Icotinib, a selective EGF receptor tyrosine kinase inhibitor, for the treatment of non-small-cell lung cancer

Papers of special note have been highlighted as: • of interest; •• of considerable interest

References

• 1 Siegel R, Naishadham D, Jemal A. Cancer statistics, 2013. CA Cancer J. Clin. 63(1), 11–30 (2013).
  MedlineGoogle Scholar
• 2 Chen W, Zheng R, Zhang S et al. Report of incidence and mortality in China cancer registries, 2009. Chin. J. Cancer Res. 25(1), 10–21 (2013).
  Medline CASGoogle Scholar
• 3 Govindan R, Page N, Morgensztern D et al. Changing epidemiology of small-cell lung cancer in the United States over the last 30 years: analysis of the surveillance, epidemiologic, and end results database. J. Clin. Oncol. 24(2), 4539–4544 (2006).
  MedlineGoogle Scholar
• 4 Deb TB, Su L, Wong L et al. Epidermal growth factor (EGF) receptor kinase-independent signaling by EGF. J. Biol. Chem. 276(18), 15554–15560 (2001).
  Medline CASGoogle Scholar
• 5 Woodburn JR. The epidermal growth factor receptor and its inhibition in cancer therapy. Pharmacol. Ther. 82, 241–250 (1999).
  Medline CASGoogle Scholar
• 6 Yarden Y, Sliwkowski MX. Untangling the ErbB signalling network. Nat. Rev. Mol. Cell Biol. 2, 127–137 (2001).
  Medline CASGoogle Scholar
• 7 Scott WJ, Howington J, Feigenberg S, Movsas B, Pisters K. American College of Chest Physicians. Treatment of non-small cell lung cancer stage I and stage II: ACCP evidence-based clinical practice guidelines (2nd Edition). Chest 132(3 Suppl.), S234–S242 (2007).
  Google Scholar
• 8 Schiller JH, Harrington D, Belani CP et al. Eastern Cooperative Oncology Group: comparison of four chemotherapy regimens for advanced non-small-cell lung cancer. N. Engl. J. Med. 346(2), 92–98 (2002).
  Medline CASGoogle Scholar
• 9 Domvri K, Darwiche K, Zarogoulidis P, Zarogoulidis K. Following the crumbs: from tissue samples, to pharmacogenomics, to NSCLC therapy. Transl. Lung Cancer Res. 2(4), 256–258 (2003).
  Google Scholar
• 10 Kim ES, Hirsh V, Mok T et al. Gefitinib versus docetaxel in previously treated non-small-cell lung cancer (INTEREST): a randomised Phase III trial. Lancet 372(9652), 1809–1818 (2008).
  Medline CASGoogle Scholar
• 11 Shepherd FA, Rodrigues Pereira J, Ciuleanu T et al. Erlotinib in previously treated non-small-cell lung cancer. N. Engl. J. Med. 353, 123–132 (2005).
  Medline CASGoogle Scholar
• 12 Mitsudomi T, Morita S, Yatabe Y et al. Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harboring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomized Phase 3 trial. Lancet Oncol. 11(2), 121–128 (2010).
  Medline CASGoogle Scholar
• 13 Maemondo M, Inoue A, Kobayashi K et al. Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. N. Engl. J. Med. 362(25), 2380–2388 (2010).
  Medline CASGoogle Scholar
• 14 Zhou C, Wu YL, Chen G et al. Erlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, Phase 3 study. Lancet Oncol. 12(8), 735–742 (2011).
  Medline CASGoogle Scholar
• 15 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. 13(3), 239–246 (2012).
  Medline CASGoogle Scholar
• 16 Mok TS, Wu YL, Thongprasert S et al. Gefitinib or carboplatin–paclitaxel in pulmonary adenocarcinoma. N. Engl. J. Med. 361(10), 947–957 (2009).
  Medline CASGoogle Scholar
• 17 Sequist LV, Yang JCH, 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. 31(27), 3327–3334 (2013).
