Drug name: Silibinin + Gefitinib


Related CSCTT Targets

EGFR mutations [ref.1]P00533

Silibinin, Silybin

Cas.no PubChem ID
22888-70-6 31553
Known Target
Structure
...
Introduction
Silibinin, also known as silybin, is the major active constituent of silymarin, a standardized extract of the milk thistle seeds, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin and others. Silibinin itself is mixture of two diastereomers, silybin A and silybin B, in approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins. Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells.

Gefitinib

Cas.no PubChem ID
184475-35-2 123631
Known Target
Epidermal growth factor receptorP00533
Structure
...
Introduction
Gefitinib inhibits the intracellular phosphorylation of numerous tyrosine kinases associated with transmembrane cell surface receptors, including the tyrosine kinases associated with the epidermal growth factor receptor. Gefitinib inhibits EGFR tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is inhibited; and malignant cells are inhibited.

Reference

  • [1] Combined treatment with silibinin and epidermal growth factor receptor tyrosine kinase inhibitors overcomes drug resistance caused by T790M mutation. Rho, J. K., et al. (2010).Mol Cancer Ther. 9(12):3233-43.
    21159609. [ 21159609 ]

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