TAS-119, a novel selective Aurora A and TRK inhibitor, exhibits antitumor efficacy in preclinical models with deregulated activation of the Myc, β-Catenin, and TRK pathways.

doi:10.1007/s10637-020-01019-9

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TAS-119, a novel selective Aurora A and TRK inhibitor, exhibits antitumor efficacy in preclinical models with deregulated activation of the Myc, β-Catenin, and TRK pathways.

Investigational new drugs - 1 Jun 2021

Miura Akihiro, Sootome Hiroshi, Fujita Naoya, Suzuki Takamasa, Fukushima Hiroto, Mizuarai Shinji, Masuko Norio, Ito Kimihiro, Hashimoto Akihiro, Uto Yoshihiro, Sugimoto Tetsuya, Takahashi Hidekazu, Mitsuya Morihiro, Hirai Hiroshi

Abstract excerpt

Aurora kinase A, a mitotic kinase that is overexpressed in various cancers, is a promising cancer drug target. Here, we performed preclinical characterization of TAS-119, a novel, orally active, and highly selective inhibitor of Aurora A. TAS-119 showed strong inhibitory effect against Aurora A, with an IC50 value of 1.04 nmol/L. The compound was highly selective for Aurora A compared with 301 other protein...

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TAS-119, a novel selective Aurora A and TRK inhibitor, exhibits antitumor efficacy in preclinical models with deregulated activation of the Myc, β-Catenin, and TRK pathways.

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