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Updated: Aug 12, 2025
Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
Published on: October 10, 2020
An updated patent review of glutaminase inhibitors (2019-2022)
Danni Wang1, Xiaohong Li1, Guangyue Gong1
1State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, China.
Introduction:
Kidney-type glutaminase (GLS1), a key enzyme controlling the hydrolysis of glutamine to glutamate to resolve the 'glutamine addiction' of cancer cells, has been shown to play a central role in supporting cancer growth and proliferation. Therefore, the inhibition of GLS1 as a novel cancer treating strategy is of great interest.
Areas Covered:
This review covers recent patents (2019-present) involving GLS1 inhibitors, which are mostly focused on their chemical structures, molecular mechanisms of action, pharmacokinetic properties, and potential clinical applications.
Expert Opinion:
Currently, despite significant efforts, the search for potent GLS1 inhibitors has not resulted in the development of compounds for therapeutic applications. Most recent patents and literature focus on GLS1 inhibitors IPN60090 and DRP104, which have entered clinical trials. While other patent disclosures during this period have not generated any drug candidates, the clinical update will inform the potential of these inhibitors as promising therapeutic agents either as single or as combination interventions.
Insights
Glutaminase inhibitors targeting cancer's glutamine addiction show promise. Recent patents focus on IPN60090 and DRP104, now in clinical trials, offering potential new cancer therapies.
Area of Science:
- Biochemistry
- Oncology
- Medicinal Chemistry
Background:
- Kidney-type glutaminase (GLS1) is crucial for cancer cell proliferation by metabolizing glutamine.
- Targeting GLS1 is a promising strategy to combat cancer's 'glutamine addiction'.
Approach:
- This review analyzes patents from 2019 to the present concerning GLS1 inhibitors.
- Focus is placed on chemical structures, mechanisms of action, pharmacokinetics, and clinical potential.
Key Points:
- Despite extensive research, no GLS1 inhibitors have reached therapeutic application yet.
- IPN60090 and DRP104 are highlighted as leading GLS1 inhibitors currently in clinical trials.
- Other patented compounds have not yet yielded drug candidates.
Conclusions:
- Ongoing clinical trials for IPN60090 and DRP104 will determine their therapeutic viability.
- These inhibitors may serve as effective single agents or in combination therapies for cancer treatment.
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