A patent review of VEGFR-2 inhibitors: an update (2022 - present)

Area of Science:

• Oncology
• Molecular Biology
• Pharmacology

Background:

• Angiogenesis, the formation of new blood vessels, fuels tumor growth, invasion, and metastasis.
• Vascular Endothelial Growth Factor (VEGF) and its receptors (VEGFRs) are critical regulators of angiogenesis and are often overexpressed in cancers.
• Inhibiting angiogenesis is a key strategy in cancer therapy.

Purpose of the Study:

• To review Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) inhibitors patented since 2022.
• To discuss their potential application in managing angiogenesis-related disorders, particularly cancer.
• To explore challenges and future directions in anti-angiogenic therapy.

Main Methods:

• Literature review of VEGFR-2 inhibitors patented since 2022.
• Analysis of small-molecule inhibitor properties, including selectivity and pharmacokinetics.
• Discussion of treatment resistance mechanisms and combination therapy strategies.

Main Results:

• Small-molecule VEGFR-2 inhibitors often lack selectivity, leading to side effects due to off-target kinase inhibition.
• Factors like poor pharmacokinetics, high costs, and treatment resistance limit current therapies.
• Tumor- and non-tumor-derived factors contribute to resistance.

Conclusions:

• Targeted inhibition of VEGFR-2 is a promising anti-cancer strategy.
• Improving selectivity and overcoming resistance are crucial for effective VEGFR-2 inhibitor therapy.
• Combination therapies involving novel VEGFR-2 inhibitors, chemotherapy, immunotherapy, or gene therapy may enhance treatment efficacy and safety.