Target intelligence / Profile preview

VEGFR1-3, FGFR1-4, RET, KIT, PDGFRα

Target
VEGFR1-3, FGFR1-4, RET, KIT, PDGFRα
Molecular classification
Receptor tyrosine kinase, Enzyme, Receptor
01

Overview

These targets are a group of receptor tyrosine kinases including the vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), fibroblast growth factor receptors (FGFR1-4), RET proto-oncogene, KIT (CD117), and platelet-derived growth factor receptor alpha (PDGFRα). They are crucial regulators of angiogenesis, cell proliferation, differentiation, and survival. Multi-targeted tyrosine kinase inhibitors such as lenvatinib, regorafenib, and sunitinib inhibit these receptors to suppress tumor angiogenesis and tumor growth. These targets play prominent roles in the pathogenesis of various cancers and proliferative diseases, making them key therapeutic targets, but with notable safety challenges due to the broad role of these kinases in normal physiologic processes

Other names
FLT1KDRFLK1FLT4c-KitCD117CD140a
02

Mechanism of action

Inhibition of tyrosine kinase activity; Blockade of growth factor-mediated signal transduction; Suppression of tumor angiogenesis; Inhibition of tumor cell proliferation and survival.

03

Biological functions

Signal transductionAngiogenesisCell proliferationCell differentiationCell survivalMigration and metastasis
04

Disease associations

CancerAngiogenesis-related diseasesThyroid cancerRenal cell carcinomaHepatocellular carcinomaGastrointestinal stromal tumorsOther proliferative disorders
05

Safety considerations

HypertensionDiarrheaFatigueHypothyroidismHand-foot syndromeProteinuriaIncreased risk of hemorrhage and impaired wound healingGastrointestinal toxicityCardiac toxicity
06

Interacting drugs

Lenvatinib

9 more in the full profile.

07

Biomarkers

Microvessel densityPhosphorylated forms of the receptorsExpression levels of VEGF, FGF, PDGF, and their receptors

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