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Cocktail and Poster Display session

54P - Resistance to MAPK pathway inhibition in BRAF-V600E mutant colorectal cancer can be overcome with insulin receptor/insulin-like growth factor-1 receptor inhibitors

Date

26 Feb 2024

Session

Cocktail and Poster Display session

Topics

Targeted Therapy

Tumour Site

Colon and Rectal Cancer

Presenters

Layla El Bouazzaoui

Citation

Annals of Oncology (2024) 9 (suppl_1): 1-11. 10.1016/esmoop/esmoop102271

Authors

L. El Bouazzaoui, D. Raats, O. Kranenburg

Author affiliations

  • Lab Translational Oncology, UMC - University Medical Center Utrecht, 3508 GA - Utrecht/NL

Resources

This content is available to ESMO members and event participants.

Abstract 54P

Background

The current standard-of-care treatment for refractory BRAF-V600E mutant metastatic colorectal cancer (mCRC) consists of the BRAF inhibitor encorafenib plus the EGFR inhibitor cetuximab. However, tumour responses to this regimen are mostly transient, presumably caused by a rebound in MAPK activation.

Methods

In this study, we combined short-term cell viability assays with long-term re-growth assays following drug removal over a period of three weeks which allows assessment of re-growth after therapy discontinuation. We applied this strategy to test the effect of combined BRAF inhibition (encorafenib) and EGFR inhibition (afatinib), on BRAF-V600E mutant CRC patient-derived organoids (PDOs).

Results

Combined EGFR/BRAF inhibition initially caused a major reduction in PDO growth capacity in BRAF-V600E mutant PDOs. This was followed by re-activation of MAPK and rapid re-growth after drug removal, as is observed in CRC patients. During re-growth, the insulin receptor (IR) and insulin-like growth factor receptor (IGF1R) were activated in BRAF-V600E mutant PDOs. The IGFR/IR inhibitor linsitinib prevented the rebound in MAPK activity following removal of afatinib and encorafenib, prevented re-growth of CRC PDOs, and improved the anti-tumour response in an in vivo model.

Conclusions

PDO re-growth assays allow the identification of pathways driving tumour recurrence. IR/IGFR-inhibition prevents re-growth following golden standard MAPK pathway-targeted therapy and provides a strategy to improve the treatment of BRAF-V600E mutant CRC.

Clinical trial identification

Editorial acknowledgement

Legal entity responsible for the study

O. Kranenburg.

Funding

U-PORT.

Disclosure

All authors have declared no conflicts of interest.

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