Li Jianxia, Cai Yue, Deng Yanhong
Department of Medical Oncology, The Sixth Affiliated Hospital, Guangdong Province Key Laboratory of Colorectal and Pelvic Floor Diseases, Sun Yat-Sen University, Guangzhou, Guangdong, 510655, People's Republic of China.
Curr Treat Options Oncol. 2021 Jun 7;22(7):55. doi: 10.1007/s11864-021-00852-1.
Intravenous administration of fluoropyrimidine-based chemotherapy has been the backbone of treatment in colorectal cancer (CRC) for decades. The availability of oral capecitabine has improved the tolerability and simplified combination schedules. In addition to capecitabine, several other oral drugs have proven efficacy, particularly in palliative treatment lines. Clinical guidelines describe several available third-line treatment options for metastatic CRC (mCRC), but few insights are provided to guide the selection and sequence. In this review, we describe the available evidence and most recent data concerning oral drugs with proven efficacy in CRC, including antiangiogenetic tyrosine kinase inhibitors (VEGFR TKIs), inhibitors blocking EGFR/Raf/MEK/ERK signaling pathway and modified fluoropyrimidine, and share recommendations and insights on selecting third-line oral therapies for mCRC in China. In general, third-line treatment options for mCRC are mainly regorafenib, fruquintinib, and chemo/targeted therapy reintroduction, while FTD/TPI was rarely used in China probably due to poor accessibility. Fruquintinib is preferred in patients with poor performance status (PS), elder age, and severe organ dysfunction, compared to regorafenib. New drugs of clinical trials were more recommended for the patients with BRAF mutant tumor, and those with good previous treatment efficacy tended to be recommended for chemo/targeted therapy reintroduction. The management of mCRC is evolving, and it must be emphasized that the consideration and recommendations presented here reflect current treatment practices in China and thus might change according to new clinical data as well as the availability of new oral drugs.
几十年来，基于氟嘧啶的静脉化疗一直是结直肠癌（CRC）治疗的主要手段。口服卡培他滨的出现提高了耐受性并简化了联合用药方案。除卡培他滨外，其他几种口服药物也已证实具有疗效，尤其是在姑息治疗线中。临床指南描述了转移性结直肠癌（mCRC）的几种可用的三线治疗选择，但在指导选择和用药顺序方面提供的见解很少。在本综述中，我们描述了关于在CRC中已证实具有疗效的口服药物的现有证据和最新数据，包括抗血管生成酪氨酸激酶抑制剂（VEGFR TKIs）、阻断EGFR/Raf/MEK/ERK信号通路的抑制剂和改良氟嘧啶，并分享了在中国选择mCRC三线口服疗法的建议和见解。一般来说，mCRC的三线治疗选择主要是瑞戈非尼、呋喹替尼以及重新引入化疗/靶向治疗，而FTD/TPI在中国很少使用，可能是因为可及性差。与瑞戈非尼相比，呋喹替尼更适合于体能状态（PS）差、年龄较大和器官功能严重障碍的患者。对于BRAF突变肿瘤患者，更推荐临床试验中的新药，而对于既往治疗效果良好的患者，倾向于推荐重新引入化疗/靶向治疗。mCRC的治疗正在不断发展，必须强调的是，这里提出的考虑因素和建议反映了中国目前的治疗实践，因此可能会根据新的临床数据以及新口服药物的可及性而发生变化。