  Medline CASGoogle Scholar
• 18 Yang JCH, Hirsh V, Schuler M et al. Symptom control and quality of life in LUX-Lung 3: a Phase III study of afatinib or cisplatin/pemetrexed in patients with advanced lung adenocarcinoma with EGFR mutations. J. Clin. Oncol. 31(27), 3342–3350 (2013).
  Medline CASGoogle Scholar
• 19 Shi Y, Zhang L, Liu X et al. Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind Phase 3 non-inferiority trial. Lancet Oncol. 14(10), 953–961 (2013).• This paper reported the registered, Phase III randomized controlled trial (ICOGEN) in which noninferiority of icotinib to gefitinib was established. Based on this study, icotinib was approved in China for unselected non-small-cell lung cancer patients as second-line or multiple-line treatment.
  Medline CASGoogle Scholar
• 20 Fenlai Tan, Aiqin Gu, Yiping Zhang et al. Safety and efficacy results of a Phase IV, open-label, multicenter, safety-monitoring study of icotinib in treating advanced non-small cell lung cancer (NSCLC): ISAFE study. Presented at: 2013 ASCO Annual Meeting. Chicago, IL, USA, 31 May–4 June 2013.
  Google Scholar
• 21 Hu S, Xie G, Zhang DX et al. Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors. Bioorg. Medicin. Chem. Lett. 22(19), 6301–6305 (2012).
  Medline CASGoogle Scholar
• 22 Mu X, Zhang Y, Qu X et al. Ubiquitin ligase Cbl-b is involved in icotinib (BPI-2009H)-induced apoptosis and G1 phase arrest of EGFR mutation-positive non-small-cell lung cancer. Biomed. Res. Int. 2013, 726375 (2013).
  MedlineGoogle Scholar
• 23 Gao Z, Chen W, Zhang X et al. Icotinib, a potent and specific EGFR tyrosine kinase inhibitor, inhibits growth of squamous cell carcinoma cell line A431 through negatively regulating AKT signaling. Biomed. Pharmacother. 67(5), 351–356 (2013).
  Medline CASGoogle Scholar
• 24 Zhejiang Beta Pharma Ltd. ZL03108814.7 (2007).
  Google Scholar
• 25 Tan F, Shen X, Wang D et al. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer 76(2), 177–182 (2012).•• Demonstrated the antitumor activities of icotinib at molecular and cell level.
  MedlineGoogle Scholar
• 26 Ding Yanqi, Jiang Beilei, Bao Yangyi. In vivo cytotoxicity effects of CIK cells combined with icotinib against lung adenocarcinoma cells. Acta Univers. Med. Anhui 48(8), 893–897 (2013).
  CASGoogle Scholar
• 27 Xu Ling, Zhang Ye, Qu Xiujuan et al. Icotinib increases the sensitivity of gastric cancer cells to tumor necrosis factor-related apoptosis-inducing ligand. Modern Oncol. 21(6), 1174–1177 (2013).
  CASGoogle Scholar
• 28 Guan Z, Chen X, Wang Y, Zhong D. Metabolite identification of a new antitumor agent icotinib in rats using liquid chromatography/tandem mass spectrometry. Rapid Commun. Mass Spectrom. 22(14), 2176–2184 (2008).
  Medline CASGoogle Scholar
• 29 Liu D, Jiang J, Zhang L et al. Clinical pharmacokinetics of Icotinib, an anti-cancer drug: evaluation of dose proportionality, food effect, and tolerability in healthy subjects. Cancer Chemother. Pharmacol. 73(4), 721–727 (2014).
  Medline CASGoogle Scholar
• 30 Zhao Q, Shentu J, Xu N et al. Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors. Lung Cancer. 73(2), 195–202 (2011).•• Paper about both the pharmacokinetics and activity of icotinib in heavily treated non-small-cell lung cancer patients, the recommended dose for Phase III study was also established in this study.
  MedlineGoogle Scholar
• 31 Ranson M, Hammond LA, Ferry D et al. ZD1839, a selective oral epidermal growth factor receptor–tyrosine kinase inhibitor, is well tolerated and active in patients with solid, malignant tumors: results of a Phase I trial. J. Clin. Oncol. 20(9), 2240–2250 (2002).
