If you had told me several weeks ago that we would write over 28 posts on #AACR16 and become very interested in mouse models, then most likely I would have laughed out loud and told you not to be so ridiculous! Here we are with the 29th one and, another, on the bromododomain landscape yet to go. Such was the vast richness of data and concepts being discussed or presented in New Orleans for those who chose to look.
Today, I want to start the segue from AACR to ASCO coverage.
One way to do that is through the second part of the Gems from the Post Hall series. This latest one looks at a range of intriguing new targeted therapies and novel targets that are emerging, including a pharma company with a particularly interesting early pipeline.
Several pharma companies presented interesting data on their very early compounds currently in development, plus I noticed a trend for a new class of targeted therapies to emerge, MNK inhibitors, which we will also discuss.
Companies mentioned: Bayer, Orion Pharma, Lilly, Novartis, Pfizer, Agios.
Targets mentioned: PI3K, CDK, Akt, TWEAK, FGFR, BUB1, IDH1, SMYD2, MNK
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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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