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Abbreviations:

4-1BB, tumor necrosis factor receptor superfamily member 9; ALL, acute lymphoblastic leukemia; AML, acute myeloid leukemia; APRIL, a proliferation inducing ligand; BAFF, B-cell activating factor from the tumor necrosis factor family; BAK, Bcl-2 homologous antagonist killer; BAX, Bcl-2-associated X protein; BCL-2, B-cell lymphoma 2; BCMA, B-cell maturation antigen; BCR, B-cell receptor; BH, Bcl-2 homology domain; BiTE, Bispecific T-cell Engager; C5, complement component 5; CD, cluster of differentiation; CIT, chemotherapy-induced thrombocytopenia; CLDN18.2, Claudin-18 isoform 2; DARPin, designed ankyrin repeat proteins; DLBCL, diffuse large B-cell lymphoma; DLL3, delta-like protein 3; EGFR, epidermal growth factor receptor; EGFRvIII, epidermal growth factor receptor variant III; Fab, fragment antigen-binding; FAP, fibroblast activation protein; Fc, fragment crystallizable; FLT3, fms-like tyrosine kinase 3; GEJ, gastroesophageal junction; GM-CSF, granulocyte-macrophage colony-stimulating factor; GvHD, graft versus host disease; HCC, hepatocellular carcinoma; HLE, half-life extended; IL-2R, interleukin 2 receptor; IL-21R, interleukin 21 receptor; IL-2Rα, interleukin 2 receptor alpha; KRAS, Kirsten rat sarcoma; MAC, membrane attack complex; MCL-1, myeloid cell leukemia-1; mCRPC, metastatic castration-resistant prostate cancer; MetMel, metastatic melanoma; MM, multiple myeloma; MOA, mechanism of action; MUC17, mucin 17; NHL, non-Hodgkin's lymphoma; NSCLC, non-small cell lung cancer; PD-1, programmed cell death protein 1; PD-L1, programmed cell death ligand 1; PD-L2, programmed cell death ligand 2; PNH, paroxysmal nocturnal hemoglobinuria; PSA, prostate-specific antigen; PSMA, prostate-specific membrane antigen; RAS, rat sarcoma; R/R, relapsed or refractory; SCLC, small cell lung cancer; STEAP1, six-transmembrane epithelial antigen of prostate 1; TPO, thrombopoietin; TPO-R, thrombopoietin receptor; Treg, regulatory T cell.

Amgen Oncology
Pipeline

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SOLID MALIGNANCIES

MALIGNANCIES

TARGETS

HEMATOLOGIC DISEASES

DISEASES

TARGETS

PIPELINE

BITE® PLATFORM

BIOSIMILARS

MODALITIES

FGFR2b

Fibroblast growth factor receptor 2 (FGFR2) is one of four FGFR family members that encode transmembrane receptor tyrosine kinases. FGFR2b is the IIIb splice isoform of FGFR2.1

Expression of FGFRs and their corresponding ligands, fibroblast growth factors, contributes to tumor progression in human malignancies by enhancing angiogenesis and proliferation.2,3 Patients whose tumors have amplification of the FGFR2 gene tend to have a poor prognosis.4-7

In tumors with FGFR2 amplification, it is the FGFR2b splice variant that is almost invariably expressed on the cell surface.8-10

FGFR2b overexpression is observed in 3%–61% of gastric and gastroesophageal junction cancers depending on tumor stage, assay, and study cutoff,1,4,11-13 and has been reported in various other cancers as well,14-19 suggesting that targeting FGFR2b may be an important therapeutic strategy.

References
1. Han N, et al. Pathobiology. 2015;82:269-279. 2. Presta M, et al. Cytokine Growth Factor Rev. 2005;16:159-178. 3. Grose R, et al. Cytokine Growth Factor Rev. 2005;16:179-186. 4. Ahn S, et al. Mod Pathol. 2016;29:1095-1103. 5. Su X, et al. Br J Cancer. 2014;110:967-975. 6. Seo S, et al. Oncotarget. 2017;8:33844-33854. 7. Jung E-J, et al. Hum Pathol. 2012;43:1559-1566. 8. Turner N, et al. Nat Rev Cancer. 2010;10:116-129. 9. Ornitz DM, et al. J Biol Chem. 1996;271:15292-15297. 10. Bai A, et al. Cancer Res. 2010;70:7630-7639. 11. Nagatsuma AK, et al. Gastric Cancer. 2015;18:227-238. 12. Tokunaga R, et al. Oncotarget. 2016;7:19748-19761. 13. Wainberg ZA, et al. Presented at: ASCO Gastrointestinal Cancer Symposium; January 15-17, 2021; Online Virtual Scientific Program. Abstract LBA160. 14. Yoshino M, et al. Int J Oncol. 2007;31:721-728. 15. Ishiwata T, et al. Am J Pathol. 1998;153:213-222. 16. Kurban G, et al. Oncol Rep. 2004;11:987-991. 17. Yamayoshi T, et al. J Pathol. 2004;204:110-118. 18. Cho K, et al. Am J Pathol. 2007;170:1964-1974. 19. Watanabe M, et al. Pathol Int. 2000;50:363-372. 20. Amgen Pipeline. https://www.amgenpipeline.com. Accessed 7/27/21.
Molecule
Modality20
Target20
Areas of Investigation20
Bemarituzumab
Target20
FGFR2b
Areas of Investigation20
PHASE 2 (GASTRIC OR GEJ CANCER)
References
1. Han N, et al. Pathobiology. 2015;82:269-279. 2. Presta M, et al. Cytokine Growth Factor Rev. 2005;16:159-178. 3. Grose R, et al. Cytokine Growth Factor Rev. 2005;16:179-186. 4. Ahn S, et al. Mod Pathol. 2016;29:1095-1103. 5. Su X, et al. Br J Cancer. 2014;110:967-975. 6. Seo S, et al. Oncotarget. 2017;8:33844-33854. 7. Jung E-J, et al. Hum Pathol. 2012;43:1559-1566. 8. Turner N, et al. Nat Rev Cancer. 2010;10:116-129. 9. Ornitz DM, et al. J Biol Chem. 1996;271:15292-15297. 10. Bai A, et al. Cancer Res. 2010;70:7630-7639. 11. Nagatsuma AK, et al. Gastric Cancer. 2015;18:227-238. 12. Tokunaga R, et al. Oncotarget. 2016;7:19748-19761. 13. Wainberg ZA, et al. Presented at: ASCO Gastrointestinal Cancer Symposium; January 15-17, 2021; Online Virtual Scientific Program. Abstract LBA160. 14. Yoshino M, et al. Int J Oncol. 2007;31:721-728. 15. Ishiwata T, et al. Am J Pathol. 1998;153:213-222. 16. Kurban G, et al. Oncol Rep. 2004;11:987-991. 17. Yamayoshi T, et al. J Pathol. 2004;204:110-118. 18. Cho K, et al. Am J Pathol. 2007;170:1964-1974. 19. Watanabe M, et al. Pathol Int. 2000;50:363-372. 20. Amgen Pipeline. https://www.amgenpipeline.com. Accessed 7/27/21.

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