Аннотация
Abstract Background Gambogic acid (GA), a caged xanthone derived primarily from Garcinia hanburyi , has shown broad anticancer activity across multiple preclinical tumour models. This narrative review critically evaluates the molecular mechanisms, pharmacokinetics, multidrug resistance‐modulating effects, delivery strategies and translational barriers relevant to GA development in oncology. Methods PubMed, Scopus and Web of Science were searched for peer‐reviewed studies addressing GA‐related anticancer activity, redox regulation, proteostasis, pharmacokinetics, formulation, combination therapy and clinical translation. Results Available evidence indicates that GA promotes reactive oxygen species accumulation, mitochondrial dysfunction, apoptosis, autophagy modulation and proteostasis disruption while suppressing nuclear factor kappa B, phosphatidylinositol‐3‐kinase/protein kinase B/mammalian target of rapamycin, mitogen‐activated protein kinase, and signal transducer and activator of transcription 3 signalling. GA may also reverse multidrug resistance by inhibiting drug‐efflux transporters and sensitising tumour cells to conventional anticancer agents. However, translation remains limited by poor aqueous solubility, extremely low oral bioavailability, rapid systemic clearance, incomplete human pharmacokinetic characterisation, uncertain tumour‐selective exposure and potential off‐target toxicity. Nanoformulations, prodrugs and carrier‐based systems improve solubility and systemic exposure in preclinical models, but comparative data on biodistribution, long‐term safety, scalability and regulatory feasibility remain insufficient. Conclusion Current evidence therefore supports GA more strongly as an exposure‐optimised, biomarker‐guided chemosensitising adjuvant than as a standalone cytotoxic agent. Future development should prioritise genetic target validation, human pharmacokinetic–pharmacodynamic studies, tumour‐exposure measurements, standardised safety assessment, scalable delivery platforms and biomarker‐guided early‐phase trials.