Recent advances and future directions on small molecule VEGFR inhibitors in oncological conditions

Area of Science:

• Oncology
• Molecular Biology
• Drug Discovery

Background:

• Vascular Endothelial Growth Factor Receptor (VEGFR) inhibitors have emerged as key antiangiogenic therapies in cancer treatment.
• Despite FDA approvals, their clinical application is hindered by complications and limited efficacy.
• Ongoing research focuses on enhancing the translation of VEGFR inhibitors from preclinical to clinical stages.

Purpose of the Study:

• To review the progress of VEGFR inhibitors as cancer therapeutics over the last decade.
• To analyze the structural and molecular properties, and physiological functions of VEGFR.
• To discuss the hurdles restricting the activity and clinical applicability of VEGFR inhibitors and propose strategies to overcome them.

Main Methods:

• Comprehensive literature review of VEGFR inhibitors in cancer therapy.
• Analysis of structural/molecular properties and physiological functions of VEGFR.
• Examination of FDA-approved VEGFR inhibitors and their limitations.
• Discussion of strategies to enhance the efficacy and clinical application of VEGFR inhibitors.

Main Results:

• VEGFR inhibitors represent a growing class of antiangiogenic therapies with significant therapeutic potential.
• Diverse structural assemblages have been designed to harness the antiproliferative potential of VEGFR inhibitors.
• Key hurdles include resistance mechanisms, toxicity, and off-target effects, limiting their activity range.

Conclusions:

• VEGFR inhibitors are crucial in modern oncology, but overcoming their limitations is essential for broader clinical success.
• Strategic design and combination therapies are vital for enhancing the efficacy of VEGFR inhibitors.
• This review provides insights for advancing VEGFR inhibitor-based cancer treatments into further clinical investigations.