Article
Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations.
Nature cancer - 1 Sept 2023
Miyazaki Isao, Odintsov Igor, Ishida Keiji, Lui Allan J W, Kato Masanori, Suzuki Tatsuya, Zhang Tom, Wakayama Kentaro, Kurth Renate I, Cheng Ryan, Fujita Hidenori, Delasos Lukas, Vojnic Morana, Khodos Inna, Yamada Yukari, Ishizawa Kota, Mattar Marissa S, Funabashi Kaoru, Chang Qing, Ohkubo Shuichi, Yano Wakako, Terada Ryuichiro, Giuliano Claudio, Lu Yue Christine, Bonifacio Annalisa, Kunte Siddharth, Davare Monika A, Cheng Emily H, de Stanchina Elisa, Lovati Emanuela, Iwasawa Yoshikazu, Ladanyi Marc, Somwar Romel
Abstract excerpt
RET receptor tyrosine kinase is activated in various cancers (lung, thyroid, colon and pancreatic, among others) through oncogenic fusions or gain-of-function single-nucleotide variants. Small-molecule RET kinase inhibitors became standard-of-care therapy for advanced malignancies driven by RET. The therapeutic benefit of RET inhibitors is limited, however, by acquired mutations in the drug target as well as...
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