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This open\u2010label Phase I dose\u2010escalation study was conducted to determine the maximum tolerated dose of continuous daily buparlisib in Japanese patients with advanced solid tumors. Secondary objectives included safety and tolerability, pharmacokinetics, antitumor activity and pharmacodynamic marker changes. Fifteen patients were treated at 25\u00a0mg\/day (<jats:italic>n<\/jats:italic>\u00a0=\u00a03), 50\u00a0mg\/day (<jats:italic>n<\/jats:italic>\u00a0=\u00a03) and 100\u00a0mg\/day (<jats:italic>n<\/jats:italic>\u00a0=\u00a09) dose levels. One dose\u2010limiting toxicity of Grade\u00a04 abnormal liver function occurred at 100\u00a0mg\/day. Considering the safety profile and the maximum tolerated dose in the first\u2010in\u2010man study of buparlisib in non\u2010Japanese patients, further dose escalation was stopped and 100\u00a0mg\/day was declared the recommended dose. The most common treatment\u2010related adverse events were rash, abnormal hepatic function (including increased transaminase levels), increased blood insulin levels and increased eosinophil count. Hyperglycemia was experienced by two patients, one Grade 1 and one Grade 4, and mood alterations were experienced by three patients, two Grade\u00a01 and one Grade\u00a02. Pharmacokinetic results showed that buparlisib was rapidly absorbed in a dose\u2010proportional manner. Best overall response was stable disease for six patients, including one unconfirmed partial response. In these Japanese patients with advanced solid tumors, buparlisib had a manageable safety profile, with similar pharmacokinetics to non\u2010Japanese patients. The recommended dose of 100\u00a0mg\/day will be used in future studies of buparlisib in Japanese patients.<\/jats:p>","DOI":"10.1111\/cas.12350","type":"journal-article","created":{"date-parts":[[2014,1,10]],"date-time":"2014-01-10T05:53:41Z","timestamp":1389333221000},"page":"347-353","source":"Crossref","is-referenced-by-count":82,"title":["Phase I dose\u2010escalation study of buparlisib (<scp>BKM<\/scp>120), an oral pan\u2010class I <scp>PI<\/scp>3K inhibitor, in Japanese patients with advanced solid tumors"],"prefix":"10.1111","volume":"105","author":[{"given":"Yuichi","family":"Ando","sequence":"first","affiliation":[{"name":"Nagoya University Hospital Nagoya Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Megumi","family":"Inada\u2010Inoue","sequence":"additional","affiliation":[{"name":"Nagoya University Hospital Nagoya Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ayako","family":"Mitsuma","sequence":"additional","affiliation":[{"name":"Nagoya University Hospital Nagoya Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Takayuki","family":"Yoshino","sequence":"additional","affiliation":[{"name":"National Cancer Center Hospital East Kashiwa Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Atsushi","family":"Ohtsu","sequence":"additional","affiliation":[{"name":"National Cancer Center Hospital East Kashiwa Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Naoko","family":"Suenaga","sequence":"additional","affiliation":[{"name":"Novartis Pharma K.K. 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