IA-Trimer

IA-Trimer is a multivalent non-peptide antagonist of integrin alpha-V/beta-3 (αvβ3), a cell surface receptor that is significantly upregulated on angiogenic endothelial cells and various tumor types. The molecule is a trimeric construct of the small molecule antagonist 4-[2-(3,4,5,6-tetrahydropyrimidine-2-ylamino)ethyloxy]benzoyl-2-(S)-aminoethylsulfonyl-amino-beta-alanine. Developed by researchers at the Methodist Hospital Research Institute and Weill Medical College of Cornell University, IA-Trimer utilizes a multivalency strategy to enhance binding affinity and therapeutic potency. In preclinical studies using B16F10 melanoma mouse models, IA-Trimer demonstrated superior anti-tumor efficacy and lower toxicity compared to its monomeric (IA-Monomer) and dimeric (IA-Dimer) counterparts, effectively slowing tumor growth when administered via intraperitoneal injection.

Other names

multivalent IA trimerintegrin alphaVbeta3 antagonist trimer