On November 20, 2017 Trillium Therapeutics Inc. (NASDAQ/TSX: TRIL), a clinical stage immuno-oncology company developing innovative therapies for the treatment of cancer, reported that new preclinical data for its novel covalent EGFR inhibitor were presented at the Society for Neuro-Oncology 22nd Annual Meeting, November 16-19, in San Francisco (Press release, Trillium Therapeutics, NOV 20, 2017, View Source [SID1234522151]).
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Poster Presentation: TTI-2341: A novel, orally bioavailable, brain-penetrant, covalent epidermal growth factor receptor (EGFR) inhibitor for treatment of glioblastoma multiforme (GBM) and brain metastases of non-small cell lung cancer (NSCLC).
This poster presentation highlighted preclinical data for TTI-2341, a novel covalent EGFR inhibitor. TTI-2341 had potent activity against a broad range of EGFR variants, including disease-relevant mutants T790M and C797S. TTI-2341 was shown to penetrate the blood brain barrier and demonstrated superior ADME properties and oral bioavailability relative to benchmark drugs afatinib and osimertinib. Notably, TTI-2341 achieved greater than 20-fold higher free drug brain exposure compared to osimertinib and was well tolerated at levels expected to be efficacious.
"Aberrant EGFR activity is clearly implicated in CNS tumors, particularly glioblastoma multiforme and brain metastases of non-small cell lung cancer," said Trillium CEO Dr. Niclas Stiernholm. "Currently available EGFR inhibitors have demonstrated limited efficacy due to poor penetration of the blood brain barrier and low activity against resistance-associated EGFR mutations. Our emerging preclinical data suggests that TTI-2341 can overcome these limitations."