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

General Information of Drug (ID: DMW1NKO)

• Drug Name: X-82 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Age-related macular degeneration	9B75.0	Phase 2	[1]
Macular degeneration	9B78.3	Phase 1	[2]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

• Cross-matching ID: TTD Drug ID: DMW1NKO

Molecule-Related Drug Atlas

Drug(s) Targeting Vascular endothelial growth factor receptor (VEGFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[5]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[4]
Fruquintinib	DMHOSCQ	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
KH-902	DM8VO16	Diabetic macular edema	9B71.02	Phase 3	[6]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[7]
BAY-57-9352	DMVA5NS	Gastric adenocarcinoma	2B72	Phase 2	[8]
Vorolanib	DMIM1U9	Non-small cell lung cancer	2C25	Phase 2	[9]
BFH-772	DMVUX1C	Psoriasis vulgaris	EA90	Phase 2	[10]
ASP-8477	DMBZQS7	Neuropathic pain	8E43.0	Phase 2	[11]
AG-013958	DMRET3H	Age-related macular degeneration	9B75.0	Phase 1/2	[12]

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	[13]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[14]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[5]
CT-102	DMB8PF3	Diabetic foot ulcer	BD54	Approved	[15]
Trapidil	DMY67U8	Acute coronary syndrome	BA41	Phase 4	[16]
Rosiglitazone + metformin	DMPIDXT	Diabetic complication	5A2Y	Phase 3	[13]
TKI258	DMYLT67	Renal cell carcinoma	2C90	Phase 3	[13]
BAY-57-9352	DMVA5NS	Gastric adenocarcinoma	2B72	Phase 2	[13]
Vorolanib	DMIM1U9	Non-small cell lung cancer	2C25	Phase 2	[9]
PMID25623274-Compound-WO2014132220C2	DMXEZWP	Pulmonary arterial hypertension	BB01.0	Patented	[17]

Drug(s) Targeting Vascular endothelial growth factor receptor 1 (FLT-1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[18]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[19]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[20]
Fruquintinib	DMHOSCQ	Solid tumour/cancer	2A00-2F9Z	Phase 3	[21]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[22]
OCV-101	DMT9QI2	Pancreatic cancer	2C10	Phase 2	[23]
LY3012212	DMRVEHY	Arteriosclerosis	BD40	Phase 2	[24]
OTSGC-A24	DMN0ZQ5	Colorectal cancer	2B91.Z	Phase 1/2	[25]
CEP-11981	DMYDTJ6	Solid tumour/cancer	2A00-2F9Z	Phase 1	[26]
EW-A-401	DM3VC6T	Peripheral vascular disease	BD4Z	Phase 1	[27]

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	Modulator	[3]
Vascular endothelial growth factor receptor (VEGFR)	TTVJ1D8	NOUNIPROTAC	Inhibitor	[4]
Vascular endothelial growth factor receptor 1 (FLT-1)	TT2Q6G1	VGFR1_HUMAN	Modulator	[3]

References

• [1] ClinicalTrials.gov (NCT02348359) X-82 to Treat Age-related Macular Degeneration. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of Tyrogenex.
• [3] National Cancer Institute Drug Dictionary (drug id 695817).
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [6] Effects of intravitreal injection of KH902, a vascular endothelial growth factor receptor decoy, on the retinas of streptozotocin-induced diabetic rats. Diabetes Obes Metab. 2012 Jul;14(7):644-53.
• [7] National Cancer Institute Drug Dictionary (drug id 452042).
• [8] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [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] CA patent application no. 841416, Method of selecting therapeutic indications.
• [11] ClinicalTrials.gov (NCT02065349) A Study Into Pain Relief Given by ASP8477 for Peripheral Neuropathic Pain (Either Post-herpetic Neuralgia or Painful Diabetic Peripheral Neuropathy) and Its Safety. U.S. National Institutes of Health.
• [12] Receptor Tyrosine Kinase Inhibitors AG013764 and AG013711 Reduce Choroidal Neovascularization in Rat Eye. Exp Eye Res. 2007 May; 84(5): 922-933.
• [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] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [15] Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
• [16] 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.
• [17] Evaluation of WO-2014132220, selective PDGFR inhibitors for the treatment of pulmonary arterial hypertension.Expert Opin Ther Pat. 2015 Apr;25(4):493-9.
• [18] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
• [19] 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.
• [20] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [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] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [23] Phase I trial of OTS11101, an anti-angiogenic vaccine targeting vascular endothelial growth factor receptor 1 in solid tumor.Cancer Sci.2013 Jan;104(1):98-104.
• [24] Icrucumab, a fully human monoclonal antibody against the vascular endothelial growth factor receptor-1, in the treatment of patients with advanced solid malignancies: a Phase 1 study. Invest New Drugs. 2014 Apr;32(2):303-11.
• [25] J Clin Oncol 33, 2015 (suppl 3; abstr 65).
• [26] 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: 8189).
• [27] DOI: http://dx.doi.org/10.1016/j.tips.2014.09.007