University of Genoa, San Martino Hospital and National Institute for Cancer Research, Department of Obstetrics and Gynecology , Largo R. Benzi 1, 16132 Genoa , Italy +01139 010511525 ; +01139 010511525 ;
Expert Opin Investig Drugs. 2013 Dec;22(12):1671-86. doi: 10.1517/13543784.2013.841138. Epub 2013 Sep 26.
Sunitinib malate (SU11248; Sutent®; Pfizer, Inc., New York) is a multi-kinase inhibitor currently approved for use in advanced renal cell carcinoma (RCC), imatinib-resistant/-intolerant gastrointestinal stromal tumours and progressive, well-differentiated pancreatic neuroendocrine tumours in patients with unresectable, locally advanced or metastatic disease.
This article describes the mechanism of action and of the pharmacokinetics of sunitinib; further, it summarizes Phase I and II trials on the clinical efficacy, tolerability and safety of this agent in the setting of ovarian cancer (OC) treatment.
On the basis of the current literature, sunitinib has shown modest antitumour activity and acceptable toxicity. Studies investigating the impact of horizontal and vertical combinations should represent a priority of future research. Although clinical Phase II trials on the use of sunitinib in the treatment of OC demonstrated an acceptable profile of AEs, a greater comprehension of the toxicity of this compound is recommended.
苹果酸舒尼替尼（SU11248；Sutent®；辉瑞公司，纽约）是一种多激酶抑制剂，目前被批准用于治疗晚期肾细胞癌（RCC）、伊马替尼耐药/不耐受的胃肠道间质瘤以及无法切除的局部晚期或转移性疾病患者的进展性、分化良好的胰腺神经内分泌肿瘤。
本文描述了舒尼替尼的作用机制和药代动力学；进一步总结了舒尼替尼在卵巢癌（OC）治疗中的临床疗效、耐受性和安全性的 I 期和 II 期试验。
根据目前的文献，舒尼替尼显示出适度的抗肿瘤活性和可接受的毒性。研究横向和纵向联合作用的影响应成为未来研究的重点。尽管在 OC 治疗中使用舒尼替尼的临床 II 期试验显示出可接受的不良反应谱，但建议更好地了解这种化合物的毒性。
