imatinib + BKM120

imatinib + BKM120 is an investigational combination of two small molecule kinase inhibitors. Imatinib is a tyrosine kinase inhibitor targeting BCR-ABL, KIT, and PDGFR, mainly used in chronic myeloid leukemia and gastrointestinal stromal tumors. BKM120 (also known as buparlisib) is a pan-class I phosphoinositide 3-kinase (PI3K) inhibitor, developed to block PI3K signaling and reduce cancer cell proliferation and survival. The combination was explored to overcome resistance to imatinib and to enhance anti-tumor efficacy, particularly in imatinib-resistant disease, by targeting both upstream tyrosine kinases and downstream PI3K pathways. Clinical evaluation includes phase 1 testing in advanced solid tumors including gastrointestinal stromal tumors (GIST) as third-line therapy[1][2].

Brand names

GleevecGlivec

Other names

imatinib mesylateimatinibum