BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: Estrogen-related receptor α (ERR-α; ESRRA; NR3B1); epidermal growth factor receptor 2 (HER2; ErbB2; neu)

August 11, 2016 7:00 AM UTC

Cell culture and mouse studies suggest combining ERR-α inhibition with the HER1 and HER2 inhibitor Tykerb lapatinib could help treat HER2-positive breast cancer. In a HER2-overexpressing, Tykerb-resistant human breast cancer cell line, Tykerb plus an ERR-α inhibitor tool compound decreased growth and migration compared with Tykerb alone. Also in the cell line, the ERR-α inhibitor increased sensitivity to Tykerb compared with no treatment. In a mouse model of HER2-positive, Tykerb-sensitive breast cancer, Tykerb plus the ERR-α inhibitor decreased tumor growth and recurrence compared with either agent alone. In a mouse model of HER2-positive, Tykerb-resistant breast cancer, Tykerb plus the ERR-α inhibitor decreased tumor growth compared with Tykerb alone. Next steps could include identifying and testing additional ERR-α inhibitors in combination with Tykerb...