Drug intelligence / Profile preview

erlotinib + silybin-phytosome

Development stage
Unknown
Lead developer
Kosin University Gospel Hospital
Modality
Small Molecules
Administration
Oral
01

Overview

Erlotinib + silybin-phytosome is a combination therapy investigated in studies for enhanced antitumor effect and to overcome resistance in certain cancers, primarily in EGFR-mutant non-small cell lung cancer. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that inhibits cancer cell proliferation by blocking EGFR signaling. Silybin-phytosome (also known as Siliphos, a complex of silybin and phosphatidylcholine) is derived from the flavonolignan silybin (silibinin), the most active component of milk thistle extract, and exhibits antitumor, antioxidant, and chemosensitizing effects, including downregulation of EGFR expression and modulation of glucose metabolism and efflux transporters. The rationale for this combination is to address acquired resistance to EGFR-TKIs, particularly that associated with the T790M mutation, through the addition of silybin, which has demonstrated the ability to overcome resistance and synergistically reduce tumor growth in preclinical studies. A phase II trial assessed the efficacy of this combination in patients with EGFR-mutant lung adenocarcinoma, though no published results are available[1][2][3][4].

Brand names
Tarceva (erlotinib)Siliphos (silybin-phytosome)
Other names
erlotinib + silybin-phosphatidylcholine complex
02

Targets

CDK2 (Cyclin-dependent kinase 2)EGFR (Epidermal growth factor receptor)CDK4 (Cyclin-dependent kinase 4)

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