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索拉非尼的临床研究进展 被引量：4

Clinical development of sorafenib in cancer treatment
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摘要 索拉非尼是第1个口服的RAF激酶和酪氨酸激酶受体抑制剂，具有同时抑制肿瘤细胞增殖和血管生成的双重作用。Ⅰ期临床试验的推荐剂量是400mg每日2次口服，Ⅱ期及Ⅲ期临床试验表明索拉非尼对肾癌、肝癌、黑色素瘤和非小细胞肺癌都有一定的治疗作用。目前FDA已批准索拉非尼用于肾癌的治疗。 Sorafenib is the first oral multikinase inhibitor of Raf and tyrosine kinases receptor, so sorafenib can inhibit the tumor cell proliferation and neovascularization. Sorafenib 400 mg twice a day is chosen as the recommended dose for several phase Ⅱ studies, and it shows broad-spectrum antitumor activity in renal cancer, hepatocellular carcinoma, melanoma and non- small- cell lung cancer （ NSCLC ） in phase Ⅱ and Ⅲ clinical trials. Now,FDA has approved sorafenib using in renal cancer therapy.
作者 顾梅（综述） 卢凯华（审校） 刘连科（审校）
机构地区 南京医科大学第一附属医院肿瘤生物治疗中心
出处 《国际肿瘤学杂志》 CAS 2007年第3期185-187,共3页 Journal of International Oncology
关键词 索拉非尼 分子靶向治疗 Sorafenib Molecular targeting therapy
分类号 R730.53 [医药卫生—肿瘤]
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参考文献16

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同被引文献83

  • 1周爱萍,孙燕.多靶点抗肿瘤新药索拉非尼的研究进展[J].癌症进展,2006,4(6):529-533. 被引量：57
  • 2Muddassar. Docking and Quantum Mechanics Guided CoMFA Analysis of b-RAF Inhibitors [J]. Bull Korean Chem Soe, 2008, 29 (21): 1499-1505.
  • 3Paul DL. Identification of Amidoheteroaryls as Potent Inhibitors of Mutant (V600E) B-Raf Kinase with In Vivo Activity[J]. Bioorg Med Chem Lett, 2009, 19 (3): 1026-1029.
  • 4Jun T. Knowledge-based design of 7-azaindoles as selective B- Raf inhibitors [J]. Bioorg MedChem Lett, 2008, 18 (16): 4610-4614.
  • 5Clara M, Jeff S. Targeting the RAF-MEK-ERK pathway in cancer therapy [J]. Cancer Letters, 2009, 283 (2) : 125-134.
  • 6Nithya R, Alex A. Inhibitors of Raf kinase and MEK signaling [J].Update on cancer therapeutics, 2007, 2 (3): 111-118.
  • 7Yoon S, Seger R. The extracellular signal-regulated kinase: multiple substrates regulate diverse cellular functions [J].Growth Factors, 2006, 24 (1):21-44.
  • 8Ensar H, David BS. Therapeutic strategies for inhibiting oncogenic BRAF signaling[J]. Current Opinion in Pharmacology, 2008, 8 (4): 419-426.
  • 9Sharma SV, Settleman J. Oncogene addiction: setting the stage for molecularly targeted cancer therapy [J]. Genes Dev, 2007, 21 (24):3214-3231.
  • 10Sebolt Leopold JS. Advances in the development of cancer therapeutics directed against the RAS-mitogen activated protein kinase pathway [J]. Clin Cancer Res, 2008, 14 (12): 3651-3656.

引证文献4

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国际肿瘤学杂志
2007年 第3期

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