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Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
Published on: September 19, 2018
Therapeutically targeted anticancer agents: inhibitors of receptor tyrosine kinases
Carlos García-Echeverría1, Doriano Fabbro
1Oncology Research, Novartis Pharma AG, CH-4002 Basel, Switzerland. carlos.garcia-echeverria@pharma.novartis.com
Abstract:
The rationale to target receptor protein tyrosine kinases (RPTKs) as an approach to cancer chemotherapy has continued to become more compelling with time. Preclinical and clinical data strongly support the involvement of specific RPTKs in the formation and progression of a subset of solid and liquid tumors. The advances in our understanding of the oncogenic activation of these receptors have been matched by the identification of new structural classes of kinase inhibitors that exhibit enormous improvements with regard to potency, specificity and efficacy. This article summarizes current knowledge of the most promising RPTK inhibitors in clinical trials or known to be in late stage preclinical development.
Insights
Targeting receptor protein tyrosine kinases (RPTKs) is a promising cancer chemotherapy strategy. New RPTK inhibitors show improved potency and efficacy, with many in clinical trials or late-stage development.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Receptor protein tyrosine kinases (RPTKs) play a crucial role in cancer development and progression.
- Growing evidence links specific RPTKs to various solid and liquid tumors.
- Understanding oncogenic activation of RPTKs is key to developing targeted therapies.
Purpose of the Study:
- To review the current landscape of receptor protein tyrosine kinase (RPTK) inhibitors.
- To highlight promising RPTK inhibitors in clinical trials and late-stage preclinical development.
- To provide an overview of advancements in RPTK-targeted cancer chemotherapy.
Main Methods:
- Literature review of preclinical and clinical data on RPTK inhibitors.
- Summary of current knowledge on RPTK inhibitors in clinical trials.
- Identification of RPTK inhibitors in late-stage preclinical development.
Main Results:
- Preclinical and clinical data confirm the involvement of RPTKs in tumorigenesis.
- New classes of RPTK inhibitors demonstrate significant improvements in potency, specificity, and efficacy.
- Several promising RPTK inhibitors are advancing through clinical trials and preclinical development.
Conclusions:
- Targeting RPTKs represents a compelling strategy for cancer chemotherapy.
- Advancements in kinase inhibitor development offer enhanced therapeutic potential.
- The reviewed RPTK inhibitors show promise for future cancer treatment applications.
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