Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTVJ1D8)

• DTT Name: Vascular endothelial growth factor receptor (VEGFR)
• Gene Name: VEGFR
• DTT Type: Successful target; [1]
• BioChemical Class: Kinase
• UniProt ID: NOUNIPROTAC
• TTD ID: T31946
• KEGG Pathway:
  Ras signaling pathway (hsa04014)
  Rap1 signaling pathway (hsa04015)
  Cytokine-cytokine receptor interaction (hsa04060)
  HIF-1 signaling pathway (hsa04066)
  Endocytosis (hsa04144)
  PI3K-Akt signaling pathway (hsa04151)
  Focal adhesion (hsa04510)
  Transcriptional misregulation in cancer (hsa05202)
  Rheumatoid arthritis (hsa05323)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[1]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[2]

12 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ABP 938	DM00ACQ	Neovascular age-related macular degeneration	9B78.3Z	Phase 3	[3]
KH-902	DM8VO16	Diabetic macular edema	9B71.02	Phase 3	[4]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[1]
ASP-8477	DMBZQS7	Neuropathic pain	8E43.0	Phase 2	[5]
BAY-57-9352	DMVA5NS	Gastric adenocarcinoma	2B72	Phase 2	[6]
BFH-772	DMVUX1C	Psoriasis vulgaris	EA90	Phase 2	[7]
Vorolanib	DMIM1U9	Non-small-cell lung cancer	2C25	Phase 2	[8]
X-82	DMW1NKO	Age-related macular degeneration	9B75.0	Phase 2	[1]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
AG-013958	DMRET3H	Age-related macular degeneration	9B75.0	Phase 1/2	[10]
AIV001	DML0GIU	Basal cell carcinoma	2C32	Phase 1/2	[11]
XL092	DM3LRAC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[12]

5 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
HuMV833	DM9LY4Q	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[13]
AZD-9935	DMFE3CD	Solid tumour/cancer	2A00-2F9Z	Terminated	[14]
Genevx	DM6JNV3	Angina pectoris	BA40	Terminated	[15]
RG-8803	DMI0CYV	Diabetic retinopathy	9B71.0	Terminated	[16]
ZD-4190	DMVWRU9	Solid tumour/cancer	2A00-2F9Z	Terminated	[17]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [3] Clinical pipeline report, company report or official report of Amgen
• [4] 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.
• [5] 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.
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] CA patent application no. 841416, Method of selecting therapeutic indications.
• [8] 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.
• [9] National Cancer Institute Drug Dictionary (drug id 452042).
• [10] Receptor Tyrosine Kinase Inhibitors AG013764 and AG013711 Reduce Choroidal Neovascularization in Rat Eye. Exp Eye Res. 2007 May; 84(5): 922-933.
• [11] Clinical pipeline report, company report or official report of AiViva BioPharma.
• [12] Clinical pipeline report, company report or official report of Exelixis.
• [13] Molecular imaging and biological evaluation of HuMV833 anti-VEGF antibody: implications for trial design of antiangiogenic antibodies. J Natl Cancer Inst. 2002 Oct 2;94(19):1484-93.
• [14] WO patent application no. 2009,0582,67, Benzomorpholine derivatives and methods of use.
• [15] Vascular Endothelial Growth Factor Gene Therapy Increases Survival, Promotes Lung Angiogenesis, and Prevents Alveolar Damage in Hyperoxia-Induced Lung Injury. Circulation. 2005; 112: 2477-2486.
• [16] US patent application no. 2010,0278,784, Methods and compositions for treating skin conditions.
• [17] ZD4190: an orally active inhibitor of vascular endothelial growth factor signaling with broad-spectrum antitumor efficacy. Cancer Res. 2000 Feb 15;60(4):970-5.