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苹果酸舒尼替尼(sunitinib malate)是目前临床上使用的多靶点酪氨酸激酶抑制剂之一。可抑制包括表皮生长因子受体、血小板源性生长因子受体、血管内皮生长因子受体在内的80多种受体的酪氨酸激酶。而受体酪氨酸激酶(RTK)的突变和过度表达被证实与包括肺癌在内的多种肿瘤的发生及发展有关。因此部分学者进行了用舒尼替尼单药或联合化疗药物(如紫杉醇、吉西他滨+顺铂)治疗进展期非小细胞肺癌的临床试验,试验结果显示舒尼替尼对非小细盹肺癌有一定的疗效。其中舒尼替尼联合吉西他滨+顺铂的临床试验显示最大耐受剂量方案:舒尼替尼(37.5 mg口服1次/日,2/1方案)+吉西他滨(1000 mg/m~2,静脉用药,d1、8,3周方案,)+顺铂(80mg/m~2,静脉用药,d1,3周方案)的部分缓解率高达66.7%。而且在临床试验中出现的舒尼替尼的毒副作用大多为1～2级,大部分患者能较好耐受。这提示舒尼替尼在非小细胞肺癌的治疗上可能有一定的运用前景,但目前相关的研究仍较少,如对舒尼替尼在不同组织学类型及基因突变情况的非小细胞肺癌中疗效差异等的研究均未见报道。
Sunitinib malate is currently one of the multi-target tyrosine kinase inhibitors used clinically. Can inhibit the epidermal growth factor receptor, platelet-derived growth factor receptor, vascular endothelial growth factor receptor, including more than 80 receptor tyrosine kinases. Mutations and overexpression of receptor tyrosine kinases (RTKs) have been associated with the development and progression of a variety of tumors, including lung cancer. Therefore, some scholars conducted a clinical trial of advanced NSCLC with sunitinib monotherapy or combination chemotherapy drugs (such as paclitaxel, gemcitabine + cisplatin). The results showed that sunitinib had no effect on non-small nap lung cancer A certain effect. The clinical trial of sunitinib combined with gemcitabine + cisplatin showed that the maximum tolerated dose regimen: sunitinib (37.5 mg orally once daily, 2/1 regimen) + gemcitabine (1000 mg / m 2 intravenous , d1, 8, 3 weeks program) + cisplatin (80mg / m ~ 2, intravenous drug, d1, 3 weeks program) partial response rate as high as 66.7%. And most of the side effects of sunitinib appeared in clinical trials are 1 ~ 2 grade, most patients can tolerate better. This suggests that sunitinib in the treatment of non-small cell lung cancer may have some application prospects, but the current research is still relatively small, such as sunitinib in different histological types and gene mutations in non-small cell lung cancer In the efficacy of different studies have not been reported.