Graham Richmond

TL;DR: A novel structurally distinct third-generation EGFR TKI that irreversibly and selectively targets both sensitizing and resistant T790M(+) mutant EGFR while harboring less activity toward wild-type EGFR is reported.

TL;DR: ZD6474 is a potent, p.o. active, low molecular weight inhibitor of kinase insert domain-containing receptor that demonstrates selectivity against a range of other tyrosine and serine-threonine kinases and translates into potent inhibition of vascular endothelial growth factor-A (VEGF)-stimulated endothelial cell proliferation in vitro.

TL;DR: The data obtained with AZD2171 are consistent with potent inhibition of VEGF signaling, angiogenesis, neovascular survival, and tumor growth.

TL;DR: Following observations of significant tumor inhibition in preclinical models, the clinical candidate AZD9291 was administered clinically to patients with T790M positive EGFR-TKI resistant NSCLC and early efficacy has been observed, accompanied by an encouraging safety profile.

TL;DR: A small molecular weight inhibitor of VEGF receptor tyrosine kinase (RTK) activity was developed that was compatible with chronic oral administration and may have utility in the treatment of a range of histologically diverse solid tumor types.