  Medline CASGoogle Scholar
• 32 Hidalgo M, Siu LL, Nemunaitis J et al. Phase I and pharmacologic study of OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. J. Clin. Oncol. 19(13), 3267–3279 (2001).
  Medline CASGoogle Scholar
• 33 Murakami H, Tamura T, Takahashi T et al. Phase I study of continuous afatinib (BIBW 2992) in patients with advanced non-small cell lung cancer after prior chemotherapy/erlotinib/gefitinib (LUX-Lung 4). Cancer Chemother. Pharmacol. 69(4), 891–899 (2012).
  Medline CASGoogle Scholar
• 34 Xin Zhang, Yang Zhao, Pei Hu, Ji Jiang. The effects of icotinib hydrochloride on rat CYP450. Presented at: 9th Conference on Chineses Drug and Xenobiotics Metabolism. Wuhan, China, October 24–26 2009.
  Google Scholar
• 35 Ruan CJ, Liu DY, Jiang J, Hu P. Effect of the CYP2C19 genotype on the pharmacokinetics of icotinib in healthy male volunteers. Eur. J. Clin. Pharmacol. 68(12), 1677–1680 (2012).
  Medline CASGoogle Scholar
• 36 Song Z, Yu X, Cai J et al. Efficacy of icotinib for advanced non-small cell lung cancer patients with EGFR status identified. Zhongguo Fei Ai Za Zhi 16(3), 138–143 (2013).
  Medline CASGoogle Scholar
• 37 Jianzhong Shentu, Guolan Wu, Jian Liu et al. An open-label, dose-escalating, Phase I trial to evaluate the tolerability and antitumor activity of icotinib in patients with advanced non-small-cell lung cancer. Presented at: 15th World Conference on Lung Cancer (15th WCLC). Sydney, Australia, 27–30 October 2013.
  Google Scholar
• 38 Wang HP, Zhang L, Wang YX et al. Phase I trial of icotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor, in Chinese patients with non-small cell lung cancer. Chin. Med. J. (Engl.) 124(13), 1933 (2011).
  Medline CASGoogle Scholar
• 39 Gu Qin A, Han Hui B, Jiang Yan L et al. Clinical observation from the treatment of icotinib for 196 cases with advanced non-small cell lung cancer. Presented at: 15th World Conference on Lung Cancer (15th WCLC). Sydney, Australia, 27–30 October 2013.
  Google Scholar
• 40 Lv C, Ma Y, Feng Q et al. A pilot study: sequential gemcitabine/cisplatin and icotinib as induction therapy for stage IIB to IIIA non-small-cell lung adenocarcinoma. World J. Surg. Oncol. 11, 96 (2013).
  MedlineGoogle Scholar
• 41 Xinjie Y, Hui Z, Na Q et al. Clinical observation of icotinib hydrochloride in first-line therapy for pulmonary adenocarcinoma. Chin. J. Lung Cancer 16(7), 364–368 (2013).
  Google Scholar
• 42 Ren GJ, Zhao YY, Zhu YJ et al. Tumor gene mutations and messenger RNA expression: correlation with clinical response to icotinib hydrochloride in non-small cell lung cancer. Chin. Med. J. (England) 124(1), 19–25 (2011).
  Medline CASGoogle Scholar
• 43 Icotinib Versus First-line Chemotherapy Plus Maintenance Treatment in EGFR Positive Lung Adenocarcinoma Patients (Convince). www.clinicaltrials.gov/ct2/show/NCT01719536?term=NCT01719536&rank=1.
  Google Scholar
• 44 Icotinib Treat the Patient With Brain Metastasis Epidermal Growth Factor Receptor (EGFR) Mutant Non Small Cell Lung Cancer Comparing With Whole Brain Radiotherapy (BRAIN). www.clinicaltrials.gov/ct2/show/NCT01724801?term=NCT01724801&rank=1.
