BioCentury
ARTICLE | Distillery Therapeutics

Cancer

November 30, 2016 2:13 PM UTC

Mouse studies suggest dual inhibition of MAP2K1/MAP2K2 or MAPK1/MAPK3 could help treat PTEN hamartoma tumor syndrome (PHTS), a type of skin hyperplasia that can become malignant. In a mouse model of PHTS, dual knockout of MAP2K1/MAP2K2 or MAPK1/MAPK3 in skin cells decreased skin thickness and expression of proliferation markers in the skin compared with normal expression of all four genes. Also in the model, a MAPK1/MAPK3 inhibitor tool compound decreased skin thickness, lesion size, and the expression of proliferation markers in the skin compared with vehicle. Next steps include identifying and testing small molecule inhibitors of MAPK activity in PTEN-deficient skin cancer.

Array BioPharma Inc. and Laboratoires Pierre Fabre S.A. have binimetinib (MEK162), a small molecule selective inhibitor of MAP2K1 and MAP2K2, in registration to treat melanoma, Phase III testing to treat ovarian and colorectal cancers, Phase II testing to treat cardiomyopathy and solid tumors, and Phase I/II testing to treat gastrointestinal and biliary cancers. ...