An updated patent review of VEGFR-2 inhibitors (2017-present)

ABSTRACT

Introduction: Angiogenesis is a vital process for cellular functions in both physiological and pathophysiological conditions and is one of the hallmarks of cancer progression and metastasis. VEGF/VEGFR-2 signaling pathway has been recognized as the most critical factor in promoting angiogenesis. Hence, several VEGFR-2 inhibitors have been clinically tested and/or approved for the treatment of angiogenesis-related diseases.

Areas covered: This review covered reports in the patent literature in the period 2017 to the end of 2020 on the small-molecule inhibitors and antibodies of VEGFR-2 and their potential use as therapeutics for several types of cancers, angiogenesis-related disorders, and Parkinson’s and Alzheimer’s diseases.

Expert opinion: VEGF inhibition has attracted considerable attention as a potential approach for antiangiogenic therapy during the last two decades. However, the effectiveness of this approach may be limited by several issues such as weak response, resistance development, and serious adverse effects. Therefore, the combination of anti-angiogenic therapy with chemotherapy and/or immunotherapy, together with the proper utilization of nanomedicine-based approaches, may have a synergistic effect on improving the efficiency of therapy, reducing side effects and lowering the cost.

KEYWORDS:

• Patent
• angiogenesis
• VEGFR-2
• inhibitors
• anticancer

Article highlights

• Angiogenesis is a vital process for cellular functions in both physiological and pathophysiological conditions and is one of the hallmarks of cancer progression and metastasis.

• VEGF/VEGFR-2 signaling pathway has been recognized as the most critical factor in promoting angiogenesis.

• Several VEGFR-2 inhibitors have been clinically tested and/or approved for the treatment of angiogenesis-related diseases.

• This review covered patent reports in the period from 2017 to the end of 2020 in the field of VEGFR-2 inhibitors and their potential use as therapeutics for angiogenesis-related disorders, particularly cancer.

• Small-molecule VEGFR-2 inhibitors disclosed in the covered patents were classified depending on their chemical structures.

• Patents related to anti- VEGFR-2 antibodies were also examined.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers in this manuscript have no relevant financial or other relationships to disclose.