Definition

An orally bioavailable, small molecule Toll-Like Receptor 7 (TLR7) agonist, with potential immunostimulating activity. Upon oral administration, TLR7 agonist APR003 targets, binds to and activates TLR7, thereby stimulating dendritic cells (DCs) and enhancing natural killer cell (NK) cytotoxicity. This activation results in the production of proinflammatory cytokines, including interferon alpha, and enhanced antibody-dependent cellular cytotoxicity (ADCC). TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity. APR003 is localized in the gastrointestinal (GI) tract and liver, which may promote local immune responses and local tumor eradication and prevent systemic adverse effects.