An overview of targeted drug delivery systems specific for fibroblast growth factor receptors and their co-receptors

The growing number of patients diagnosed with cancer highlights the need for development of new therapeutic strategies. Targeted therapies, especially DDSs, have attracted increasing interest in recent years, mostly because of selective delivery of cytotoxic agents to cancer cells and overcoming some cancer resistance mechanisms.

FGFRs and their co-receptors, especially HSPGs, represent attractive molecular targets for DDSs due to their dysregulation across multiple cancer types. To date, nearly 60 DDSs targeting FGFRs and/or HSPGs have been reported in the literature, spanning a wide range of cytotoxic efficacy and developmental stages. Several of these candidates have entered Phase I of clinical trials, but none has yet received FDA approval. In this review, we provide a comprehensive overview of DDSs targeting FGFRs and HSPGs in cancer. Literature was identified through PubMed up to March 2026, with selection focused on studies related to targeted drug delivery systems specific for fibroblast growth factor receptors and their co-receptors.

FGFR/HSPG-targeted DDSs show potential mainly within targeted therapies, but clinical translation is limited by target expression in normal tissues and insufficient efficacy of current ADCs. Future progress depends on better target validation, co-expression analysis, and development of multivalent or PDC-based strategies integrated with molecular patient stratification.