Phase I study of XL281 (BMS-908662), a potent oral RAF kinase inhibitor, in patients with advanced solid tumors
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  • 作者:Mark A. Dickson (1) (2)
    Michael S. Gordon (3)
    Gerald Edelman (4)
    Johanna C. Bendell (5)
    Ragini R. Kudchadkar (6)
    Patricia M. LoRusso (7)
    Stuart H. Johnston (8)
    Douglas O. Clary (8)
    Gary K. Schwartz (9)

    1. Memorial Sloan Kettering Cancer Center
    ; New York ; NY ; USA
    2. Weill Cornell Medical College
    ; New York ; NY ; USA
    3. Pinnacle Oncology Hematology
    ; Scottsdale ; AZ ; USA
    4. Mary Crowley Cancer Research Center
    ; Dallas ; TX ; USA
    5. Sarah Cannon Research Institute
    ; Nashville ; TN ; USA
    6. Emory University
    ; Atlanta ; GA ; USA
    7. Yale University
    ; New Haven ; CT ; USA
    8. Exelixis Inc.
    ; South San Francisco ; CA ; USA
    9. Columbia University Medical Center
    ; New York ; NY ; USA
  • 关键词:Phase I Trials ; Kinase inhibitors ; Pharmacokinetics and pharmacodynamics
  • 刊名:Investigational New Drugs
  • 出版年:2015
  • 出版时间:April 2015
  • 年:2015
  • 卷:33
  • 期:2
  • 页码:349-356
  • 全文大小:591 KB
  • 参考文献:1. Kolch, W, Kotwaliwale, A, Vass, K, Janosch, P (2002) The role of Raf kinases in malignant transformation. Expert Rev Mol Med 4: pp. 1-18 CrossRef
    2. Sebolt-Leopold, JS, Herrera, R (2004) Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer 4: pp. 937-947 CrossRef
    3. Bos, JL (1989) ras oncogenes in human cancer: a review. Cancer Res 49: pp. 4682-4689
    4. Davies, H, Bignell, GR, Cox, C, Stephens, P, Edkins, S, Clegg, S, Teague, J, Woffendin, H, Garnett, MJ, Bottomley, W, Davis, N, Dicks, E, Ewing, R, Floyd, Y, Gray, K, Hall, S, Hawes, R, Hughes, J, Kosmidou, V, Menzies, A, Mould, C, Parker, A, Stevens, C, Watt, S, Hooper, S, Wilson, R, Jayatilake, H, Gusterson, BA, Cooper, C, Shipley, J, Hargrave, D, Pritchard-Jones, K, Maitland, N, Chenevix-Trench, G, Riggins, GJ, Bigner, DD, Palmieri, G, Cossu, A, Flanagan, A, Nicholson, A, Ho, JW, Leung, SY, Yuen, ST, Weber, BL, Seigler, HF, Darrow, TL, Paterson, H, Marais, R, Marshall, CJ, Wooster, R, Stratton, MR, Futreal, PA (2002) Mutations of the BRAF gene in human cancer. Nature 417: pp. 949-954 CrossRef
    5. Satyamoorthy, K, Li, G, Gerrero, MR, Brose, MS, Volpe, P, Weber, BL, Belle, P, Elder, DE, Herlyn, M (2003) Constitutive mitogen-activated protein kinase activation in melanoma is mediated by both BRAF mutations and autocrine growth factor stimulation. Cancer Res 63: pp. 756-759
    6. Cohen, Y, Xing, M, Mambo, E, Guo, Z, Wu, G, Trink, B, Beller, U, Westra, WH, Ladenson, PW, Sidransky, D (2003) BRAF mutation in papillary thyroid carcinoma. J Natl Cancer Inst 95: pp. 625-627 CrossRef
