Receptor tyrosine kinase targeting in glioblastoma: performance, limitations and future approaches
Oana Alexandru1, Cristina Horescu2, Ani-Simona Sevastre3
1Department of Neurology, University of Medicine and Pharmacy of Craiova and Clinical Hospital of Neuropsychiatry Craiova, Craiova, Romania.
Abstract:
From all central nervous system tumors, gliomas are the most common. Nowadays, researchers are looking for more efficient treatments for these tumors, as well as ways for early diagnosis. Receptor tyrosine kinases (RTKs) are major targets for oncology and the development of small-molecule RTK inhibitors has been proven successful in cancer treatment. Mutations or aberrant activation of the RTKs and their intracellular signaling pathways are linked to several malignant diseases, including glioblastoma. The progress in the understanding of malignant glioma evolution has led to RTK targeted therapies with high capacity to improve the therapeutic response while reducing toxicity. In this review, we present the most important RTKs (i.e. EGFR, IGFR, PDGFR and VEGFR) currently used for developing cancer therapeutics together with the potential of RTK-related drugs in glioblastoma treatment. Also, we focus on some therapeutic agents that are currently at different stages of research or even in clinical phases and proved to be suitable as re-purposing candidates for glioblastoma treatment.
Insights
This review explores receptor tyrosine kinases (RTKs) as key targets for glioblastoma treatment. It highlights RTK inhibitors and repurposed drugs for more effective and less toxic cancer therapies.
Area of Science:
- Oncology
- Molecular Biology
- Neuro-oncology
Background:
- Gliomas are the most common central nervous system tumors, necessitating improved treatments and early diagnostic methods.
- Receptor tyrosine kinases (RTKs) are crucial in cancer development, with mutations linked to glioblastoma.
- Targeted therapies inhibiting RTKs offer potential for improved glioblastoma treatment outcomes and reduced toxicity.
Purpose of the Study:
- To review significant RTKs (EGFR, IGFR, PDGFR, VEGFR) targeted in cancer therapeutics.
- To discuss the potential of RTK-targeted drugs in glioblastoma treatment.
- To identify existing therapeutic agents suitable for glioblastoma treatment repurposing.
Main Methods:
- Literature review of current research on RTKs in glioblastoma.
- Analysis of RTK inhibitors and targeted therapies in oncology.
- Evaluation of drug repurposing candidates for glioblastoma.
Main Results:
- Identified EGFR, IGFR, PDGFR, and VEGFR as key RTKs in glioblastoma.
- Summarized the efficacy and toxicity profiles of RTK inhibitors.
- Highlighted several drugs in research or clinical phases as potential glioblastoma repurposing candidates.
Conclusions:
- RTK-targeted therapies represent a promising strategy for glioblastoma treatment.
- Drug repurposing offers a viable avenue for developing novel glioblastoma therapies.
- Continued research into RTKs and targeted agents is essential for advancing glioblastoma care.


