ethaselen

Ethaselen is an orally bioavailable organoselenium small molecule that acts as a selective inhibitor of thioredoxin reductase 1 (TrxR1), an enzyme upregulated in many cancer cell types. By binding to the selenocysteine-cysteine redox pair at the C-terminal active site of TrxR1, ethaselen inhibits its activity, leading to growth inhibition and induction of apoptosis in tumor cells with high TrxR1 expression. This mechanism disrupts redox-dependent cellular pathways, transcription factor regulation, and cell survival processes. Ethaselen has demonstrated antitumor effects in various cancer models—including non-small cell lung cancer, gastric cancer, hematologic neoplasms, and colorectal cancer—and is being investigated for its ability to reverse cisplatin resistance by promoting reactive oxygen species generation and mitochondrial apoptosis pathways. The drug has reached Phase 2 clinical trials for hematologic neoplasms and Phase 1 trials for advanced solid tumors and non-small cell lung cancer[1][3][4][5][7].

Other names

ethaselenEthaselen-1Ethaselen1Ethaselen 1