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VEGFR1-3, FGFR1-4, PDGFRα, RET, KIT

Target: VEGFR1-3, FGFR1-4, PDGFRα, RET, KIT
Molecular classification: Receptor, Tyrosine kinase, Growth factor receptor, Enzyme (specifically, kinase)

Overview

This group of targets consists of growth factor binding receptor tyrosine kinases: VEGFR1-3 (key effectors for vascular endothelial growth factor, regulating angiogenesis and lymphangiogenesis), FGFR1-4 (receptors for fibroblast growth factors, important for development and cancer cell proliferation), PDGFRα (cell growth, angiogenesis), RET (proto-oncogene receptor, often aberrantly activated in cancers), and KIT (stem cell growth factor receptor involved in hematopoiesis and mutations found in gastrointestinal tumors). These kinases are major therapeutic targets in oncology, particularly in solid tumors, due to their roles in neovascularization and tumor growth. Several drugs approved for cancer therapy target multiple members of this receptor group simultaneously to block signaling redundancy and enhance clinical efficacy.

Other names: VEGFR: FLT1 (VEGFR1)VEGFR: KDR (VEGFR2)VEGFR: FLT4 (VEGFR3)FGFR: CD331 (FGFR1)FGFR: CD332 (FGFR2)FGFR: CD333 (FGFR3)FGFR: CD334 (FGFR4)PDGFRα: PDGFRARET: RET proto-oncogeneKIT: CD117KIT: stem cell growth factor receptor (SCFR)KIT: c-KIT

Mechanism of action

Inhibition of receptor tyrosine kinase activity; Blockade of downstream VEGF, FGF, PDGF, and SCF signaling pathways; Anti-angiogenesis; Suppression of tumor cell proliferation and migration

Biological functions

Signal transductionCell proliferationAngiogenesisLymphangiogenesisCell survivalCell migrationApoptosis regulation

Disease associations

CancerTumor angiogenesisInflammationOther proliferative disorders

Safety considerations

HypertensionFatigueDiarrheaHypothyroidismRisk of hemorrhageProteinuriaCardiotoxicityOff-target toxicities (class-wide)

Interacting drugs

Lenvatinib

7 more in the full profile.

Biomarkers

Overexpression or mutation of VEGFRs, FGFRs, PDGFRα, RET, or KIT in tumor tissueVEGF, FGF levelsCD117 immunostaining for KITRET mutations/rearrangementsOthers as relevant for each component

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