Blueprint Medicines Presents Foundational Preclinical Data for BLU-945 Showing Robust Anti-Tumor Activity in Treatment-Resistant EGFR-Mutated Lung Cancer at ESMO Virtual Congress 2020
Currently, there are no approved therapies for patients with osimertinib-resistant EGFRm NSCLC, and there is an urgent need for new therapies to address tumor resistance. BLU-945 was designed to potently inhibit triple-mutant EGFR harboring either the activating L858R or exon 19 deletion mutations combined with the acquired T790M and C797S mutations, the most common on-target resistance to standard EGFR inhibitors. In addition, BLU-945 was designed to be wild-type EGFR and kinome selective with the potential for improved tolerability and combination strategies.
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In preclinical data presented at the ESMO congress, BLU-945 inhibited triple mutant EGFR with sub-nanomolar potency and demonstrated greater than 900-fold selectivity over wild-type EGFR along with excellent overall kinome selectivity. In a triple mutant EGFR cell-line, BLU-945 potently inhibited the EGFR pathway, while osimertinib demonstrated limited activity. BLU-945 monotherapy resulted in robust anti-tumor activity in multiple cell line-derived and patient-derived xenograft (PDX) models of triple mutant EGFR NSCLC. In addition, BLU-945 treatment in combination with osimertinib or gefitinib resulted in tumor regression in a triple mutant EGFR NSCLC PDX model derived from a patient with progressive disease following five lines of prior therapy. BLU-945 was also highly active in an intracranial disease model.
Based on these preclinical proof-of-concept data,
About EGFRm NSCLC
Lung cancer is the leading cause of cancer death worldwide. Among the 80 to 85 percent of lung cancers classified as NSCLC, about 10 to 15 percent of cases in the US and
Cautionary Note Regarding Forward-Looking Statement
This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995, as amended, including, without limitation, statements regarding plans and timelines for the development of BLU-945 and an additional EGFR development candidate; the potential benefits of
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