EGFR (epidermal growth factor receptor) is a protein known to play a role in the growth of cancer cells. Tyrosine kinase inhibitors (TKIs) are drugs used to treat non-small-cell lung cancer (NSCLC) driven by EGFR mutations. However, most patients eventually develop resistance to TKIs, and up to 60% of patients will develop an EGFR T790M mutation when using first- and second-generation TKIs.
Blueprint Medicines have been developing a third-generation drug called Osimertinib which hopes to combat this resistance. The drug has gone through pre-clinical trials and has shown promising results in terms of efficacy and safety, and is now being tested in early-phase clinical trials for the treatment of EGFR-driven lung cancer.
The team at Blueprint used macromolecular crystallography at Diamond to determine the structure of the drug and understand how it interacts with its target molecule, EGFR (found in cancer cells). This information can also be used to develop new drugs that work similarly or to find new targets for treating cancer.
Diamond Light Source is the UK's national synchrotron science facility, located at the Harwell Science and Innovation Campus in Oxfordshire.
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