Table 1.
FGFR inhibitors in cancer treatment
| Inhibitors | Targets | Function | Adverse events | Ref. |
|---|---|---|---|---|
| BGJ398 | FGFR1‐3 | Inhibits cell proliferation; exerts anti‐tumour activity in several tumour types including lung cancer, bladder, urothelial cancers, cholangiocarcinoma | Hyperphosphatemia, constipation, decreased appetite, diarrhoea, fatigue, alopecia, nausea in patients | 109, 124, 125, 126, 127 |
| SSR128129E | FGFR1‐4 | Inhibits proliferation, angiogenesis and metastasis in pancreatic, breast and colon cancer cells | A therapeutic dose minimally elevated plasma levels of the prothrombotic PAI‐1, a minor anaemia in mice | 97 |
| Dovitinib (TKI258) | FGFR, PDGFRβ, VEGFR2 | Inhibits tumour growth, motility and metastasis; enhances the therapeutic effect of gemcitabine and capecitabine | Fatigue, neutropenia, thrombocytopenia, anaemia, nausea, palmar‐plantar erythrodysesthesia syndrome in patients | 98, 99 |
| Lenvatinib | FGFR1‐4, KIT, RET, VEGFR1‐3, PDGFRα | Inhibits tumour growth, angiogenesis in pancreatic cancer, hepatocellular cancer and melanoma | Hypertension, palmar‐plantar erythrodysesthesia syndrome, decrease appetite, proteinuria, fatigue, nausea | 100, 128, 129 |
| Masitinib | c‐Kit, FGFR and PDGFR | Inhibits inflammation, combined with gemcitabine exhibited synergy on proliferation inhibition | Back pain, constipation, pulmonary embolism, vomiting, nausea, rash, thrombocytopenia, thrombosis, hypokalemia, pyrexia, neutropenia and anaemia | 101, 102, 103, 104 |
| PD173074 | FGFR1, VEGFR2 | Blocks the proliferation and induces apoptosis. Inhibits stem cell proliferation and self‐renewal | No body weight loss and appearance change in mice | 105, 108, 130 |
| Nintedanib | VEGFR1/2/3, FGFR1/2/3, PDGFRα/β | Inhibits cell proliferation, induces apoptosis, enhances gemcitabine, or afatinib, or docetaxel, or cisplatin inhibitory effect | Diarrhoea, asthenia, nausea, vomiting, anaemia, anorexia, hepatic enzyme elevation, hypertension, hypothyroidism, hand‐foot syndrome, cardiac disorder, haematological abnormalities. Nintedanib plus docetaxel leads to sepsis, pneumonia, respiratory failure and pulmonary embolism | 110, 111, 112, 113, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140 |
| Ponatinib | FGFRs, Bcr‐Abl, Src, PDGFRa, VEGFR2 | Anti‐tumour activity in leukaemia. Combines an MEK inhibitor to inhibit pancreatic cancer cell growth | Hypertension, myelosuppression, cerebrovascular, vaso‐occlusive disease, lipase and rash | 115, 141, 142, 143, 144, 145 |