AST1306, A Novel Irreversible Inhibitor of the Epidermal Growth Factor Receptor 1 and 2, Exhibits Antitumor Activity Both In Vitro and In Vivo
2011

AST1306: A New Drug for Cancer Treatment

publication 10 minutes Evidence: high

Author Information

Author(s): Xie Hua, Lin Liping, Tong Linjiang, Jiang Yong, Zheng Mingyue, Chen Zhuo, Jiang Xiaoyan, Zhang Xiaowei, Ren Xiaowei, Qu Wenchao, Yang Yang, Wan Hua, Chen Yi, Zuo Jianping, Jiang Hualiang, Geng Meiyu, Ding Jian

Primary Institution: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China

Hypothesis

AST1306 is a novel irreversible inhibitor of EGFR and ErbB2 that can overcome resistance to reversible inhibitors in cancer treatment.

Conclusion

AST1306 effectively inhibits tumor growth in models overexpressing ErbB2 and shows potential as a treatment for cancers resistant to other therapies.

Supporting Evidence

  • AST1306 was found to inhibit the enzymatic activities of both wild-type and mutant forms of EGFR.
  • AST1306 showed more potent effects in ErbB2-overexpressing cancer cell lines compared to EGFR-overexpressing lines.
  • In vivo studies demonstrated significant tumor growth suppression in models with high ErbB2 expression.

Takeaway

AST1306 is a new medicine that helps fight cancer by blocking certain proteins that help tumors grow, especially in patients who don't respond to other treatments.

Methodology

The study involved in vitro assays to test the inhibitory effects of AST1306 on cancer cell lines and in vivo experiments using mouse models.

Potential Biases

Potential bias due to funding from pharmaceutical sources involved in the development of AST1306.

Limitations

The study primarily focused on specific cancer cell lines and mouse models, which may not fully represent human responses.

Statistical Information

P-Value

p<0.05

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.1371/journal.pone.0021487

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