Related Experiment Video
Updated: Jun 13, 2025
Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
Published on: June 26, 2019
Ephrin receptor type-A2 (EphA2) targeting in cancer: a patent review (2018-present)
Massimiliano Tognolini1, Francesca Romana Ferrari1, Alfonso Zappia1
1Food and Drug Department, University of Parma, Parma, Italy.
Introduction:
EphA2 is a tyrosine kinase receptor and is considered a promising target in cancer. Different approaches are used to target EphA2 receptor, and a lot of preclinical data demonstrate the potential exploitation of this receptor in clinical oncology for diagnosis and cancer therapy, including immunotherapy.
Areas Covered:
In this review, we have summarized the recent patents involving the EphA2 targeting in cancer. For this aim, we used the patent database Patentscope covering the time period of 2018-present. Preclinical and clinical data of the inventions were considered when published on peer reviewed journals. Moreover, the clinicalTrial.gov identifiers (NCT numbers) were included when available. For an easier and more immediate reading, we classify the patents in different categories, considering the nature (aptamers, small molecules, antibodies, peptides, antigens and chimeric antigen receptors) of the inventions exploiting EphA2 in clinical oncology.
Expert Opinion:
Despite the availability of a plethora of chemically diverse agents, there are no approved anticancer drugs targeting EphA2 yet. However, these intellectual properties, some of which supported by strong preclinical evidence, keep the hope that, after more than 30 years from its discovery, we will finally see the first EphA2 targeting agent approved in clinical oncology.
Insights
Researchers reviewed recent patents on targeting the EphA2 receptor for cancer therapy. Despite promising preclinical data, no EphA2-targeting drugs are approved yet, but hope remains for future clinical applications.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- EphA2 is a tyrosine kinase receptor with significant potential in cancer diagnosis and therapy.
- Preclinical data support the exploitation of EphA2 targeting strategies in clinical oncology, including immunotherapy.
Purpose of the Study:
- To summarize recent patents (2018-present) involving EphA2 targeting in cancer.
- To categorize EphA2-targeting inventions based on their nature (aptamers, small molecules, antibodies, peptides, antigens, CARs).
Main Methods:
- Patent database search (Patentscope) from 2018 to present.
- Inclusion of preclinical and clinical data from peer-reviewed publications.
- Inclusion of clinical trial identifiers (NCT numbers) where available.
Main Results:
- A review of recent intellectual properties targeting EphA2 in cancer therapy.
- Classification of patents into categories based on the targeting agent's nature.
Conclusions:
- Despite numerous diverse agents and strong preclinical evidence, no approved anticancer drugs targeting EphA2 currently exist.
- Ongoing patent activity suggests continued hope for the eventual approval of an EphA2-targeting agent for clinical oncology.
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
01:22Role of Ephrin-Eph Signalling in Intestinal Stem Cell Renewal
02:38Mitogens and the Cell Cycle
01:27Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
01:18Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
01:26Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...