On the right, the presence within EGFR of a residue able to form additional interactions with osimertinib (as for the L718Q mutant form) prevents its reaction with Cys797 allowing EGFR to work and cancer cells to survive. (sciencedaily.com)
Osimertinib showed preclinical evidence of concentrations in mouse brain tissue 5 - to 25-fold higher than in plasma, [16] and has shown greater penetration of the BBB in mouse models than gefitinib, rociletinib, or afatinib. (cancernetwork.com)
Solomon and his colleagues plan to start trial participants on osimertinib and then monitor resistance by tracking tumour DNA that circulates in their blood. (scientificamerican.com)