Article
The first-in-human phase I study of a brain-penetrant mutant IDH1 inhibitor DS-1001 in patients with recurrent or progressive IDH1-mutant gliomas.
Neuro-oncology - 14 Feb 2023
Natsume Atsushi, Arakawa Yoshiki, Narita Yoshitaka, Sugiyama Kazuhiko, Hata Nobuhiro, Muragaki Yoshihiro, Shinojima Naoki, Kumabe Toshihiro, Saito Ryuta, Motomura Kazuya, Mineharu Yohei, Miyakita Yasuji, Yamasaki Fumiyuki, Matsushita Yuko, Ichimura Koichi, Ito Kazumi, Tachibana Masaya, Kakurai Yasuyuki, Okamoto Naoko, Asahi Takashi, Nishijima Soichiro, Yamaguchi Tomoyuki, Tsubouchi Hiroshi, Nakamura Hideo, Nishikawa Ryo
Abstract excerpt
BACKGROUND: Approximately 70% of lower-grade gliomas harbor isocitrate dehydrogenase 1 (IDH1) mutations, resulting in the accumulation of oncometabolite D-2-hydroxyglutarate (D-2-HG); this leads to epigenetic dysregulation, oncogenesis, and subsequent clonal expansion. DS-1001 is an oral brain-penetrant mutant IDH1 selective inhibitor. This first-in-human study investigated the safety, pharmacokinetics,...
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