Brain tumors pose a significant therapeutic challenge due to their
heterogeneity, invasive properties, and limited availability of treatment options.
Targeted therapies offer a promising approach to address the complexity of brain
tumors by selectively inhibiting molecular pathways critical for tumor growth and
survival. Among these targeted approaches, receptor-ligand based targeting strategies
have emerged as a promising avenue for precision therapy. This chapter provides a
comprehensive overview of receptor-ligand based targeting approaches for brain
tumors, focusing on the molecular interactions between receptors and their cognate
ligands, the expression profiles of key receptors in different tumor subtypes, and the
development of targeted therapeutics. The diverse range of receptors and ligands is
implicated in brain tumor biology. Epidermal growth factor receptor (EGFR), vascular
endothelial growth factor receptor (VEGFR), and human epidermal growth factor
receptor 2 (HER2) are important in the context of this discussion.
Additionally, this chapter examines the challenges associated with delivering targeted
therapeutics permeating the blood-brain barrier (BBB) and explores innovative
strategies to enhance the delivery of drugs to brain tumors. Promising outcomes and
areas for further investigation are highlighted based on a review of preclinical and
clinical studies that have evaluated the efficacy and safety of receptor-ligand-based
targeting approaches. A discussion on the challenges and future directions in this field,
including strategies to overcome resistance mechanisms, enhance treatment specificity,
and advance personalized medicine approaches, is incorporated. Overall, this chapter
offers valuable insights into the current state and future prospects of receptor-ligandbased targeting approaches for brain tumors. This chapter therefore provides a roadmap
for the development of innovative and operational therapies in the fight against this
disease.
Keywords: Brain tumor, Clinical studies, Chemotherapy, Drug repurposing, In-silico interactions, Multi-target approaches, Malignancy, Preclinical studies, Receptor-ligand interaction, Small molecules, Targeted approaches.
