General Information of the Drug (ID: M6APDG00882)
Name
Famitinib
Synonyms
Receptor tyrosine kinase inhibitors (cancer); SHR-1020; Receptor tyrosine kinase inhibitors (cancer), Shanghai Hengrui; Tyrosine-kinase inhibitor (oral, cancer), Jiangsu Hengrui; C-Kit/VEGFR2/PDGFR/VEGFR3/Flt1/Flt3 inhibitor (oral, cancer), Jiangsu Hengrui
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Status
Phase 2
Structure
Formula
C23H27FN4O2
InChI
1S/C23H27FN4O2/c1-4-27(5-2)10-11-28-9-8-19-21(23(28)30)14(3)20(25-19)13-17-16-12-15(24)6-7-18(16)26-22(17)29/h6-7,12-13,25H,4-5,8-11H2,1-3H3,(H,26,29)/b17-13-
InChIKey
GKEYKDOLBLYGRB-LGMDPLHJSA-N
PubChem CID
16662431
TTD Drug ID
D0Z6MT
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Platelet-derived growth factor receptor alpha (PDGFRA)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Platelet-derived growth factor receptor alpha (PDGFRA) is a therapeutic target for Famitinib. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Famitinib through regulating the expression of Platelet-derived growth factor receptor alpha (PDGFRA). [1], [2]
Platelet-derived growth factor receptor beta (PDGFRB)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Platelet-derived growth factor receptor beta (PDGFRB) is a therapeutic target for Famitinib. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Famitinib through regulating the expression of Platelet-derived growth factor receptor beta (PDGFRB). [3], [4]
References
Ref 1 METTL3-mediated N (6)-methyladenosine modification governs pericyte dysfunction during diabetes-induced retinal vascular complication. Theranostics. 2022 Jan 1;12(1):277-289. doi: 10.7150/thno.63441. eCollection 2022.
Ref 2 The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations. Invest New Drugs. 2015 Apr;33(2):300-9. doi: 10.1007/s10637-015-0205-y. Epub 2015 Jan 20.
Ref 3 Mutant NPM1-Regulated FTO-Mediated m(6)A Demethylation Promotes Leukemic Cell Survival via PDGFRB/ERK Signaling Axis. Front Oncol. 2022 Feb 8;12:817584. doi: 10.3389/fonc.2022.817584. eCollection 2022.
Ref 4 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. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6.