Literature DB >> 27525836

Activity of erlotinib when dosed below the maximum tolerated dose for EGFR-mutant lung cancer: Implications for targeted therapy development.

Benjamin L Lampson1, Mizuki Nishino2, Suzanne E Dahlberg3,4, Danie Paul3, Abigail A Santos5, Pasi A Jänne1,5, Geoffrey R Oxnard1,5.   

Abstract

BACKGROUND: Erlotinib is a standard first-line therapy for patients who have metastatic nonsmall cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) mutations. The recommended dose of 150 mg daily is the maximum tolerated dose (MTD). Few clinical data are available regarding its efficacy at doses less than the MTD.
METHODS: An institutional database was queried for patients with advanced NSCLC who were positive for EGFR L858R mutations or exon 19 deletions and had received treatment with erlotinib. The treatment course, including the erlotinib dose at initiation of treatment, at 4 months into therapy, and at disease progression, was retrospectively studied. Progression-free survival (PFS) was compared between patients who received the MTD (150 mg) and those who received reduced-dose erlotinib (≤100 mg).
RESULTS: In total, 198 eligible patients were identified. Thirty-one patients (16%) were initiated on reduced-dose erlotinib; they were older (P = .001) and had lower performance status (P = .01) compared with those who were initiated on erlotinib at the MTD. The response rate to reduced-dose erlotinib was 77%. The median PFS of patients initiated on reduced-dose erlotinib was 9.6 months versus 11.4 months for those initiated at the MTD, a difference that was not statistically significant (hazard ratio, 0.81; 95% confidence interval, 0.54-1.21; P = .30). There was a nonsignificant trend toward higher rates of progression within the central nervous system with reduced-dose erlotinib.
CONCLUSIONS: At doses below the MTD, erlotinib treatment results in a high response rate and a prolonged median PFS. Review of the literature indicates that 15 of 30 small-molecule inhibitors that are approved or in late-stage development for cancer therapy have recommended doses below the MTD. When the toxicities of MTD dosing are a concern, an investigation of small-molecule inhibitors at doses below the MTD is warranted. Cancer 2016;122:3456-63.
© 2016 American Cancer Society. © 2016 American Cancer Society.

Entities:  

Keywords:  epidermal growth factor receptor (EGFR) gene; erlotinib; molecular-targeted therapy; nonsmall cell lung carcinoma; pharmacokinetics

Year:  2016        PMID: 27525836      PMCID: PMC5311035          DOI: 10.1002/cncr.30270

Source DB:  PubMed          Journal:  Cancer        ISSN: 0008-543X            Impact factor:   6.860


  27 in total

1.  Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial.

Authors:  Rafael Rosell; Enric Carcereny; Radj Gervais; Alain Vergnenegre; Bartomeu Massuti; Enriqueta Felip; Ramon Palmero; Ramon Garcia-Gomez; Cinta Pallares; Jose Miguel Sanchez; Rut Porta; Manuel Cobo; Pilar Garrido; Flavia Longo; Teresa Moran; Amelia Insa; Filippo De Marinis; Romain Corre; Isabel Bover; Alfonso Illiano; Eric Dansin; Javier de Castro; Michele Milella; Noemi Reguart; Giuseppe Altavilla; Ulpiano Jimenez; Mariano Provencio; Miguel Angel Moreno; Josefa Terrasa; Jose Muñoz-Langa; Javier Valdivia; Dolores Isla; Manuel Domine; Olivier Molinier; Julien Mazieres; Nathalie Baize; Rosario Garcia-Campelo; Gilles Robinet; Delvys Rodriguez-Abreu; Guillermo Lopez-Vivanco; Vittorio Gebbia; Lioba Ferrera-Delgado; Pierre Bombaron; Reyes Bernabe; Alessandra Bearz; Angel Artal; Enrico Cortesi; Christian Rolfo; Maria Sanchez-Ronco; Ana Drozdowskyj; Cristina Queralt; Itziar de Aguirre; Jose Luis Ramirez; Jose Javier Sanchez; Miguel Angel Molina; Miquel Taron; Luis Paz-Ares
Journal:  Lancet Oncol       Date:  2012-01-26       Impact factor: 41.316

2.  Cerebrospinal fluid concentration of gefitinib and erlotinib in patients with non-small cell lung cancer.

Authors:  Yosuke Togashi; Katsuhiro Masago; Satohiro Masuda; Tomoyuki Mizuno; Masahide Fukudo; Yasuaki Ikemi; Yuichi Sakamori; Hiroki Nagai; Young Hak Kim; Toshiya Katsura; Michiaki Mishima
Journal:  Cancer Chemother Pharmacol       Date:  2012-07-18       Impact factor: 3.333

3.  Erlotinib in patients with advanced non-small-cell lung cancer: impact of dose reductions and a novel surrogate marker.

Authors:  Daniel Binder; Ann-Christin Buckendahl; Ralf-Harto Hübner; Peter Schlattmann; Bettina Temmesfeld-Wollbrück; Thomas Beinert; Norbert Suttorp
Journal:  Med Oncol       Date:  2010-12-14       Impact factor: 3.064

4.  Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors.

