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

INTRODUCTION

A complicated process called angiogenesis creates new blood vessels from existing ones. Oxygen and nutrients from angiogenesis support tumor development, invasion, and metastasis. Many biological agents cause angiogenesis. EGF, FGF, VEGF, transcription factors, cytokines, adhesion molecules, proteinases, and growth factors. VEGF-A, B, C, and D are necessary for angiogenesis. VEGF family members interact with VEGFR-1,-2, and-3. Overexpression of VEGF proteins and receptors occurs during cancer progression. Novel signaling pathways, transcription factors, and mechanisms may help cure cancers by inhibiting angiogenesis.

AREAS COVERED: This review discusses VEGFR-2 inhibitors patented since 2022 and their potential use in the management of angiogenesis-related disorders like cancer.

EXPERT OPINION: Small-molecule VEGFR-2 inhibitors have minimal selectivity and cause fatigue, anorexia, hypertension, hemorrhage, and bleeding due to their affinity for PDGF, EGFR, and RAF, which is conserved in many tyrosine kinases. Poor pharmacokinetics, side effects, and high manufacturing costs may limit biomolecule adoption despite clinical success. Proangiogenic and non-tumor proangiogenic chemicals and myeloid cells produced treatment resistance. Thus, multimodal targeted medications or combination therapy with anti-angiogenic therapies, chemotherapeutic agents, immune checkpoint inhibitors, or gene therapy are needed to block pathological angiogenesis and increase selectivity, safety, diagnosis, and therapy response.