Abstract：
UNASSIGNED: Available treatments for colorectal cancer are limited. However, in the last few years several advances and new treatment options became available and expanded the continuum of care in metastatic colorectal cancer (mCRC).
UNASSIGNED: Fruquintinib, a tyrosine kinase inhibitor, has been shown to be effective in heavily pretreated mCRC progressing to trifluridine-tipiracil (FTD/TPI) or regorafenib or both. Preclinical studies have shown that fruquintinib inhibits with high selectivity VEGFR 1-2-3, leading to a blockade in angiogenesis process, but also acts, with weak inhibition, on RET, FGFR-1, and c-kit kinases. Fruquintinib demonstrated good efficacy and tolerance in chemorefractory mCRC in two phase III trial: FRESCO and FRESCO 2. These results led to FDA approval of fruquintinib for pretreated mCRC patients who received prior fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy.
UNASSIGNED: Fruquintinib is a valid therapeutic option for heavily pretreated mCRC patients. However, an optimal sequence of treatments is yet to be defined. In this review, we propose an algorithm for later lines of treatment to integrate fruquintinib as a standard of care together with the new therapeutic combinations that recently showed clinical benefit for chemorefractory mCRC, in both molecularly selected (e.g. KRASG12C or HER2 amplification) and in non-oncogenic driven patients.
UNASSIGNED: Fruquintinib, a tyrosine kinase inhibitor, has been shown to be effective in heavily pretreated mCRC progressing to trifluridine-tipiracil (FTD/TPI) or regorafenib or both. Preclinical studies have shown that fruquintinib inhibits with high selectivity VEGFR 1-2-3, leading to a blockade in angiogenesis process, but also acts, with weak inhibition, on RET, FGFR-1, and c-kit kinases. Fruquintinib demonstrated good efficacy and tolerance in chemorefractory mCRC in two phase III trial: FRESCO and FRESCO 2. These results led to FDA approval of fruquintinib for pretreated mCRC patients who received prior fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy.
UNASSIGNED: Fruquintinib is a valid therapeutic option for heavily pretreated mCRC patients. However, an optimal sequence of treatments is yet to be defined. In this review, we propose an algorithm for later lines of treatment to integrate fruquintinib as a standard of care together with the new therapeutic combinations that recently showed clinical benefit for chemorefractory mCRC, in both molecularly selected (e.g. KRASG12C or HER2 amplification) and in non-oncogenic driven patients.
摘要：
■结直肠癌的可用治疗方法有限。然而,在过去的几年中,在转移性结直肠癌(mCRC)中取得了一些进展和新的治疗选择,并扩大了治疗连续性.
■Fruquintinib，酪氨酸激酶抑制剂，已被证明对重度预处理的mCRC进展为氟尿苷-替哌嘧啶（FTD/TPI）或瑞戈非尼或两者均有效。临床前研究表明，氟喹替尼以高选择性抑制VEGFR1-2-3，导致血管生成过程的阻断，但也会采取行动，具有弱抑制作用，在RET上,FGFR-1和c-kit激酶。在FRESCO和FRESCO2两项III期试验中，Fruquintinib在化学难治性mCRC中表现出良好的疗效和耐受性。这些结果导致FDA批准氟喹替尼用于预先接受氟嘧啶治疗的mCRC患者，奥沙利铂-,和基于伊立替康的化疗。
■Fruquintinib是重度预处理mCRC患者的有效治疗选择。然而,治疗的最佳顺序尚未确定。在这次审查中,我们提出了一种算法，用于以后的治疗路线，将氟喹替尼作为标准护理与新的治疗组合整合在一起，这些新的治疗组合最近显示出对化学难治性mCRC的临床益处，在分子选择（例如KRASG12C或HER2扩增）和非致癌驱动的患者中。
■Fruquintinib，酪氨酸激酶抑制剂，已被证明对重度预处理的mCRC进展为氟尿苷-替哌嘧啶（FTD/TPI）或瑞戈非尼或两者均有效。临床前研究表明，氟喹替尼以高选择性抑制VEGFR1-2-3，导致血管生成过程的阻断，但也会采取行动，具有弱抑制作用，在RET上,FGFR-1和c-kit激酶。在FRESCO和FRESCO2两项III期试验中，Fruquintinib在化学难治性mCRC中表现出良好的疗效和耐受性。这些结果导致FDA批准氟喹替尼用于预先接受氟嘧啶治疗的mCRC患者，奥沙利铂-,和基于伊立替康的化疗。
■Fruquintinib是重度预处理mCRC患者的有效治疗选择。然而,治疗的最佳顺序尚未确定。在这次审查中,我们提出了一种算法，用于以后的治疗路线，将氟喹替尼作为标准护理与新的治疗组合整合在一起，这些新的治疗组合最近显示出对化学难治性mCRC的临床益处，在分子选择（例如KRASG12C或HER2扩增）和非致癌驱动的患者中。
