T
Toshiyuki Tsukaguchi
Researcher at Chugai Pharmaceutical Co.
Publications - 20
Citations - 1480
Toshiyuki Tsukaguchi is an academic researcher from Chugai Pharmaceutical Co.. The author has contributed to research in topics: ALK inhibitor & Alectinib. The author has an hindex of 12, co-authored 20 publications receiving 1358 citations.
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Journal ArticleDOI
CH5424802, a Selective ALK Inhibitor Capable of Blocking the Resistant Gatekeeper Mutant
Hiroshi Sakamoto,Toshiyuki Tsukaguchi,Sayuri Hiroshima,Tatsushi Kodama,Takamitsu Kobayashi,Takaaki A. Fukami,Nobuhiro Oikawa,Takuo Tsukuda,Nobuya Ishii,Yuko Aoki +9 more
TL;DR: CH5424802 is identified, a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cellsExpressing NPM-alk fusion in vitro and in vivo.
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Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance.
TL;DR: Alectinib led to tumor size reduction in EML4-ALK-positive xenograft tumors that failed to regress fully during the treatment with crizotinib, and inhibited the growth of some EML 4-ALK mutant-driven tumors, including the G1269A model.
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Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).
Kazutomo Kinoshita,Kohsuke Asoh,Noriyuki Furuichi,Toshiya Ito,Hatsuo Kawada,Sousuke Hara,Jun Ohwada,Takuho Miyagi,Takamitsu Kobayashi,Kenji Takanashi,Toshiyuki Tsukaguchi,Hiroshi Sakamoto,Takuo Tsukuda,Nobuhiro Oikawa +13 more
TL;DR: This work optimized the side-chains and identified highly selective, orally active and potent ALK inhibitor CH5424802 (18a) as the clinical candidate.
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Alectinib Shows Potent Antitumor Activity against RET-Rearranged Non–Small Cell Lung Cancer
Tatsushi Kodama,Toshiyuki Tsukaguchi,Yasuko Satoh,Miyuki Yoshida,Yoshiaki Watanabe,Osamu Kondoh,Hiroshi Sakamoto +6 more
TL;DR: The results suggest that alectinib is effective against RET fusion–positive tumors and might be a therapeutic option for patients with RET fusion-positive NSCLC, and test its ability to inhibit the activity of kinases other than ALK.
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The Fibroblast Growth Factor Receptor Genetic Status as a Potential Predictor of the Sensitivity to CH5183284/Debio 1347, a Novel Selective FGFR Inhibitor
Yoshito Nakanishi,Nukinori Akiyama,Toshiyuki Tsukaguchi,Toshihiko Fujii,Kiyoaki Sakata,Hitoshi Sase,Takehito Isobe,Kenji Morikami,Hidetoshi Shindoh,Toshiyuki Mio,Hirosato Ebiike,Naoki Taka,Yuko Aoki,Nobuya Ishii +13 more
TL;DR: The identification of CH5183284/Debio 1347 is reported, a selective and orally available FGFR1, FGFR2, and FGFR3 inhibitor that has a unique chemical scaffold and shows preferential antitumor activity against cancer cells with various FGFR genetic alterations in a panel of 327 cancer cell lines and in xenograft models.