    7. Kimura, ET, Nikiforova, MN, Zhu, Z, Knauf, JA, Nikiforov, YE, Fagin, JA (2003) High prevalence of BRAF mutations in thyroid cancer: genetic evidence for constitutive activation of the RET/PTC-RAS-BRAF signaling pathway in papillary thyroid carcinoma. Cancer Res 63: pp. 1454-1457
    8. Schwartz, GK, Robertson, S, Shen, A, Wang, E, Pace, L, Dials, H, Mendelson, D, Shannon, P, Gordon, M (2009) A phase I study of XL281, a selective oral RAF kinase inhibitor, in patients with advanced solid tumors. J Clin Oncol 27: pp. abstr 3513
    9. Sosman, JA, Kim, KB, Schuchter, L, Gonzalez, R, Pavlick, AC, Weber, JS, McArthur, GA, Hutson, TE, Moschos, SJ, Flaherty, KT, Hersey, P, Kefford, R, Lawrence, D, Puzanov, I, Lewis, KD, Amaravadi, RK, Chmielowski, B, Lawrence, HJ, Shyr, Y, Ye, F, Li, J, Nolop, KB, Lee, RJ, Joe, AK, Ribas, A (2012) Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med 366: pp. 707-714 CrossRef
    10. Chapman, PB, Hauschild, A, Robert, C, Haanen, JB, Ascierto, P, Larkin, J, Dummer, R, Garbe, C, Testori, A, Maio, M, Hogg, D, Lorigan, P, Lebbe, C, Jouary, T, Schadendorf, D, Ribas, A, O鈥橠ay, SJ, Sosman, JA, Kirkwood, JM, Eggermont, AM, Dreno, B, Nolop, K, Li, J, Nelson, B, Hou, J, Lee, RJ, Flaherty, KT, McArthur, GA, Group, B-S (2011) Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 364: pp. 2507-2516 CrossRef
    11. Hauschild, A, Grob, JJ, Demidov, LV, Jouary, T, Gutzmer, R, Millward, M, Rutkowski, P, Blank, CU, Miller, WH, Kaempgen, E, Martin-Algarra, S, Karaszewska, B, Mauch, C, Chiarion-Sileni, V, Martin, AM, Swann, S, Haney, P, Mirakhur, B, Guckert, ME, Goodman, V, Chapman, PB (2012) Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet 380: pp. 358-365 CrossRef
    12. Ascierto, PA, Minor, D, Ribas, A, Lebbe, C, O鈥橦agan, A, Arya, N, Guckert, M, Schadendorf, D, Kefford, RF, Grob, JJ, Hamid, O, Amaravadi, R, Simeone, E, Wilhelm, T, Kim, KB, Long, GV, Martin, AM, Mazumdar, J, Goodman, VL, Trefzer, U (2013) Phase II trial (BREAK-2) of the BRAF inhibitor Dabrafenib (GSK2118436) in patients with metastatic melanoma. J Clin Oncol 31: pp. 3205-3211 CrossRef
    13. Bollag, G, Hirth, P, Tsai, J, Zhang, J, Ibrahim, PN, Cho, H, Spevak, W, Zhang, C, Zhang, Y, Habets, G, Burton, EA, Wong, B, Tsang, G, West, BL, Powell, B, Shellooe, R, Marimuthu, A, Nguyen, H, Zhang, KY, Artis, DR, Schlessinger, J, Su, F, Higgins, B, Iyer, R, D鈥橝ndrea, K, Koehler, A, Stumm, M, Lin, PS, Lee, RJ, Grippo, J, Puzanov, I, Kim, KB, Ribas, A, McArthur, GA, Sosman, JA, Chapman, PB, Flaherty, KT, Xu, X, Nathanson, KL, Nolop, K (2010) Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 467: pp. 596-599 CrossRef
  • 刊物类别:Medicine
  • 刊物主题:Medicine & Public Health
    Oncology
    Pharmacology and Toxicology
  • 出版者:Springer Netherlands
  • ISSN:1573-0646
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