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Published on: December 7, 2014
RET kinase inhibitors: a review of recent patents (2012-2015)
Luca Mologni1,2, Carlo Gambacorti-Passerini1,2, Peter Goekjian3,2
1a School of Medicine and Surgery , University of Milano-Bicocca , Monza , Italy.
Introduction:
Tyrosine kinases are involved in the control of several biological processes and have been recognized as hot spots of oncogenic transformation, thus representing a major therapeutic target. Dysregulated activation of RET kinase, either through point mutations or gene fusions, is accountable for a significant fraction of thyroid carcinomas, as well as a minor population of lung cancers. Two drugs are currently available for the treatment of medullary thyroid carcinoma and two additional compounds have been approved for differentiated thyroid carcinoma. Several other molecules are under preclinical and clinical evaluation. Areas covered: This review covers the most recent patent literature (2012-2015) describing compounds with activity against the RET kinase, trying to catch a view of the next generation of potential anti-RET drugs. Expert opinion: RET has been a focus of molecularly targeted efforts for over a decade. However, none of the drugs currently on the clinical stage were specifically developed to hit RET, which was rather an off-target. Besides, only two of four drugs have activity on metastatic medullary carcinoma. Therefore, there is still a need of additional, more potent and more specific RET inhibitors, which will hopefully emerge from the new generation of compounds disclosed in most recent patents.
Insights
New drug patents reveal next-generation RET kinase inhibitors for thyroid and lung cancers. While current therapies target RET off-label, novel compounds show promise for more specific and potent treatments.
Area of Science:
- Oncology
- Molecular Biology
- Medicinal Chemistry
Background:
- Tyrosine kinases, including RET kinase, are critical in cellular processes and are frequent targets in cancer therapy.
- Dysregulated RET kinase activity drives thyroid and lung cancers, necessitating targeted therapeutic strategies.
- Current treatments for RET-driven cancers have limitations, highlighting the need for improved inhibitors.
Purpose of the Study:
- To review recent patent literature (2012-2015) on compounds targeting RET kinase.
- To identify emerging next-generation anti-RET drugs.
- To assess the potential of novel compounds for treating RET-driven malignancies.
Main Methods:
- Literature review of patent filings from 2012-2015.
- Analysis of compounds described in patents for their activity against RET kinase.
- Evaluation of the therapeutic potential of identified compounds.
Main Results:
- The patent literature reveals ongoing development of novel RET kinase inhibitors.
- Several new compounds are under preclinical and clinical investigation.
- These emerging drugs aim for increased potency and specificity compared to existing therapies.
Conclusions:
- Despite existing treatments, there remains a significant need for more effective and specific RET inhibitors.
- The reviewed patents showcase promising next-generation compounds that could address this unmet need.
- Future therapies may benefit from these novel, specifically designed anti-RET agents.
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