摘要Oroxylin A(OA)is a natural flavonoid primarily derived from the plants Oroxylum indicum and Scutellaria baicalensis.Currently,OA is obtainable through chemical synthesis and exhib-its polypharmacological properties,including anti-cancer,anti-inflammatory,anti-microbial,and multi-organ protective effects.The first-in-class drug OA tablets are presently undergo-ing phase Ⅰb/Ⅱa clinical trials for hepatocellular carcinoma(HCC)treatment.Substantial evid-ence suggests that OA demonstrates therapeutic potential against various hepatic and gastrointestinal(GI)disorders,including HCC,hepatic fibrosis,fatty liver disease,hepatitis,liver injury,colitis,and colorectal cancer(CRC).OA exerts its therapeutic effects primarily by modulating several crucial signaling pathways,including those associated with apoptosis,ox-idative stress,inflammation,glucolipid metabolism,and fibrosis activation.The oral pharma-cokinetics of OA is characterized by phase Ⅱ metabolism,hydrolysis,and enterohepatic recyc-ling.This review provides a comprehensive overview of the critical stages involved in the de-velopment of OA tablets,presenting a holistic perspective on the progression of this first-in-class drug from preclinical to clinical phases.It encompasses the synthesis of active pharma-ceutical ingredients,pharmacokinetics,pharmacological efficacy,toxicology,drug delivery,and recent advancements in clinical trials.Importantly,this review examines the potential mechanisms by which OA may influence the gut-liver axis,hypothesizing that these interac-tions may confer health benefits associated with OA that transcend the limitations posed by its poor bioavailability.