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Neratinib, an Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor: Results of a Phase II Trial in Patients With Advanced Non–Small-Cell Lung Cancer

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Sequist, Lecia V., Besse, Benjamin, Lynch, Thomas J., Miller, Vincent A., Wong, Kwok K., Gitlitz, Barbara, Eaton, Keith, Zacharchuk, Charles, Freyman, Amy, Powell, Christine, Ananthakrishnan, Revathi, Quinn, Susan, Soria, Jean-Charles·2010·Journal of Clinical Oncology

DOI 10.1200/jco.2009.27.9414

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Abstract

Purpose: Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have had a significant impact on non–small-cell lung cancer (NSCLC) outcomes, particularly for patients with EGFR mutations. Resistance emerges after 9 to 12 months, primarily mediated by the T790M resistance mutation. We studied neratinib, an irreversible pan-ErbB TKI that may overcome T790M. Patients and Methods: Patients with advanced NSCLC underwent EGFR sequencing of available tumor tissue at enrollment. Those with ≥ 12 weeks of prior TKI therapy were placed in arm A if they were EGFR mutation positive or arm B if they were wild-type. Arm C included TKI-naïve patients with adenocarcinoma and light smoking histories (≤ 20 pack-years). All patients received daily oral neratinib, initially at 320 mg but subsequently reduced to 240 mg because of excessive diarrhea. The primary end point was objective response rate (RR). Results: One-hundred sixty-seven patients were treated: 91 in arm A, 48 in arm B, and 28 in arm C. Diarrhea was the most common toxicity; grade 3 incidence was 50% at 320 mg but improved to 25% after dose reduction. The RR was 3% in arm A and zero in arms B and C. No patients with known T790M responded. Notably, three of four patients with an exon 18 G719X EGFR mutation had a partial response and the fourth had stable disease lasting 40 weeks. Conclusion: Neratinib had low activity in patients with prior benefit from TKIs and in TKI-naïve patients, potentially because of insufficient bioavailability from diarrhea-imposed dose limitation. Responses were seen in patients with the rare G719X EGFR mutation, highlighting the importance of obtaining comprehensive genetic information on trials of targeted agents.

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Authors: Sequist, L. V., Besse, B., Lynch, T. J., Miller, V. A., Wong, K. K., Gitlitz, B., Eaton, K., Zacharchuk, C., Freyman, A., Powell, C., Ananthakrishnan, R., Quinn, S., & Soria, J.-C.
Venue: Journal of Clinical Oncology
Publisher: American Society of Clinical Oncology (ASCO)
Published: 2010-06-20
Volume: 28
Issue: 18
Pages: 3076-3083
ISSN: 0732-183X (ISSN-L)
1527-7755
DOI: 10.1200/jco.2009.27.9414
OpenAlex: W2109080255
Cited by: 429
References: 10
FWCI: 36.40
Type: journal article
Language: en
Open access: bronze

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Neratinib, an Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor: Results of a Phase II Trial in Patients With Advanced Non–Small-Cell Lung Cancer

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