Drug name: Silibinin + Erlotinib


Related CSCTT Targets

EGFR mutations [ref.1, 2]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.

Erlotinib

Cas.no PubChem ID
183321-74-6 176870
Known Target
Epidermal growth factor receptorP00533
Nuclear receptor subfamily 1 group I member 2O75469
Structure
...
Introduction
Erlotinib is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer. Similar to gefitinib, erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. Erlotinib has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders.

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 ]
  • [2] Stem cell-like ALDH(bright) cellular states in EGFR-mutant non-small cell lung cancer: a novel mechanism of acquired resistance to erlotinib targetable with the natural polyphenol silibinin. Corominas-Faja, B., et al. (2013).Cell Cycle. 12(21):3390-404.
    24047698. [ 24047698 ]

Back to top