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The clinical application of fruquintinib on colorectal cancer
1a Department of Pharmaceutical, Central Hospital of Linyi City , Yishui , Shandong , China.
Abstract:
Introduction: Anti-angiogenetic agents are currently the most commonly used drugs for the treatment of colorectal cancer (CRC) patients, including various inhibitors targeting the epidermal growth factor receptor (EGFR), vascular endothelial growth factor (VEGF), and VEGF receptors (VEGFRs). Fruquintinib (HMPL-013), a highly selective and long-term small-molecule inhibitor of VEGFR (VEGFR1, 2, and 3) was recently approved in China for CRC treatment. Clinical studies have shown it has many advantages, such as low off-target toxicity, good drug tolerance, and strong effect. Areas covered: In the review, the molecular structure, mechanism of action, pharmacokinetics, clinical efficacy, and safety of fruquintinib are introduced in detail. The potential clinic application on non-small cell lung cancer (NSCLC) and gastric cancer is also discussed. Expert commentary: Fruquintinib was approved for patients with metastatic colorectal cancer (RAS wild type) who have previously received fluorouracil, oxaliplatin, and irinotecan-based chemotherapy and who have received or are not suitable for anti- VEGF therapy and anti- EGFR therapy. As a novel, therapeutic approach to CRC, Fruquintinib could be used as a third-line drug for the treatment of CRC patients. Due to drug resistance during the long-term therapy, the combination of fruquintinib with other targeted therapy drugs may be an effective option for CRC treatment.
Insights
Fruquintinib is a new VEGFR inhibitor approved for colorectal cancer treatment. It shows advantages in efficacy and safety, offering a potential third-line therapy option.
Area of Science:
- Oncology
- Pharmacology
Background:
- Anti-angiogenic agents targeting EGFR, VEGF, and VEGFRs are standard for colorectal cancer (CRC).
- Fruquintinib, a selective VEGFR inhibitor, is approved in China for CRC treatment, demonstrating clinical advantages.
Purpose of the Study:
- To review the molecular aspects, pharmacokinetics, clinical efficacy, and safety of fruquintinib.
- To explore potential applications of fruquintinib in non-small cell lung cancer (NSCLC) and gastric cancer.
Main Methods:
- Detailed review of existing literature on fruquintinib.
- Analysis of clinical trial data regarding efficacy and safety profiles.
Main Results:
- Fruquintinib exhibits high selectivity for VEGFRs (1, 2, and 3) with low off-target toxicity.
- Clinical studies indicate good drug tolerance and significant efficacy in CRC patients.
Conclusions:
- Fruquintinib is approved as a third-line therapy for metastatic colorectal cancer (RAS wild type) patients.
- Combination therapy with fruquintinib may overcome drug resistance and enhance treatment outcomes in CRC.
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