Definition

An orally available, small molecule antagonist of C-C chemokine receptor type 4 (CCR4) with potential immunomodulatory and antineoplastic activities. Upon oral administration, tivumecirnon inhibits the binding of CCR4 to its signaling molecules, thereby blocking the recruitment of regulatory T cells (Tregs) to the tumor microenvironment (TME). This may abrogate the immunosuppressive effects of Tregs and promote an effective anti-tumor immune response. CCR4, a chemokine receptor normally expressed on circulating and tissue-resident T cells, is highly expressed on circulating Tregs and is associated with poor prognosis in certain cancers.