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Improving the Armamentarium of PI3K Inhibitors with Isoform-Selective Agents: A New Light in the Darkness
Jordi Rodon1, Josep Tabernero2
1Investigational Cancer Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, Texas. JRodon@mdanderson.org.
Abstract:
Excitement and drug-development efforts aimed at targetable genetic aberrations in the PI3K/AKT/mTOR pathway have declined due to the limited clinical performance of these inhibitors as monotherapies. New, more isoform-selective treatments, such as taselisib, promise to both expand the therapeutic window and increase efficacy. Cancer Discov; 7(7); 666-9. ©2017 AACR.See related article by Juric et al., p. 704.
Insights
Targeting the PI3K/AKT/mTOR pathway with inhibitors has shown limited success. New, selective drugs like taselisib aim to improve treatment efficacy and safety for cancer patients.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Targetable genetic aberrations in the PI3K/AKT/mTOR pathway are crucial in cancer.
- Previous PI3K/AKT/mTOR inhibitors showed limited clinical efficacy as monotherapies.
- This led to decreased interest in drug development for this pathway.
Purpose of the Study:
- To evaluate the potential of new, isoform-selective inhibitors.
- To investigate if taselisib can improve therapeutic window and efficacy.
- To address the limitations of previous monotherapy treatments.
Main Methods:
- Preclinical studies of taselisib.
- Clinical trial data analysis (implied).
- Pharmacological profiling of isoform-selective inhibitors.
Main Results:
- New isoform-selective treatments show promise.
- Taselisib is highlighted as a potential advancement.
- Improved efficacy and therapeutic window are anticipated.
Conclusions:
- Despite past challenges, PI3K/AKT/mTOR pathway inhibitors remain an area of interest.
- Isoform-selective drugs like taselisib offer a renewed therapeutic strategy.
- Further clinical investigation is warranted to confirm efficacy and safety.
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