Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy

A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors

“…With the 3-week-on/1-week-off regimen, fruquintinib was nearly eliminated after a 7-day break, and the PK parameters on day 29 were very close to those observed on day 1. During the 1-week drug break, fruquintinib concentrations in plasma remained above the EC 80 for 3 days and EC 50 for 5 days, which was important for antitumor efficacy [13]. The data indicated that inhibition of the target was maintained (Fig.…”

“…In cellular assays, Fruquintinib potently inhibited VEGF-stimulated VEGFR phosphorylation and proliferation in human umbilical vein endothelial cells. Fruquintinib demonstrated potent antiangiogenic effect and anti-tumor activity in xenograft models of colon adenocarcinoma (HT-29), non-small cell lung cancer (NSCLC; NCI-H460), renal clear cell carcinoma (Caki-1), and gastric carcinoma (BGC823) in mice treated for 3 weeks [13].…”

Safety and efficacy of fruquintinib in patients with previously treated metastatic colorectal cancer: a phase Ib study and a randomized double-blind phase II study

“…Fruquintinib is a potent and highly selective small molecule inhibitor of VEGFR-1, VEGFR-2, and VEGFR-3 tyrosine and has shown strong anti-tumor activity in various preclinical models [11, 12]. In phase I trials, fruquintinib demonstrated good pharmacokinetic properties, tolerable safety, and promising anti-tumor activity against multiple tumor types [13].…”

Preparation and Application of Modified VEGFR-2 Cell Membrane Chromatographic Separation System

“…Many known EGFR agonists including sunitinib, cetuximab, gefitinib and the others are selective for VEGFR. Therefore, they are often used as positive controls [7]. Ten new compounds of anthranilic diamides which are small molecule VEGFR-2 inhibitors in this study were synthesized by computer aided design and different cheminformatics approaches like target identification, active site prediction.…”