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Updated: Jun 13, 2025

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Published on: December 7, 2014
MEK inhibitors in oncology: a patent review and update (2016 - present)
Anjali Suryavanshi1, Vandana1, Yugal Kishor Shukla1
1Department of Pharmacy, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, India.
Introduction:
Mitogen-activated protein kinase (MEK) is one of the important components of Ras/Raf/MEK/ERK signaling pathway, transduces signal for cell growth, differentiation, and development. Deregulation of MEK leads to a wide variety of cancer; hence, MEK is considered as potential therapeutic targets for the treatment of cancer. The MEK1/2 inhibitors in combination with other inhibitors showed better therapeutic outcomes in various malignancies including resistant or relapsed or refractory cancer.
Areas Covered:
A comprehensive patent literature from the year 2016 to May 2024 on MEK inhibitors in oncology, their combination products and structural insights have been reviewed through searching relevant information in PubMed, Scopus, Espacenet, Web of Science, World Intellectual Property Organization and Google Patent databases.
Expert Opinion:
Overexpression and mutation of MEK have been reported to cause a wide variety of cancers especially resistant cancers. The MEK1/2 inhibitors in combination with other kinase (BRaf/KRas/PI3K) inhibitors showed significant anti-proliferative activity. Other combination of MEK inhibitor with PD-1, DYRK1, EGFR, BTK and/or VEGF inhibitors, etc. showed promising results in many cancers including colorectal, pancreatic, gastrointestinal, solid tumor, breast cancer, melanoma and multiple myeloma, etc. The dual or multi-targeted approaches of these combinations showed better and precise treatment of patients with resistant cancer.
Insights
Mitogen-activated protein kinase (MEK) inhibitors, especially in combination therapies, show significant promise for treating various cancers. These targeted approaches are particularly effective against resistant or relapsed malignancies.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Mitogen-activated protein kinase (MEK) is crucial in the Ras/Raf/MEK/ERK pathway, regulating cell growth and development.
- MEK deregulation is linked to various cancers, making it a key therapeutic target.
- MEK inhibitors are being explored for cancer treatment, particularly in combination strategies.
Purpose of the Study:
- To review patent literature on MEK inhibitors in oncology from 2016 to May 2024.
- To analyze combination products and structural insights of MEK inhibitors.
- To assess the therapeutic potential of MEK inhibitors in various malignancies.
Main Methods:
- Comprehensive patent literature search (2016-2024).
- Databases searched: PubMed, Scopus, Espacenet, Web of Science, WIPO, Google Patents.
- Analysis of MEK inhibitors, combination therapies, and structural data.
Main Results:
- MEK inhibitors combined with other kinase inhibitors (e.g., BRaf, KRas, PI3K) demonstrate significant anti-proliferative activity.
- Combinations with PD-1, EGFR, BTK, and VEGF inhibitors show promise in colorectal, pancreatic, breast cancers, melanoma, and multiple myeloma.
- Dual or multi-targeted approaches offer improved and precise treatment for resistant cancers.
Conclusions:
- MEK inhibitors are vital in developing targeted cancer therapies.
- Combination therapies involving MEK inhibitors show enhanced efficacy in diverse and resistant cancers.
- Future research should focus on optimizing these multi-targeted strategies for better patient outcomes.
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