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AVEO Presents Preclinical Efficacy Data on AV-412, a Novel Oral,Tyrosine Kinase Inhibitor of EGFR/HER2 for EGFR Mutant and,Drug-Resistant Lung Cancer

LOS ANGELES & CAMBRIDGE, Mass.--(BUSINESS WIRE)--Apr 17, 2007 - AVEO Pharmaceuticals, Inc., a biopharmaceutical company focused on the discovery and development of novel, targeted cancer medicines, today announced encouraging preclinical data of AV-412, a novel, next generation oral tyrosine kinase inhibitor of EGFR/HER2 using AVEO's unique EGFR mutant and drug-resistant lung cancer tumor models. The results from the preclinical study showed that AV-412 is greater than 10 times more potent than erlotinib in genetically engineered lung tumor models with the EGFR L858R mutation, producing rapid and complete tumor regression at a daily dose of 1 mg/kg. Additionally, AV-412 is also active against tumors carrying the EGFR kinase-resistance mutation EGFR L858R/T790M. These data were presented today in the EGFR Inhibition poster session at the 100th American Association for Cancer Research (AACR) Annual Meeting.

The molecularly targeted drugs - erlotinib (Tarceva(R)) and gefitinib (Iressa(R)) - inhibit EGFR kinase activity and are important therapies for patients with non-small cell lung cancer; however, recent clinical observations from independent groups suggest that lung cancer patients harboring the EGFR L858R mutation (approximately 44 percent of all EGFR mutants) exhibit poorer response rates, progression free survival and overall survival after treatment with EGFR kinase inhibitors when compared with patients harboring other EGFR mutations. This suggests the need for inhibitors that are more effective against patients with EGFR L858R mutations. In addition, resistance to EGFR kinase inhibitors uniformly develops over time often due to the acquisition of resistance mutations within the EGFR gene. Erlotinib and gefitinib have no effect on the EGFR L858R/T790M double mutant, which is estimated to account for approximately 50 percent of all drug resistance in EGFR mutant non-small cell lung cancer - representing a key unmet medical need.






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