649
Views
19
CrossRef citations to date
0
Altmetric
Drug Evaluation

Rociletinib, a third generation EGFR tyrosine kinase inhibitor: current data and future directions

, &
Pages 989-993 | Received 22 Dec 2015, Accepted 03 Mar 2016, Published online: 04 Apr 2016

References

  • Paez JG, Jänne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science. 2004;304(5676):1497–1500.
  • Mok TS, Wu Y-L, Thongprasert S, et al. Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. N Engl J Med. 2009;361(10):947–957.
  • Rosell R, Carcereny E, Gervais R, et al. 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. Lancet Oncol. 2012;13(3):239–246.
  • Pao W, Miller V, Zakowski M, et al. EGF receptor gene mutations are common in lung cancers from ‘never smokers’ and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A. 2004;101(36):13306–13311.
  • Sequist LV, Yang JC-H, Yamamoto N, et al. Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations. J Clin Oncol. 2013;31(27):3327–3334.
  • Wu Y-L, Zhou C, Hu C-P, et al. Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial. Lancet Oncol. 2014;15(2):213–222.
  • Chong CR, Janne PA. The quest to overcome resistance to EGFR-targeted therapies in cancer. Nat Med. 2013;19(11):1389–1400.
  • Engelman JA, Zejnullahu K, Mitsudomi T, et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science. 2007;316(5827):1039–1043.
  • Turke AB, Zejnullahu K, Wu Y-L, et al. Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer Cell. 2010;17(1):77–88.
  • Ercan D, Xu C, Yanagita M, et al. Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov. 2012;2(10):934–947.
  • Moreira-Leite FF, Harrison LR, Mironov A, et al. Inducible EGFR T790M-mediated gefitinib resistance in non-small cell lung cancer cells does not modulate sensitivity to PI103 provoked autophagy. J Thorac Oncol. 2010;5(6):765–777.
  • Zhou W, Ercan D, Chen L, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009;462(7276):1070–1074.
  • Sequist LV, Soria J-C, Goldman JW, et al. Rociletinib in EGFR-mutated non-small-cell lung cancer. N Engl J Med. 2015;372(18):1700–1709.
  • Herbst RS, Prager D, Hermann R, et al. TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer. J Clin Oncol. 2005;23(25):5892–5899.
  • Sequist LV, Soria J-C, Gadgeel SM, et al. First-in-human evaluation of CO-1686, an irreversible, highly selective tyrosine kinase inhibitor of mutations of EGFR (activating and T790M). J Clin Oncol. 2014;32:5s (suppl; abstr 8010). ASCO Annual Meeting, Abstract 8010.
  • Sequist LV, Goldman J, Wakelee HA, et al. Efficacy of rociletinib (CO-1686) in plasma-genotyped T790M-positive NSCLC patients. J Clin Oncol 33, 2015 (suppl; abstr 8001). 2015 ASCO Annual Meeting Abstract 8001.
  • Goldman JW, Wakelee H, Gadgeel S, et al. Dose optimization of rociletinib for EGFR mutated NSCLC. 16th World Conference on Lung Cancer; Sep 2015; Denver, CO. Abstract # 967.
  • Wakelee H, Sequist LV, Gadgeel S, et al. Rociletinib in NSCLC patients with negative central testing for T790M in TIGER-X. 16th World Conference on Lung Cancer, Denver, CO; Sep 2015; Abstract # 951.
  • Solomon B, Wakelee H, Sequist LV, et al. Rociletinib treatment and outcomes in non-small cell lung cancer (NSCLC) patients with negative central testing for T790M. 18th ECCO – 40th ESMO European Cancer Congress, Vienna; 2015; Poster 356.
  • Heon S, Yeap BY, Lindeman NI, et al. The impact of initial gefitinib or erlotinib versus chemotherapy on central nervous system progression in advanced non-small cell lung cancer with EGFR mutations. Clin Cancer Res. 2012;18(16):4406–4414.
  • Camidge DR, Sequist LV, Soria J-C, et al. Activity of rociletinib in EGFR mutant NSCLC patients with a history of CNS involvement. 16th World Conference on Lung Cancer, Denver, CO; Sep 2015; Abstract # 965.
  • Karlovich C. Evaluation of EGFR mutations in plasma from NSCLC patients: utility in managing patients on TKI therapy. Cambridge Healthtech Institute CHI Digital PCR; Oct 2014; La Jolla.
  • Goldman J, Karlovich C, Mann E, et al. Abstract 927: pretreatment and serial plasma assessments of EGFR mutations in NSCLC patients treated with rociletinib (CO-1686). Apr 2015 AACR Annual Meeting, Philadelphia, PA; 2015.
  • Simmons AD, Jaw-Tsai S, Haringsma HJ, et al. Abstract 793: insulin-like growth factor 1 (IGF1R)/insulin receptor (INSR) inhibitory activity of rociletinib (CO-1686) and its metabolites in nonclinical models. 2015 AACR Annual Meeting Poster 793, Philadelphia, PA; Apr 2015.
  • Lin L, Bivona TG. Mechanisms of resistance to epidermal growth factor receptor inhibitors and novel therapeutic strategies to overcome resistance in NSCLC patients. Chemother Res Pract. 2012;2012:817297.
  • Janne PA, Yang JC-H, Kim D-W, et al. AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer. N Engl J Med. 2015;372(18):1689–1699.
  • Sequist LV, Piotrowska Z, Niederst MJ, et al. Osimertinib responses after disease progression in patients who had been receiving rociletinib. JAMA Oncol. Published online December 17, 2015.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.