Abstract
Colorectal cancer (CRC) is one of the most common malignancies worldwide, with high morbidity and mortality rates. Conventional treatments, including surgery, radiotherapy, and chemotherapy, have limited effects on advanced and metastatic CRC (mCRC). Fruquintinib, a novel and highly selective vascular endothelial growth factor receptor (VEGFR) inhibitor, has shown significant efficacy and tolerance in treating mCRC. The FRESCO and FRESCO-2 trials demonstrated that fruquintinib significantly prolongs progression-free survival and the overall survival of refractory mCRC patients, establishing it as the standard third-line treatment strategy for mCRC. In addition, the combination of fruquintinib with other anticancer drugs and immune checkpoint inhibitors demonstrated potential for enhanced efficacy, which warrants further exploration. In this review, we aimed to systematically summarize the current knowledge about the pharmacological mechanisms, pharmacokinetic characteristics, adverse events, and corresponding treatment options of fruquintinib and provide an update on the clinical trials related to fruquintinib in CRC by conducting a comprehensive literature search of PubMed and consulting the relevant clinical trials via ClinicalTrials.gov and the ChiCTR website, aiming to offer new insights into the role of fruquintinib in the comprehensive treatment of CRC.