carotegrast methyl

Carotegrast methyl (AJG501, AJM300) is an orally active, small-molecule antagonist of α4 integrin, specifically targeting the α4β1 and α4β7 integrin heterodimers. Developed by EA Pharma (a joint venture between Ajinomoto and Eisai) and Kissei Pharmaceutical, it is the first oral integrin antagonist approved for the treatment of ulcerative colitis. The drug functions by blocking the interaction between α4 integrins on the surface of inflammatory cells and their ligands, such as vascular cell adhesion molecule-1 (VCAM-1) and mucosal addressin cell adhesion molecule-1 (MAdCAM-1), thereby inhibiting the infiltration of lymphocytes into the inflamed intestinal tissue. While approved in Japan under the brand name Carogra for the induction of remission in moderate ulcerative colitis, the code AJG501 has been specifically utilized in Phase II/III clinical trials evaluating its efficacy and safety for the maintenance of remission in patients who have previously responded to induction therapy.

Brand names

Carogra

Other names

carotegrast