Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA.
Expert Opin Pharmacother. 2010 Aug;11(11):1943-55. doi: 10.1517/14656566.2010.496453.
Sorafenib is an oral receptor tyrosine kinase inhibitor that inhibits Raf serine/threonine kinases and receptor tyrosine kinases (vascular endothelial growth factor receptors 1, 2, 3 and platelet-derived growth factor-beta, Flt-3 and c-kit) that are implicated in tumorigenesis and tumor progression. Sorafenib is approved for the treatment of advanced inoperable hepatocellular cancer and advanced renal cell cancer.
The findings from the major Phase III studies that led to FDA approval of this drug for the above indications are reviewed. Key aspects of sorafenib pharmacology, dosing in the presence of organ dysfunction, toxicities and weaknesses of the research done so far are summarized.
The reader will have the knowledge of the major studies that form the basis of the clinical use of sorafenib, information on the upcoming Phase III trials that could lead to changes in clinical practice and some insights on aspects of the drugs' mechanism of action and toxicity that still remain unclear.
Sorafenib is a well-tolerated oral antiangiogenic agent approved for treatment of two angiogenesis-driven cancers. Studies to broaden the clinical indications and increase understanding of the clinical and laboratory biomarkers of response are needed.
索拉非尼是一种口服受体酪氨酸激酶抑制剂，可抑制丝氨酸/苏氨酸激酶和受体酪氨酸激酶（血管内皮生长因子受体 1、2、3 和血小板衍生生长因子-β、Flt-3 和 c-kit），这些激酶与肿瘤发生和肿瘤进展有关。索拉非尼被批准用于治疗不可切除的晚期肝细胞癌和晚期肾细胞癌。
审查了导致 FDA 批准该药物用于上述适应证的主要 III 期研究结果。总结了索拉非尼药理学、在器官功能障碍时的剂量、毒性以及迄今为止研究的弱点等关键方面。
读者将了解构成索拉非尼临床应用基础的主要研究，了解可能导致临床实践改变的即将进行的 III 期试验，并对药物作用机制和毒性的某些方面有一些深入了解，这些方面仍然不清楚。
索拉非尼是一种耐受性良好的口服抗血管生成药物，已被批准用于治疗两种血管生成驱动的癌症。需要进行研究来扩大临床适应证，并增加对反应的临床和实验室生物标志物的了解。
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