作者
AL Wong, Ross A Soo, DS Tan, Soo Chin Lee, JS Lim, PC Marban, Li Ren Kong, YJ Lee, LZ Wang, Win Lwin Thuya, R Soong, MQ Yee, TM Chin, Maricel Tiemsim Cordero, Bernadette Reyna Asuncion, B Pang, Shazib Pervaiz, Jayshree L Hirpara, Arvind Sinha, WW Xu, M Yuasa, T Tsunoda, M Motoyama, T Yamauchi, Boon Cher Goh
发表日期
2015/5/1
期刊
Annals of Oncology
卷号
26
期号
5
页码范围
998-1005
出版商
Elsevier
简介
This phase I study evaluated the safety, pharmacokinetics and pharmacodynamics of OPB-51602, a novel oral small-molecule STAT3 inhibitor, in patients with advanced solid tumors. A tolerable dose was established; gastrointestinal toxicities and peripheral neuropathy were dose-limiting. Responses observed in EGFR TKI-resistant NSCLC patients suggest anti-tumor activity, warranting further studies.
Background
The aim of this study was to determine the maximum-tolerated dose (MTD), safety, pharmacokinetics, and pharmacodynamics of OPB-51602, an oral, direct signal transduction activator of transcription 3 (STAT3) inhibitor, in patients with refractory solid tumors.
Patients and methods
Three cohorts were studied: cohort A, a sequential dose escalation of OPB-51602 administered intermittently (days 1–14 every 21 days); cohort B, an expansion cohort evaluating the dose lower than the MTD; cohort C …
引用总数
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