug (ID: DMF2CZ9)

• Drug Name: OSI-930 Drug Info
• Synonyms: OSI 930; OSI930; OSI-930 is a multi-targeted tyrosine kinase inhibitor; 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide

Indication

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

• Therapeutic Class: Anticancer Agents
• Cross-matching ID:
  PubChem CID: 9868037
  ChEBI ID: CHEBI:91433
  CAS Number: CAS 728033-96-3
  TTD Drug ID: DMF2CZ9

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	Hepatocellular carcinoma	2C12.02	Approved	[4]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[5]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	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]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[4]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[12]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[6]
Sunitinib	DMCBJSR	Gastrointestinal cancer	2C11	Approved	[13]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[14]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[3]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[7]
Cabozantinib	DMIYDT4	Thyroid cancer	2D10	Approved	[15]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[16]
Lenvatinib	DMB1IU4	Thyroid cancer	2D10	Approved	[17]

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	Modulator	[1] , [2]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Modulator	[1] , [2]

References

• [1] OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74.
• [2] Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9.
• [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).
• [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] Clinical pipeline report, company report or official report of Exelixis (2011).
• [16] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
• [17] Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.