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Specific <jats:italic>FGFR<\/jats:italic> mutations have been observed in several types of cancers, including gastric carcinoma and cholangiocarcinoma. Dose escalation data of 24 Japanese patients with solid tumors treated with Tasurgratinib (previously known as E7090), a potent, selective FGFR1\u20133 inhibitor, was reported in a phase I, first\u2010in\u2010human, single\u2010center study. Based on the safety, pharmacokinetic, and pharmacodynamic profiles observed in this study, the recommended dose of 140\u2009mg once daily was selected for the expansion part (Part 2), a multicenter expansion of the dose\u2010finding study restricted to patients with tumors harboring <jats:italic>FGFR<\/jats:italic> gene alterations. Safety and preliminary efficacy were assessed in Part 2. Pharmacodynamic pharmacogenomic markers (serum phosphate, FGF23, and 1,25\u2010(OH)<jats:sub>2<\/jats:sub>\u2010vitamin D, circulating tumor DNA) and pharmacokinetic profiles were also evaluated. A total of 16 patients were enrolled in Part 2, six with cholangiocarcinoma and 10 with gastric cancer. The most common treatment\u2010emergent adverse events were hyperphosphatemia, palmar\u2010plantar erythrodysesthesia syndrome, and paronychia. Five partial responses (83.3%) in cholangiocarcinoma patients and one partial response (11.1%) in gastric cancer patients were observed; median progression\u2010free survival was 8.26\u2009months (95% confidence interval [CI] 3.84, not evaluable [NE]) and 3.25\u2009months (95% CI 0.95, 4.86), and overall survival was 22.49\u2009months (95% CI 6.37, NE) and 4.27\u2009months (95% CI 2.23, 7.95), respectively, in the two groups. In conclusion, Tasurgratinib 140\u2009mg has a tolerable safety profile with good clinical efficacy in patients with cholangiocarcinoma harboring <jats:italic>FGFR2<\/jats:italic> gene rearrangements.<\/jats:p>","DOI":"10.1111\/cas.16354","type":"journal-article","created":{"date-parts":[[2024,10,27]],"date-time":"2024-10-27T10:31:38Z","timestamp":1730025098000},"page":"192-203","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Tasurgratinib in patients with cholangiocarcinoma or gastric cancer: Expansion part of the first\u2010in\u2010human phase I study"],"prefix":"10.1111","volume":"116","author":[{"given":"Chigusa","family":"Morizane","sequence":"first","affiliation":[{"name":"National Cancer Center Hospital  Tokyo Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Makoto","family":"Ueno","sequence":"additional","affiliation":[{"name":"Kanagawa Cancer Center  Yokohama Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tatsuya","family":"Ioka","sequence":"additional","affiliation":[{"name":"Oncology Center Yamaguchi University Hospital  Ube Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Masahiro","family":"Tajika","sequence":"additional","affiliation":[{"name":"Aichi Cancer Center Hospital  Nagoya Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4050-2086","authenticated-orcid":false,"given":"Masafumi","family":"Ikeda","sequence":"additional","affiliation":[{"name":"National Cancer Center Hospital East  Kashiwa Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kensei","family":"Yamaguchi","sequence":"additional","affiliation":[{"name":"The Cancer Institute Hospital Japanese Foundation for Cancer Research  Tokyo Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hiroki","family":"Hara","sequence":"additional","affiliation":[{"name":"Saitama Cancer Center  Saitama Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hiroshi","family":"Yabusaki","sequence":"additional","affiliation":[{"name":"Niigata Cancer Center Hospital  Niigata Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Atsushi","family":"Miyamoto","sequence":"additional","affiliation":[{"name":"National Hospital Organization Osaka National Hospital  Osaka Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3863-9582","authenticated-orcid":false,"given":"Satoru","family":"Iwasa","sequence":"additional","affiliation":[{"name":"National Cancer Center Hospital  Tokyo Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3127-8203","authenticated-orcid":false,"given":"Manabu","family":"Muto","sequence":"additional","affiliation":[{"name":"Kyoto University Hospital  Kyoto Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tsutomu","family":"Takashima","sequence":"additional","affiliation":[{"name":"Graduate School of Medicine Osaka Metropolitan University  Osaka Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Keiko","family":"Minashi","sequence":"additional","affiliation":[{"name":"Chiba Cancer Center  Chiba Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1570-6802","authenticated-orcid":false,"given":"Yoshito","family":"Komatsu","sequence":"additional","affiliation":[{"name":"Hokkaido University Hospital  Sapporo Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tomohiro","family":"Nishina","sequence":"additional","affiliation":[{"name":"National Hospital Organization Shikoku Cancer Center  Matsuyama Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Takako Eguchi","family":"Nakajima","sequence":"additional","affiliation":[{"name":"St. Marianna University School of Medicine  Kawasaki Japan"},{"name":"Department of Early Clinical Development Kyoto University Graduate School of Medicine  Kyoto Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Atsuchi","family":"Takeno","sequence":"additional","affiliation":[{"name":"Kansai Rosai Hospital  Amagasaki Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Toshikazu","family":"Moriwaki","sequence":"additional","affiliation":[{"name":"University of Tsukuba Hospital  Tsukuba Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Masayuki","family":"Furukawa","sequence":"additional","affiliation":[{"name":"National Hospital Organization Kyushu Cancer Center  Fukuoka Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Takatoshi","family":"Sahara","sequence":"additional","affiliation":[{"name":"Eisai Co., Ltd.  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