Antitumor activity of alectinib, a selective ALK inhibitor, in an ALK-positive NSCLC cell line harboring G1269A mutation

详细信息    查看全文

• 作者：Yasushi Yoshimura ; Mitsue Kurasawa ; Keigo Yorozu…
• 关键词：Anaplastic lymphoma kinase ; ALK ; Alectinib ; Resistance mutation ; ALK G1269A mutation
• 刊名：Cancer Chemotherapy and Pharmacology
• 出版年：2016
• 出版时间：March 2016
• 年：2016
• 卷：77
• 期：3
• 页码：623-628
• 全文大小：673 KB
• 参考文献：1.Soda M, Choi YL, Enomoto M, Takada S, Yamashita Y, Ishikawa S, Fujiwara S, Watanabe H, Kurashina K, Hatanaka H, Bando M, Ohno S, Ishikawa Y, Aburatani H, Niki T, Sohara Y, Sugiyama Y, Mano H (2007) Identification of the transforming EML4–ALK fusion gene in non-small-cell lung cancer. Nature 448(7153):561–566. doi:10.​1038/​nature05945 CrossRef PubMed
  2.Shaw AT, Kim DW, Nakagawa K, Seto T, Crino L, Ahn MJ, De Pas T, Besse B, Solomon BJ, Blackhall F, Wu YL, Thomas M, O’Byrne KJ, Moro-Sibilot D, Camidge DR, Mok T, Hirsh V, Riely GJ, Iyer S, Tassell V, Polli A, Wilner KD, Janne PA (2013) Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N Engl J Med 368(25):2385–2394. doi:10.​1056/​NEJMoa1214886 CrossRef PubMed
  3.Solomon BJ, Mok T, Kim DW, Wu YL, Nakagawa K, Mekhail T, Felip E, Cappuzzo F, Paolini J, Usari T, Iyer S, Reisman A, Wilner KD, Tursi J, Blackhall F, Investigators P (2014) First-line crizotinib versus chemotherapy in ALK-positive lung cancer. N Engl J Med 371(23):2167–2177. doi:10.​1056/​NEJMoa1408440 CrossRef PubMed
  4.Choi YL, Soda M, Yamashita Y, Ueno T, Takashima J, Nakajima T, Yatabe Y, Takeuchi K, Hamada T, Haruta H, Ishikawa Y, Kimura H, Mitsudomi T, Tanio Y, Mano H (2010) EML4–ALK mutations in lung cancer that confer resistance to ALK inhibitors. N Engl J Med 363(18):1734–1739. doi:10.​1056/​NEJMoa1007478 CrossRef PubMed
  5.Isozaki H, Takigawa N, Kiura K (2015) Mechanisms of acquired resistance to ALK inhibitors and the rationale for treating ALK-positive lung cancer. Cancers 7(2):763–783. doi:10.​3390/​cancers7020763 PubMedCentral CrossRef PubMed
  6.Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y (2011) CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell 19(5):679–690. doi:10.​1016/​j.​ccr.​2011.​04.​004 CrossRef PubMed
  7.Kodama T, Hasegawa M, Takanashi K, Sakurai Y, Kondoh O, Sakamoto H (2014) Antitumor activity of the selective ALK inhibitor alectinib in models of intracranial metastases. Cancer Chemother Pharmacol 74(5):1023–1028. doi:10.​1007/​s00280-014-2578-6 CrossRef PubMed
  8.Kodama T, Tsukaguchi T, Yoshida M, Kondoh O, Sakamoto H (2014) Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance. Cancer Lett 351(2):215–221. doi:10.​1016/​j.​canlet.​2014.​05.​020 CrossRef PubMed
  9.Katayama R, Lovly CM, Shaw AT (2015) Therapeutic targeting of anaplastic lymphoma kinase in lung cancer: a paradigm for precision cancer medicine. Clin Cancer Res 21(10):2227–2235. doi:10.​1158/​1078-0432.​CCR-14-2791 CrossRef PubMed
  10.Kim S, Kim TM, Kim DW, Go H, Keam B, Lee SH, Ku JL, Chung DH, Heo DS (2013) Heterogeneity of genetic changes associated with acquired crizotinib resistance in ALK-rearranged lung cancer. J Thorac Oncol 8(4):415–422. doi:10.​1097/​JTO.​0b013e318283dcc0​ CrossRef PubMed
  11.Yamashita-Kashima Y, Iijima S, Yorozu K, Furugaki K, Kurasawa M, Ohta M, Fujimoto-Ouchi K (2011) Pertuzumab in combination with trastuzumab shows significantly enhanced antitumor activity in HER2-positive human gastric cancer xenograft models. Clin Cancer Res 17(15):5060–5070. doi:10.​1158/​1078-0432.​ccr-10-2927 CrossRef PubMed
  12.Gadgeel SM, Gandhi L, Riely GJ, Chiappori AA, West HL, Azada MC, Morcos PN, Lee RM, Garcia L, Yu L, Boisserie F, Di Laurenzio L, Golding S, Sato J, Yokoyama S, Tanaka T, Ou SH (2014) Safety and activity of alectinib against systemic disease and brain metastases in patients with crizotinib–resistant ALK-rearranged non-small-cell lung cancer (AF-002JG): results from the dose-finding portion of a phase 1/2 study. Lancet Oncol 15(10):1119–1128. doi:10.​1016/​s1470-2045(14)70362-6 CrossRef PubMed
  13.Seto T, Kiura K, Nishio M, Nakagawa K, Maemondo M, Inoue A, Hida T, Yamamoto N, Yoshioka H, Harada M, Ohe Y, Nogami N, Takeuchi K, Shimada T, Tanaka T, Tamura T (2013) CH5424802 (RO5424802) for patients with ALK-rearranged advanced non-small-cell lung cancer (AF-001JP study): a single-arm, open-label, phase 1–2 study. Lancet Oncol 14(7):590–598. doi:10.​1016/​S1470-2045(13)70142-6 CrossRef PubMed
  14.Iwama E, Takayama K, Harada T, Okamoto I, Ookubo F, Kishimoto J, Baba E, Oda Y, Nakanishi Y (2015) Highly sensitive and quantitative evaluation of the EGFR T790M mutation by nanofluidic digital PCR. Oncotarget 6(24):20466–20473. doi:10.​18632/​oncotarget.​4058 PubMedCentral CrossRef PubMed
  
• 作者单位：Yasushi Yoshimura (1)
  Mitsue Kurasawa (1)
  Keigo Yorozu (1)
  Oscar Puig (2)
  Walter Bordogna (3)
  Naoki Harada (1)
  
  1. Product Research Department, Chugai Pharmaceutical Co., Ltd., 200 Kajiwara, Kamakura, Kanagawa, 247-8530, Japan
  2. Pharma Early Research and Development, F. Hoffmann-La Roche, 430 East 29th Street, New York, NY, 10016, USA
  3. Product Development, F. Hoffmann-La Roche, Grenzacherstrasse 124, 4070, Basel, Switzerland
  
• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Biomedicine
  Cancer Research
  Pharmacology and Toxicology
  Oncology
  
• 出版者：Springer Berlin / Heidelberg
• ISSN：1432-0843

文摘

Purpose Alectinib is a highly selective next-generation anaplastic lymphoma kinase (ALK) inhibitor. Although alectinib shows inhibitory activity against various crizotinib-resistant ALK mutations in studies using cell-free kinase assays and Ba/F3 cell-based assays, it has not been tested for efficacy against non-small cell lung cancer (NSCLC) with the ALK mutations.