Abstract | OBJECTIVE:
Neratinib (HKI-272), a potent, irreversible, small-molecule, orally administered, pan-ErbB inhibitor that blocks signal transduction via inhibition of three epidermal growth factor receptors [ErbB1, ErbB2 (Her2) and ErbB4], is being developed for the treatment of solid tumors, including breast cancer. This Phase 1 dose-escalation study assessed the safety, tolerability, maximum-tolerated dose, antitumor activity and pharmacokinetics of neratinib in Japanese patients with advanced solid tumors. METHODS: Patients received neratinib 80, 160, 240 or 320 mg orally; each patient enrolled in only one dose cohort. Patients received a single dose in week 1, followed by daily continuous doses. Blood samples collected were on days 1 and 21 for pharmacokinetic analyses. RESULTS: CONCLUSIONS: The safety, efficacy and pharmacokinetic profiles of neratinib are consistent with those reported for non-Japanese patients and warrant further investigation of neratinib in Japanese patients with solid tumors.
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Authors | Yoshinori Ito, Mitsukuni Suenaga, Kiyohiko Hatake, Shunji Takahashi, Masahiro Yokoyama, Yusuke Onozawa, Kentaro Yamazaki, Shuichi Hironaka, Kiyoshi Hashigami, Hirotaka Hasegawa, Nobuko Takenaka, Narikazu Boku |
Journal | Japanese journal of clinical oncology
(Jpn J Clin Oncol)
Vol. 42
Issue 4
Pg. 278-86
(Apr 2012)
ISSN: 1465-3621 [Electronic] England |
PMID | 22371427
(Publication Type: Clinical Trial, Phase I, Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Quinolines
- ErbB Receptors
- neratinib
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Topics |
- Adult
- Aged
- Antineoplastic Agents
(adverse effects, pharmacokinetics, therapeutic use)
- Asian People
- Drug Administration Schedule
- ErbB Receptors
(antagonists & inhibitors)
- Female
- Humans
- Male
- Maximum Tolerated Dose
- Middle Aged
- Quinolines
(adverse effects, pharmacokinetics, therapeutic use)
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