Erdafitinib | FGFR inhibitor

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Erdafitinib (1346242-81-6) is a potent (IC50s = 1.2 nM FGFR1, 2.5 nM FGFR2, 3 nM FGFR3, 5.7 nM FGFR4) and selective pan-inhibitor of FGFR.1 Alone and in combination with PD-1 blockade it increased T-cell infiltration, decreased Treg cells, and down-regulation of PD-L1 expression leading to enhanced antitumor immunity and survival in a lung cancer model.2 Erdafitinib elicited antitumor responses through direct inhibition of oncogenic signaling as well as normalization of the tumor microenvironment in various cancer models including bladder (for which it is FDA approved)3, triple negative breast4, and pancreatic5.

References/Citations:

  1. Perera et al. (2017), Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), A Functionally Selective Small-Molecule FGFR Family Inhibitor; Mol. Cancer Ther. 16 1010
  2. Palakurthi et al. (2019); The Combined Effect of FGFR Inhibition and PD-1 Blockade Promotes Tumor-Intrinsic Induction of Antitumor Immunity, Cancer Immunol. Res. 7 1457
  3. Lee and Seo (2021); Fibroblast Growth Factor Inhibitors for Treating Locally Advanced/Metastatic Bladder Urothelial Carcinomas via Dual Targeting of Tumor-Specific Oncogenic Signaling and the Tumor Immune Microenvironment, Int. J. Mol. Sci.. 22 9526
  4. Wu et al. (2022); FGFR blockade boosts T cell infiltration into triple-negative breast cancer by regulating cancer-associated fibroblasts, Theranostics 12 4564
  5. Ng et al. (2022); Exceptional Response to Erdafitinib in FGFR2-Mutated Metastatic Pancreatic Ductal Adenocarcinoma, J. Natl. Compr. Canc. Netw. 20 1076
1346242-81-6, Erdafitinib, Erdafitinib supplier, FGFR inhibitor, JNJ-42756493, pan-FGFR inhibitor
Alternate Name:
JNJ-42756493

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Erdafitinib (1346242-81-6) is a potent (IC50s = 1.2 nM FGFR1, 2.5 nM FGFR2, 3 nM FGFR3, 5.7 nM FGFR4) and selective pan-inhibitor of FGFR.1 Alone and in combination with PD-1 blockade it increased T-cell infiltration, decreased Treg cells, and down-regulation of PD-L1 expression leading to enhanced antitumor immunity and survival in a lung cancer model.2 Erdafitinib elicited antitumor responses through direct inhibition of oncogenic signaling as well as normalization of the tumor microenvironment in various cancer models including bladder (for which it is FDA approved)3, triple negative breast4, and pancreatic5.

References/Citations:

  1. Perera et al. (2017), Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), A Functionally Selective Small-Molecule FGFR Family Inhibitor; Mol. Cancer Ther. 16 1010
  2. Palakurthi et al. (2019); The Combined Effect of FGFR Inhibition and PD-1 Blockade Promotes Tumor-Intrinsic Induction of Antitumor Immunity, Cancer Immunol. Res. 7 1457
  3. Lee and Seo (2021); Fibroblast Growth Factor Inhibitors for Treating Locally Advanced/Metastatic Bladder Urothelial Carcinomas via Dual Targeting of Tumor-Specific Oncogenic Signaling and the Tumor Immune Microenvironment, Int. J. Mol. Sci.. 22 9526
  4. Wu et al. (2022); FGFR blockade boosts T cell infiltration into triple-negative breast cancer by regulating cancer-associated fibroblasts, Theranostics 12 4564
  5. Ng et al. (2022); Exceptional Response to Erdafitinib in FGFR2-Mutated Metastatic Pancreatic Ductal Adenocarcinoma, J. Natl. Compr. Canc. Netw. 20 1076