Authors:  Patricia M LoRusso; Charles M Rudin; Josina C Reddy; Raoul Tibes; Glen J Weiss; Mitesh J Borad; Christine L Hann; Julie R Brahmer; Ilsung Chang; Walter C Darbonne; Richard A Graham; Kenn L Zerivitz; Jennifer A Low; Daniel D Von Hoff
Journal:  Clin Cancer Res       Date:  2011-02-07       Impact factor: 12.531

5.  Erlotinib at a dose of 25 mg daily for non-small cell lung cancers with EGFR mutations.

Authors:  Wee-Lee Yeo; Gregory J Riely; Beow Y Yeap; Michelle W Lau; Jeremy L Warner; Kelly Bodio; Mark S Huberman; Mark G Kris; Daniel G Tenen; William Pao; Susumu Kobayashi; Daniel B Costa
Journal:  J Thorac Oncol       Date:  2010-07       Impact factor: 15.609

6.  Dramatic response to low-dose erlotinib of epidermal growth factor receptor mutation-positive recurrent non-small cell lung cancer after severe cutaneous toxicity.

Authors:  Joline S W Lind; Pieter E Postmus; Daniëlle A M Heideman; Erik B Thunnissen; Otto Bekers; Egbert F Smit
Journal:  J Thorac Oncol       Date:  2009-12       Impact factor: 15.609

7.  Functional analysis of epidermal growth factor receptor (EGFR) mutations and potential implications for EGFR targeted therapy.

Authors:  Rama Krishna Kancha; Nikolas von Bubnoff; Christian Peschel; Justus Duyster
Journal:  Clin Cancer Res       Date:  2009-01-15       Impact factor: 12.531

8.  Second- and third-line treatment of patients with non-small-cell lung cancer with erlotinib in the community setting: retrospective study of patient healthcare utilization and symptom burden.

Authors:  Edward J Stepanski; Arthur C Houts; Lee S Schwartzberg; Mark S Walker; Carolina M Reyes; Johnetta Blakely
Journal:  Clin Lung Cancer       Date:  2009-11       Impact factor: 4.785

9.  The concentration of erlotinib in the cerebrospinal fluid of patients with brain metastasis from non-small-cell lung cancer.

Authors:  Yanming Deng; Weineng Feng; Jing Wu; Zecheng Chen; Yicong Tang; Hua Zhang; Jianmiao Liang; Haibing Xian; Shunda Zhang
Journal:  Mol Clin Oncol       Date:  2013-09-23

10.  Efficacy of increased-dose erlotinib for central nervous system metastases in non-small cell lung cancer patients with epidermal growth factor receptor mutation.

Authors:  Yosuke Togashi; Katsuhiro Masago; Masahide Fukudo; Yasuhiro Tsuchido; Chiyuki Okuda; Young Hak Kim; Yasuaki Ikemi; Yuichi Sakamori; Tadashi Mio; Toshiya Katsura; Michiaki Mishima
Journal:  Cancer Chemother Pharmacol       Date:  2011-06-17       Impact factor: 3.333

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  5 in total

Review 1.  Paradigm shift of therapeutic management of brain metastases in EGFR-mutant non-small cell lung cancer in the era of targeted therapy.

Authors:  Akimasa Sekine; Hiroaki Satoh
Journal:  Med Oncol       Date:  2017-05-29       Impact factor: 3.064

2.  Difference in central nerve system metastasis during gefitinib or erlotinib therapy in patients with EGFR-mutated non-small cell lung cancer: a retrospective study.

Authors:  Kazushi Yoshida; Shintaro Kanda; Hideaki Shiraishi; Keiko Goto; Kota Itahashi; Yasushi Goto; Hidehito Horinouchi; Yutaka Fujiwara; Hiroshi Nokihara; Noboru Yamamoto; Yuichiro Ohe
Journal:  J Thorac Dis       Date:  2019-04       Impact factor: 2.895

Review 3.  Optimized Dosing: The Next Step in Precision Medicine in Non-Small-Cell Lung Cancer.

Authors:  René J Boosman; Jacobus A Burgers; Egbert F Smit; Neeltje Steeghs; Anthonie J van der Wekken; Jos H Beijnen; Alwin D R Huitema; Rob Ter Heine
Journal:  Drugs       Date:  2021-12-11       Impact factor: 9.546

4.  The clinical efficacy of Afatinib 30 mg daily as starting dose may not be inferior to Afatinib 40 mg daily in patients with stage IV lung Adenocarcinoma harboring exon 19 or exon 21 mutations.

Authors:  Chih-Jen Yang; Ming-Ju Tsai; Jen-Yu Hung; Mei-Hsuan Lee; Ying-Ming Tsai; Yu-Chen Tsai; Jui-Feng Hsu; Ta-Chih Liu; Ming-Shyan Huang; Inn-Wen Chong
Journal:  BMC Pharmacol Toxicol       Date:  2017-12-13       Impact factor: 2.483

5.  Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.

Authors:  Yumie Yamanaka; Akimasa Sekine; Terufumi Kato; Hideaki Yamakawa; Satoshi Ikeda; Tomohisa Baba; Tae Iwasawa; Koji Okudela; Takashi Ogura
Journal:  Intern Med       Date:  2017-09-25       Impact factor: 1.271

  5 in total

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