General Information of Drug (ID: DMW1NKO)

Drug Name
X-82
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 ID
D0L2ZY

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]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Age-related macular degeneration
ICD Disease Classification 9B75.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Vascular endothelial growth factor receptor 1 (FLT-1) DTT FLT1 4.94E-03 0.74 1.24
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

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