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FGR2/3 Inhibitor

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FGR2/3 Inhibitor, Fibroblast Growth Factor Receptor 2/3 Inhibitor, Erdafitinib, Balversa

  • See Also
  1. Small Molecule Inhibitor-Mediated Chemotherapy
  2. Chemotherapy
  3. Fibroblast Growth Factor Receptor
  • Indications
  1. Bladder Cancer or Urothelial Cancer (FGR2/3+, advanced or metastatic)
  • Mechanism
  1. Fibroblast Growth Factor Receptor (FGFR)
    1. FGFR2 has 2 isoforms: Mesenchymal (activated by FGF2) and Epithelial (activated by FGF7 and 10)
      1. Mutations are associated with Craniosynostosis (Apert syndrome, crouzon syndrome)
    2. FGFR3 regulates chrondrocyte growth and cell differentiation
      1. Mutations are associated with Achondroplasia, thanatophoric dysplasia as well as neoplasms
  2. Cancers that may express FGFR Activity
    1. Urothelial carcinoma
    2. Hepatocellular Carcinoma
    3. Ovarian Cancer
    4. Lung Adenocarcinoma
  • Medications
  1. Erdafitinib (Balversa)
  • Dosing
  1. See other references for disease specific dosing protocols
  • Safety
  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters, pregnancy category X)
    1. Use reliable Contraception
  3. Monitoring
    1. Dilated Eye Exam monthly for first 4 months, then every 3 months (or as needed for Vision change)
  • Adverse Effects
  1. Central Serous Retinopathy (or Retinal Detachment)
  2. Hyperphosphatemia
  3. Hand-Foot Syndrome
  4. Oncholysis
  • Drug Interactions
  1. Avoid with CYP2C9 Inhibitors
  2. Avoid with Moderate to strong CYP3A4 inhibitors and inducers
  • Resources
  1. Erdafitinib (Dailymed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2a8aa5c0-6c92-4566-8c45-e8f4d1fc20ee
  • References
  1. Krook (2021) Br J Cancer 124(5):880-92 +PMID: 33268819 [PubMed]