Cited by 349Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchGastric Cancer Management and Outcomes

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Phase I Trial of the Irreversible EGFR and HER2 Kinase Inhibitor BIBW 2992 in Patients With Advanced Solid Tumors

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Yap, Timothy A., Vidal, Laura, Adam, Jan, Stephens, Peter, Spicer, James, Shaw, Heather, Ang, Jooern, Temple, Graham, Bell, Susan, Shahidi, Mehdi, Uttenreuther-Fischer, Martina, Stopfer, Peter, Futreal, Andrew, Calvert, Hilary, de Bono, Johann S., Plummer, Ruth·2010·Journal of Clinical Oncology

DOI 10.1200/jco.2009.26.7278

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Abstract

PURPOSE: Preclinical data have demonstrated that BIBW 2992 is a potent irreversible inhibitor of ErbB1 (EGFR/HER1) and mutated ErbB1 receptors including the T790M variant, as well as ErbB2 (HER2). A phase I study of continuous once-daily oral BIBW 2992 was conducted to determine safety, maximum-tolerated dose, pharmacokinetics (PK), food effect, and preliminary antitumor efficacy. PATIENTS AND METHODS: Patients with advanced solid tumors were treated. PK evaluation was performed after the first dose and at steady-state. RESULTS: Fifty-three patients received BIBW 2992 at 10 to 50 mg/d. BIBW 2992 was generally well-tolerated. The most common adverse effects included diarrhea, nausea, vomiting, rash, and fatigue. Dose-limiting toxicities included grade 3 rash (n = 2) and reversible dyspnea secondary to pneumonitis (n = 1). The recommended phase II dose was 50 mg/d. PK was dose proportional with a terminal elimination half-life ranging between 21.3 and 27.7 hours on day 1 and between 22.3 and 67.0 hours on day 27; BIBW 2992 exposure decreased after food intake. Three patients with non-small-cell lung carcinoma (NSCLC; two with in-frame exon 19 mutation deletions) experienced confirmed partial responses (PR) sustained for 24, 18, and 34 months, respectively. Two other patients (esophageal carcinoma and NSCLC) had nonconfirmed PRs. A patient with a PR at 10 mg/d progressed and developed symptomatic brain metastases, which subsequently regressed with an increased dose of 40 mg/d of BIBW 2992. A further seven patients had disease stabilization lasting > or = 6 months. CONCLUSION: Continuous, daily, oral BIBW 2992 is safe and has durable antitumor activity. It is currently being evaluated in phase III trials.

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New Guidelines to Evaluate the Response to Treatment in Solid Tumors
Therasse, P., Arbuck, S. G., Eisenhauer, E. A., Wanders, J., Kaplan, R. S., Rubinstein, L., Verweij, J., Van Glabbeke, M., van Oosterom, A. T., Christian, M. C., et al. (2000) · JNCI: Journal of the National Cancer Institute · doi:10.1093/jnci/92.3.205 · Cited by 15,660
Toxicity and response criteria of the Eastern Cooperative Oncology Group
Oken, M. M., Creech, R. H., Tormey, D. C., Horton, J., Davis, T. E., Mcfadden, E. T., & Carbone, P. P. (1982) · American Journal of Clinical Oncology · doi:10.1097/00000421-198212000-00014 · Cited by 11,686
Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma
Mok, T. S., Wu, Y.-L., Thongprasert, S., Yang, C.-H., Chu, D.-T., Saijo, N., Sunpaweravong, P., Han, B., Margono, B., Ichinose, Y., et al. (2009) · New England Journal of Medicine · doi:10.1056/nejmoa0810699 · Cited by 8,261
Erlotinib in Previously Treated Non–Small-Cell Lung Cancer
Shepherd, F. A., Rodrigues Pereira, J., Ciuleanu, T., Tan, E. H., Hirsh, V., Thongprasert, S., Campos, D., Maoleekoonpiroj, S., Smylie, M., Martins, R., et al. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa050753 · Cited by 5,419
EGFR Mutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib
Kobayashi, S., Boggon, T. J., Dayaram, T., Jänne, P. A., Kocher, O., Meyerson, M., Johnson, B. E., Eck, M. J., Tenen, D. G., & Halmos, B. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa044238 · Cited by 3,964
Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the National Cancer Institute of Canada Clinical Trials Group
Moore, M. J., Goldstein, D., Hamm, J., Figer, A., Hecht, J. R., Gallinger, S., Au, H. J., Murawa, P., Walde, D., Wolff, R. A., et al. (2007) · Journal of Clinical Oncology · doi:10.1200/jco.2006.07.9525 · Cited by 3,848
Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain
Pao, W., Miller, V. A., Politi, K. A., Riely, G. J., Somwar, R., Zakowski, M. F., Kris, M. G., & Varmus, H. (2005) · PLoS Medicine · doi:10.1371/journal.pmed.0020073 · Cited by 3,527
Lapatinib plus Capecitabine for HER2-Positive Advanced Breast Cancer
Geyer, C. E., Forster, J. K., Lindquist, D. L., Chan, S. Y. T., Romieu, C. G., Pieńkowski, T., Jagiełło-Gruszfeld, A., Crown, J. P., Chan, A., Kaufman, B., et al. (2006) · New England Journal of Medicine · doi:10.1056/nejmoa064320 · Cited by 3,458
ERBB receptors and cancer: the complexity of targeted inhibitors
Hynes, N. E., & Lane, H. A. (2005) · Nature reviews. Cancer · doi:10.1038/nrc1609 · Cited by 3,379
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Solca F, Proceedings of the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, 118
Agus DB, 2006, J Clin Oncol, 24, 97s
Lewis N, 2006, J Clin Oncol, 24, 143s
Shih JY, 2009, J Clin Oncol, 27, 410s

