Metabolism, toxicity and management of fruquintinib: a novel drug for metastatic colorectal cancer.

Publisher: Informa Healthcare Country of Publication: England NLM ID: 101228422 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1744-7607 (Electronic) Linking ISSN: 17425255 NLM ISO Abbreviation: Expert Opin Drug Metab Toxicol Subsets: MEDLINE

Publication: London : Informa Healthcare
Original Publication: London : Ashley Publications, Ltd., c2005-

Colorectal Neoplasms*/drug therapy ; Colorectal Neoplasms*/pathology ; Benzofurans*/administration & dosage ; Benzofurans*/adverse effects ; Benzofurans*/pharmacology ; Antineoplastic Agents*/adverse effects ; Antineoplastic Agents*/administration & dosage ; Antineoplastic Agents*/pharmacokinetics ; Antineoplastic Agents*/pharmacology ; Neoplasm Metastasis* ; Protein Kinase Inhibitors*/adverse effects ; Protein Kinase Inhibitors*/administration & dosage ; Protein Kinase Inhibitors*/pharmacology ; Protein Kinase Inhibitors*/pharmacokinetics ; Quinazolines*/adverse effects ; Quinazolines*/administration & dosage ; Quinazolines*/pharmacokinetics ; Quinazolines*/pharmacology ; Receptors, Vascular Endothelial Growth Factor*/antagonists & inhibitors; Humans ; Animals ; Prognosis

Introduction: Colorectal cancer (CRC) is the third most diagnosed cancer globally and despite therapeutic strides, the prognosis for patients with metastatic disease (mCRC) remains poor. Fruquintinib is an oral vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor (TKI) targeting VEGFR -1, -2, and -3, and has recently received approval by the U.S. Food and Drug Administration for treatment of mCRC refractory to standard chemotherapy, anti-VEGF therapy, and anti-epidermal growth factor receptor (EGFR) therapy.
Areas Covered: This article provides an overview of the pre-clinical data, pharmacokinetics, clinical efficacy, and safety profile of fruquintinib, as well as the management of clinical toxicities associated with fruquintinib.
Expert Opinion: Fruquintinib is a valuable additional treatment option for patients with refractory mCRC. The pivotal role of vigilant toxicity management cannot be understated. While fruquintinib offers a convenient and overall, well-tolerated treatment option, ongoing research is essential to determine its efficacy in different patient subsets, evaluate it in combination with chemotherapy and immunotherapy, and determine its role in earlier lines of therapy.

Keywords: Colon cancer; fruquintinib; metastatic cancer; rectal cancer; targeted therapy; vascular endothelial growth factor

0 (Benzofurans)
0 (Antineoplastic Agents)
0 (Protein Kinase Inhibitors)
49DXG3M5ZW (HMPL-013)
0 (Quinazolines)
EC 2.7.10.1 (Receptors, Vascular Endothelial Growth Factor)

Date Created: 20240318 Date Completed: 20240425 Latest Revision: 20240503

20240504

10.1080/17425255.2024.2332364

38497279