One of the interesting new developments at AACR was the return of FGFR inhibitors with more enthusiasm and encouraging data compared to the past. Recall that previous small molecule inhibitors such as brivanib (BMS) and dovitinib (Novartis) didn’t fare particularly well, despite a multitude of clinical trials in different tumour types where FGFR was thought to matter.

This begs several key questions:

  • Does the target matter to the tumour?
  • Do we have enough therapeutic index to shut down the pathway?
  • Is it better to be a specific or a pan-FGFR inhibitor?
  • Does having multi-kinase effects offer off-target adverse events to the detriment of efficacy?
  • Do we need an antibody or an ADC rather than a small molecule to improve potency?

And many other questions that cannot be addressed or answered on the basis of two chemical entities.

Interestingly, and perhaps even surprisingly, new data emerged in San Diego that might help us answer some of these questions.

In this review, a number of anti-FGFR compounds are mentioned including brivanib (BMS), dovitinib (Novartis), lenvatinib (Eisai), ponatinib (Ariad), BGJ398 (Novartis) and BAY 1179470 (Bayer).  

Here, we take a particular focus on promising new FGFR compounds with new data at AACR from Novartis (BGJ398) and Bayer (BAY 1179470, BAY 1163877, FGFR2-ADC).

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 Next generation FGFR inhibitors are early but promising in selected cancers

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