Фруквинтиниб|HMPL-013

Описание

Fruquintinib is a VEGFR inhibitor (IC₅₀s = 33, 35, and 0.5 nM for VEGFR1, -2, and -3, respectively). It also inhibits RET, FGFR1, and c-Kit (IC₅₀s = 128, 181, and 458 nM, respectively) in a panel of 253 kinases. Fruquintinib inhibits VEGF-A-induced proliferation of human umbilical vein endothelial cells (HUVECs) and VEGF-C-induced proliferation of human lymphatic endothelial cells (HLECs; IC₅₀s = 1.7 and 4.2 nM, respectively). It decreases tube formation by HUVECs by 74 and 94% when used at concentrations of 30 and 300 nM, respectively. Fruquintinib (0.5-20 mg/kg per day for 21 days) reduces tumor growth in BGC-823, HT-29, Caki-1, and NCI H460 mouse xenograft models.

Использование

Fruquintinib (HMPL-013) is a highly selective VEGFR-1/2/3 tyrosine kinase inhibitor. It was approved by the FDA on 8 November 2023 for the treatment of adult patients with metastatic colorectal cancer. and these patients had previously received fluoropyrimidine, oxaliplatin and irinotecan chemotherapy, anti-vascular endothelial growth factor therapy, and anti-epidermal growth factor receptor (EGFR) therapy. Fruquintinib has also been shown to improve cognitive deficits and pathological changes in a mouse model of cerebral amyloid angiopathy (CAA).

Использование

Fruquintinib is a multi-targeted tyrosine kinase inhibitor, a third-line regimen involved in the treatment of advanced non-small cell lung cancer in humans. Fruquintinib is a potent, highly selective and orally active inhibitor of VEGFR1, 2, 3 tyrosine kinases.