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Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
Published on: June 26, 2019
Clinical development of SRC tyrosine kinase inhibitors in lung cancer
1CIG Media Group, LP, Dallas, TX, USA.
Abstract:
Src tyrosine kinases regulate a large number of important mechanisms in normal and cancerous cells, are overexpressed in a broad range of tumors including lung cancer, and thus represent a potential target for cancer therapy. Preclinical experiments indicate that small-molecule inhibitors of Src block tumor growth, metastasis, and angiogenesis. Phase I data from healthy volunteers also suggest that inhibitors of Src prevent bone resorption. Several phase II trials with small-molecule inhibitors of Src are under way or have been initiated in lung cancer and in other malignancies, as discussed herein.
Insights
Src tyrosine kinases are crucial in cancer and are overexpressed in many tumors. Small-molecule inhibitors targeting these kinases show promise in blocking tumor growth and metastasis, with ongoing clinical trials for lung cancer.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Src tyrosine kinases play vital roles in cellular functions.
- These kinases are frequently overexpressed in various cancers, including lung cancer.
- Overexpression suggests Src kinases are potential therapeutic targets.
Purpose of the Study:
- To review the role of Src tyrosine kinases in cancer.
- To discuss the therapeutic potential of small-molecule Src inhibitors.
- To summarize ongoing clinical trials involving Src inhibitors in malignancies.
Main Methods:
- Review of preclinical data on Src inhibitor efficacy.
- Analysis of Phase I clinical trial data in healthy volunteers.
- Summary of ongoing and initiated Phase II clinical trials.
Main Results:
- Preclinical studies demonstrate Src inhibitors can impede tumor growth, metastasis, and angiogenesis.
- Phase I data indicate Src inhibitors may prevent bone resorption.
- Multiple Phase II trials are underway for lung cancer and other cancers.
Conclusions:
- Src tyrosine kinases are significant targets for cancer therapy.
- Small-molecule Src inhibitors exhibit therapeutic potential in preclinical and early clinical settings.
- Further investigation in Phase II trials is warranted for various malignancies.
