Wang Y
International Biomedical Communications, Frederick, MD, USA.
Drugs Today (Barc). 2010 Aug;46(8):557-66. doi: 10.1358/dot.2010.46.8.1516824.
Everolimus (also known as RAD-001; Afinitor®) is an orally active inhibitor of the intracellular protein kinase mammalian target of rapamycin. The U.S. Food and Drug Administration and the European Medicines Agency recently approved everolimus for the treatment of advanced renal cell carcinoma (RCC) on the basis of the results of a randomized phase III clinical trial. In the trial, 10 mg daily everolimus was effective and well tolerated by patients with advanced RCC, whose disease had progressed while under the treatment with sunitinib and/or sorafenib. Everolimus treatment led to 36% of 6-month progression-free survival (PFS) rate and 31% of 3-month PFS rate. Most of the adverse events were mild to moderate (grade 1-2) in severity. The most frequent grade 3-4 adverse events were stomatitis, fatigue, pneumonitis and infections. Clinical trials on everolimus in combination with sunitinib, sorafenib, imatinib and vatalanib for the treatment of RCC are ongoing.
依维莫司（也称为RAD - 001；飞尼妥®）是一种细胞内蛋白激酶哺乳动物雷帕霉素靶蛋白的口服活性抑制剂。基于一项随机III期临床试验的结果，美国食品药品监督管理局和欧洲药品管理局最近批准依维莫司用于治疗晚期肾细胞癌（RCC）。在该试验中，对于晚期RCC患者，每日服用10 mg依维莫司有效且耐受性良好，这些患者在接受舒尼替尼和/或索拉非尼治疗期间病情出现进展。依维莫司治疗使6个月无进展生存期（PFS）率达到36%，3个月PFS率达到31%。大多数不良事件的严重程度为轻度至中度（1 - 2级）。最常见的3 - 4级不良事件为口腔炎、疲劳、肺炎和感染。关于依维莫司联合舒尼替尼、索拉非尼、伊马替尼和凡他尼布治疗RCC的临床试验正在进行中。