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A phase I dose escalation study of BIBW 2992, an irreversible dual EGFR/HER2 receptor tyrosine kinase inhibitor, in a continuous schedule in patients with advanced solid tumours
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A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours
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A phase I dose escalation study of BIBW 2992, an irreversible dual EGFR/HER2 receptor tyrosine kinase inhibitor, in a 3 week on 1 week off schedule in patients with advanced solid tumors
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A phase I dose escalation study of BIBW 2992, an irreversible dual EGFR/HER2 receptor tyrosine kinase inhibitor, in patients with advanced solid tumours
Shaw, H. M., Plummer, R., Vidal, L., Perrett, R. M., Pilkington, M., Temple, G., Fong, P. C. C., Amelsberg, A., Calvert, H., & Bono, J. S. D. (2006) · Journal of Clinical Oncology · doi:10.1200/jco.2006.24.18_suppl.3027 · Cited by 22
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Authors: Yap, T. A., Vidal, L., Adam, J., Stephens, P., Spicer, J., Shaw, H., Ang, J., Temple, G., Bell, S., Shahidi, M., Uttenreuther-Fischer, M., Stopfer, P., Futreal, A., Calvert, H., de Bono, J. S., & Plummer, R.
Affiliations: Royal Marsden NHS Foundation Trust (GB)
National Health Service (GB)
From the Drug Development Unit, the Royal Marsden National Health Service Foundation Trust, and The Institute of Cancer Research, Sutton, Surrey; Northern Institute for Cancer Research, Newcastle upon Tyne; Boehringer Ingelheim, Bracknell; Wellcome Trust Sanger Institute, Hinxton, Cambridge, United Kingdom; and Boehringer Ingelheim Pharma GmbH & Co KG, Biberach, Germany.
ORCID: Yap, Timothy A.
Vidal, Laura
Spicer, James
Shaw, Heather
Stopfer, Peter
Plummer, Ruth
Venue: Journal of Clinical Oncology
Publisher: American Society of Clinical Oncology (ASCO)
Published: 2010-09-01
Volume: 28
Issue: 25
Pages: 3965-3972
ISSN: 0732-183X (ISSN-L)
1527-7755
DOI: 10.1200/jco.2009.26.7278
OpenAlex: W2114095518
Cited by: 349
References: 34
Citations by year: 2026: 3 · 2025: 6 · 2024: 7 · 2023: 14 · 2022: 4 · 2021: 12 · 2020: 8 · 2019: 12 · 2018: 18 · 2017: 18 · 2016: 33 · 2015: 40 · 2014: 47 · 2013: 42 · 2012: 48
FWCI: 33.76
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Journal of Clinical Oncology (publishedVersion)
PubMed (publishedVersion)
UCL Discovery (University College London) (submittedVersion)
Newcastle University ePrints (Newcastle Univesity)
Funders: AstraZeneca
American Society of Clinical Oncology
Royal Marsden NHS Foundation Trust
NIHR Biomedical Research Centre, Royal Marsden NHS Foundation Trust/Institute of Cancer Research
Cancer Research UK
National Institute for Health and Care Research
Newcastle University
Genentech
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
Health Sciences › Medicine › Oncology › Gastric Cancer Management and Outcomes
Keywords: afatinib, irreversible kinase inhibitors, EGFR, HER2, EGF receptor, T790M mutation, advanced solid tumors, non-small cell lung cancer, pharmacokinetics, food effect, safety, maximum tolerated dose, anticancer activity, brain metastases, esophageal cancer
MeSH terms: Afatinib, Adult, Aged, Drug Administration Schedule, Female, Humans, Male, Middle Aged, Neoplasms, Quinazolines, Erb-b2 Receptor Tyrosine Kinases, Protein Kinase Inhibitors, ErbB Receptors

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Phase I Trial of the Irreversible EGFR and HER2 Kinase Inhibitor BIBW 2992 in Patients With Advanced Solid Tumors

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