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

General Information of Drug (ID: DMZAL8C)

• Drug Name: Motesanib Drug Info
• Synonyms: N-(2,3-dihydro-3,3-dimethyl-1H-indol-6-yl)-2-((4-pyridinylmethyl)amino)-3-pyridinecarboxamide; N-(3,3-dimethyl-2,3-dihydro-1H-indol-6-yl)-2-[(pyridin-4-ylmethyl)amino]pyridine-3-carboxamide

Indication

Disease Entry	ICD 11	Status	REF
Non-small-cell lung cancer	2C25.Y	Discontinued in Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 11667893
  ChEBI ID: CHEBI:51098
  CAS Number: CAS 453562-69-1
  TTD Drug ID: DMZAL8C

Molecule-Related Drug Atlas

Drug(s) Targeting Platelet-derived growth factor receptor (PDGFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[3]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[4]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[5]
CT-102	DMB8PF3	Diabetic foot ulcer	BD54	Approved	[6]
Trapidil	DMY67U8	Acute coronary syndrome	BA41	Phase 4	[7]
TKI258	DMYLT67	Renal cell carcinoma	2C90	Phase 3	[3]
BAY-57-9352	DMVA5NS	Gastric adenocarcinoma	2B72	Phase 2	[3]
X-82	DMW1NKO	Age-related macular degeneration	9B75.0	Phase 2	[8]
Vorolanib	DMIM1U9	Non-small-cell lung cancer	2C25	Phase 2	[9]
PMID25623274-Compound-WO2014132220C2	DMXEZWP	Pulmonary arterial hypertension	BB01.0	Patented	[10]

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	[11]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[12]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[13]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[13]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[4]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[14]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[15]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[16]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[17]

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	[18]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[13]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[19]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[20]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[3]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[4]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[21]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[22]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[23]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Platelet-derived growth factor receptor (PDGFR)	TTI2WET	NOUNIPROTAC	Inhibitor	[2]
Tyrosine-protein kinase Kit (KIT)	TTX41N9	KIT_HUMAN	Inhibitor	[2]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[2]

References

• [1] 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. (Ligand id: 5660).
• [2] Clinical pipeline report, company report or official report of Amgen (2009).
• [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] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [5] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [6] Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
• [7] Osteitis fibrosa is mediated by Platelet-Derived Growth Factor-A via a phosphoinositide 3-kinase-dependent signaling pathway in a rat model for chr... Endocrinology. 2008 Nov;149(11):5735-46.
• [8] National Cancer Institute Drug Dictionary (drug id 695817).
• [9] Vorolanib, an oral VEGFR/PDGFR dual tyrosine kinase inhibitor for treatment of patients with advanced solid tumors: An open-label, phase I dose escalation and dose expansion trial. Chin J Cancer Res. 2021 Feb 28;33(1):103-114.
• [10] Evaluation of WO-2014132220, selective PDGFR inhibitors for the treatment of pulmonary arterial hypertension.Expert Opin Ther Pat. 2015 Apr;25(4):493-9.
• [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] 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.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [16] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [17] National Cancer Institute Drug Dictionary (drug id 452042).
• [18] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [19] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [20] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [21] 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.
• [22] Clinical pipeline report, company report or official report of Exelixis (2011).
• [23] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services