Medicinal Chemistry of Fourth-generation Tyrosine Kinase Inhibitors.
2/5 보강
OpenAlex 토픽 ·
Lung Cancer Treatments and Mutations
Fibroblast Growth Factor Research
Melanoma and MAPK Pathways
[UNLABELLED] Introduction / Objectives: Resistance to chemotherapies represents a critical challenge in the treatment of Non-Small Cell Lung Cancer (NSCLC).
APA
Mohamed F. Zayed (2026). Medicinal Chemistry of Fourth-generation Tyrosine Kinase Inhibitors.. Mini reviews in medicinal chemistry. https://doi.org/10.2174/0113895575451047260306044852
MLA
Mohamed F. Zayed. "Medicinal Chemistry of Fourth-generation Tyrosine Kinase Inhibitors.." Mini reviews in medicinal chemistry, 2026.
PMID
41920754 ↗
Abstract 한글 요약
[UNLABELLED] Introduction / Objectives: Resistance to chemotherapies represents a critical challenge in the treatment of Non-Small Cell Lung Cancer (NSCLC). This clinical imperative drove the discovery of Fourth-Generation Tyrosine Kinase Inhibitors (FGTKIs) to defeat such resistance mechanisms. The study comprehensively reviews and critically analyzes the medicinal chemistry of FGTKIs, focusing on their rational design, mechanisms of action, Structure-Activity Relationships (SARs), and therapeutic potential for overcoming resistance mutations in oncology.
[METHODS] A systematic search of major medical databases was conducted to recognize and integrate related literature.
[RESULTS] FGTKIs represent a class of structurally efficient anticancer agents that function through the allosteric inhibition of TKs via reversible interactions. This mechanism confers potent inhibitory activity along with improved pharmacokinetic and pharmacodynamic properties.
[DISCUSSION] They target the mutant-EGFR to overcome the tertiary resistant mutations (Del19/T790M/C797S), which represent a major clinical challenge against other Tyrosine Kinase Inhibitors (TKIs). They have definite molecular designs and pharmacokinetic properties supporting their action.
[CONCLUSION] FGTKIs have altered the therapeutic concept for mutant NSCLC patients and offered unprecedented efficacy and durability compared to earlier-generation inhibitors.
[METHODS] A systematic search of major medical databases was conducted to recognize and integrate related literature.
[RESULTS] FGTKIs represent a class of structurally efficient anticancer agents that function through the allosteric inhibition of TKs via reversible interactions. This mechanism confers potent inhibitory activity along with improved pharmacokinetic and pharmacodynamic properties.
[DISCUSSION] They target the mutant-EGFR to overcome the tertiary resistant mutations (Del19/T790M/C797S), which represent a major clinical challenge against other Tyrosine Kinase Inhibitors (TKIs). They have definite molecular designs and pharmacokinetic properties supporting their action.
[CONCLUSION] FGTKIs have altered the therapeutic concept for mutant NSCLC patients and offered unprecedented efficacy and durability compared to earlier-generation inhibitors.
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