  Google Scholar
• 45 Miller VA, Hirsh V, Cadranel J et al. Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a Phase 2b/3 randomised trial[J]. Lancet Oncol. 13(5), 528–538 (2012).
  Medline CASGoogle Scholar
• 46 Lynch TJ, Bell DW, Sordella R et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N. Engl. J. Med. 350(21), 2129–2139 (2004).
  Medline CASGoogle Scholar
• 47 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. USA 101(36), 13306–13311 (2004).
  Medline CASGoogle Scholar
• 48 Liang W, Wu X, Fang W et al. Network meta-analysis of erlotinib, gefitinib, afatinib and icotinib in patients with advanced non-small-cell lung cancer harboring EGFR mutations. PLoS ONE 9(2), e85245 (2014).
  MedlineGoogle Scholar
• 49 Yang JCH, Shih JY, Su WC et al. Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a Phase 2 trial. Lancet Oncol. 13(5), 539–548 (2012).
  Medline CASGoogle Scholar
• 50 Sequist LV, Yang JCH, 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. 31(27), 3327–3334 (2013).
  Medline CASGoogle Scholar
• 51 Cappuzzo F, Ciuleanu T, Stelmakh L et al. Erlotinib as maintenance treatment in advanced non-small-cell lung cancer: a multicentre, randomised, placebo-controlled Phase 3 study. Lancet Oncol. 11(6), 521–529 (2010).
  Medline CASGoogle Scholar
• 52 Zhang L, Ma S, Song X et al. Gefitinib versus placebo as maintenance therapy in patients with locally advanced or metastatic non-small-cell lung cancer (INFORM; C-TONG 0804): a multicentre, double-blind randomised Phase 3 trial. Lancet Oncol. 13(5), 466–475 (2012).
  Medline CASGoogle Scholar
• 53 Gaafar RM, Surmont VF, Scagliotti GV et al. A double-blind, randomised, placebo-controlled Phase III intergroup study of gefitinib in patients with advanced NSCLC, non-progressing after first line platinum-based chemotherapy (EORTC 08021/ILCP 01/03). Eur. J. Cancer 47(15), 2331–2340 (2011).
  Medline CASGoogle Scholar
• 54 Janjigian YY, Park BJ, Zakowski MF et al. Impact on disease-free survival of adjuvant erlotinib or gefitinib in patients with resected lung adenocarcinomas that harbor epidermal growth factor receptor (EGFR) mutations. J. Thorac Oncol. 6(3), 569–575 (2011).
  MedlineGoogle Scholar
• 55 Richardson F, Richardson K, Young D et al. O28.01 select biomarker analyses of completely resected NSCLC tumors from enrolled patients in an adjuvant erlotinib (Tarceva) clinical trial (RADIANT). Presented at: 14th World Conference on Lung Cancer (WCLC). Amsterdam, The Netherlands, 6 July 2011.
  Google Scholar
• 56 Li N, Ou W, Ye X et al. Pemetrexed-carboplatin adjuvant chemotherapy with or without gefitinib in resected stage IIIA-N2 non-small cell lung cancer harbouring EGFR mutations: a randomized, Phase II study. Ann. Surg. Oncol. 2014, 1–6 (2014).
  Google Scholar
• 57 Song Z, Yu X, Cai J et al. Efficacy of icotinib for advanced non-small cell lung cancer patients with EGFR status identified. Zhongguo Fei Ai Za Zhi 16(3), 138–143 (2013).
  Medline CASGoogle Scholar
• 58 Carey KD, Garton AJ, Romero MS et al. Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib. Cancer Res. 66(16), 8163–8171 (2006).
  Medline CASGoogle Scholar
• 59 Li D, Ambrogio L, Shimamura T et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 27(34), 4702–4711 (2008).
  Medline CASGoogle Scholar
• 60 Qian K, Zheng Y. Pharmacoeconomic evaluation of EGFR-TKIs in the treatment of advanced non-small cell lung cancer. Chin. J. Drug Eval. 30(5), 305–308 (2013).
  Google Scholar