GLPG-0187

GLPG-0187 is a small molecule, broad-spectrum integrin receptor antagonist with potential antineoplastic activity. It binds to and blocks the activity of several RGD-integrin receptor subtypes, including αvβ1, αvβ3, αvβ5, αvβ6, and α5β1. By inhibiting these integrins—which are transmembrane glycoproteins involved in cell adhesion and migration—GLPG‑0187 disrupts endothelial cell-cell and cell-matrix interactions. This leads to inhibition of angiogenesis and metastasis in tumor cells expressing these receptors. Additionally, by blocking integrin-mediated activation of TGF‑β (transforming growth factor beta), it may reduce immune evasion by cancer cells through suppression of SMAD/TGF‑β signaling pathways. The drug has been investigated primarily for the treatment of solid tumors; phase I clinical trials have been completed but did not show monotherapy efficacy[1][3][4][5][6].

Other names

1320346-97-1UNII-43A5P87Z4TUNII43A5P87Z4TUNII 43A5P87Z4T43A5P87Z4T