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Updated: Nov 5, 2025

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Protein kinase inhibitors for the treatment of prostate cancer
Vincent Chau1, Ravi A Madan1, Jeanny B Aragon-Ching2,3
1Genitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA.
Introduction:
Protein kinases have emerged as targetable pathways used in metastatic prostate cancer given their role in prostatic tumor growth, proliferation and metastases. Protein kinase inhibitors are small molecules that target varying pathways including the breakpoint cluster region (BCR)-Abelson tyrosine kinase (ABL), colony stimulating factor-1 receptor (CSF1R), vascular endothelial growth factor (VEGF)/VEGF receptor (VEGFR) and phosphoinositide 3-kinase (PI3K) pathways and have been studied in prostate cancer trials with variable results. In particular, cabozantinib when used in combination trials and ipatasertib, when used with abiraterone in patients who harbor phosphatase and tensin homologue (PTEN) loss, have been promising.
Areas Covered:
This article reviews the key early and late phase clinical trials currently investigating the use of protein kinase inhibitors in prostate cancer.
Expert Opinion:
While multiple kinase inhibitors show promising results in prostate cancer, none have yet garnered Food and Drug Administration (FDA) approval. Studies are ongoing with the best candidate drugs discussed herein. However, multiple drugs have failed primary endpoints in prostate cancer. Therefore, further understanding of the potential mechanisms of resistance, combination and trial design of combination therapy may help pave the way for targeting kinase inhibition in prostate cancer.
Insights
Protein kinase inhibitors show promise for metastatic prostate cancer, but none have FDA approval yet. Further research into resistance mechanisms and combination therapies is crucial for successful kinase inhibition in prostate cancer.
Area of Science:
- Oncology
- Pharmacology
Background:
- Protein kinases are key targets in metastatic prostate cancer due to their role in tumor growth and spread.
- Various protein kinase inhibitors targeting pathways like BCR-ABL, CSF1R, VEGF/VEGFR, and PI3K have been investigated.
- Cabozantinib and ipatasertib show promise in specific prostate cancer patient populations.
Purpose of the Study:
- To review early and late-phase clinical trials of protein kinase inhibitors in prostate cancer.
- To summarize the current landscape of kinase inhibitor research in prostate cancer.
Main Methods:
- Literature review of clinical trials.
- Analysis of ongoing and completed studies involving protein kinase inhibitors for prostate cancer.
Main Results:
- Multiple kinase inhibitors have demonstrated promising results in clinical trials for prostate cancer.
- No protein kinase inhibitors have received FDA approval for prostate cancer treatment to date.
- Several drug candidates have unfortunately failed to meet primary endpoints in clinical trials.
Conclusions:
- Despite promising early results, challenges remain in achieving FDA approval for kinase inhibitors in prostate cancer.
- Understanding resistance mechanisms and optimizing combination therapy trial designs are essential for future success.
- Ongoing studies are evaluating promising drug candidates, with potential for improved outcomes in prostate cancer treatment.
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