Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations

Isao Miyazaki; Igor Odintsov; Keiji Ishida; Allan J.W. Lui; Masanori Kato; Tatsuya Suzuki; Tom Zhang; Kentaro Wakayama; Renate I. Kurth; Ryan R. Cheng; Hidenori Fujita; Lukas Delasos; Morana Vojnic; Inna Khodos; Yukari Yamada; Kota Ishizawa; Marissa S. Mattar; Kaoru Funabashi; Qing Chang; Shuichi Ohkubo; Wakako Yano; Ryuichiro Terada; Claudio Giuliano; Yue Lü; Annalisa Bonifacio; Siddharth Kunte; Monika A. Davare; Emily H. Cheng; Elisa de Stanchina; Emanuela Lovati; Yoshikazu Iwasawa; Marc Ladanyi; Romel Somwar

doi:10.1038/s43018-023-00630-y

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Abstract

), and shows superior pharmacokinetic properties in the brain when compared to currently approved RET drugs. We further show that these properties translate into improved tumor control in an intracranial model of RET-driven cancer. Our results underscore the clinical potential of vepafestinib in treating RET-driven cancers.

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Miyazaki et al. (2023) studied this question.

synapsesocial.com/papers/69fc06147c10856f85dd6b40 https://doi.org/10.1038/s43018-023-00630-y

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Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations

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Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations

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