APR002

APR002 is a novel, orally administered small molecule agonist of toll-like receptor 7 (TLR7), developed to act locally in the gastrointestinal tract and liver, thereby minimizing systemic exposure and improving tolerability. It incorporates a liver-targeting moiety to enhance hepatic selectivity via organic-anion-transporting polypeptide (OATP) transporters. The drug is designed to stimulate innate immune responses, particularly interferon-stimulated gene expression, with the goal of achieving functional cure in chronic hepatitis B infection by breaking immune tolerance and promoting antiviral immunity. In preclinical studies, APR002 demonstrated efficacy in combination with entecavir for durable viral suppression in woodchuck models of hepatitis B virus infection. It is also under clinical development for COVID-19 disease as an enterohepatic-restricted TLR7 agonist[1][2][3][4][5].