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Updated: May 8, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Cyclin Dependent Kinase 2 (CDK2) Inhibitors in Oncology Clinical Trials: A Review
Isabelle House1, Mari Valore-Caplan1, Elijah Maris1
1Sarah Cannon Research Institute at HealthONE, Denver, CO, USA.
Abstract:
Cyclin dependent kinase 2 (CDK2) is responsible for enforcing progression through the G1-S phase transition. Mutations and alterations in the CDK2 signaling pathway are associated with various cancers, most commonly breast, ovarian, prostate, leukemia, and lymphoma. CDK2 inhibitors have shown promising preclinical and early clinical results, and this class of agents may be most effective against cancers with cyclin E overactivity. Common side effects observed include nausea, vomiting, diarrhea, anemia, and fatigue. This clinical review summarizes past and current CDK2 inhibitors in clinical trials.
Insights
Cyclin dependent kinase 2 (CDK2) inhibitors show promise for treating cancers driven by cell cycle dysregulation. This review covers CDK2 inhibitors in clinical trials, highlighting their potential and observed side effects.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Cyclin dependent kinase 2 (CDK2) regulates the critical G1-S phase transition in the cell cycle.
- Aberrations in CDK2 signaling are implicated in the pathogenesis of numerous cancers, including breast, ovarian, prostate, leukemia, and lymphoma.
- Targeting CDK2 represents a potential therapeutic strategy for cancer treatment.
Purpose of the Study:
- To review the current landscape of CDK2 inhibitors in clinical development.
- To summarize the efficacy and safety profiles of these agents.
- To identify patient populations most likely to benefit from CDK2 inhibition.
Main Methods:
- Literature search of preclinical and clinical studies on CDK2 inhibitors.
- Analysis of data from ongoing and completed clinical trials.
- Review of molecular mechanisms and clinical outcomes.
Main Results:
- CDK2 inhibitors have demonstrated promising preclinical and early clinical activity.
- The efficacy of CDK2 inhibitors may be most pronounced in cancers with overactive cyclin E.
- Commonly observed side effects include nausea, vomiting, diarrhea, anemia, and fatigue.
Conclusions:
- CDK2 inhibitors are a developing class of targeted cancer therapies.
- Further clinical investigation is warranted to optimize their use in specific cancer types.
- Understanding the role of cyclin E overactivity can guide patient selection for CDK2 inhibitor therapy.
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