GSK2879552 + tretinoin

GSK2879552 + tretinoin is a combination of a selective small-molecule inhibitor of lysine-specific demethylase 1A (LSD1/KDM1A) and all-trans retinoic acid (ATRA, also known as tretinoin), an agent that induces differentiation in hematopoietic cells. This oral combination has been studied primarily in relapsed or refractory acute myeloid leukemia (AML) and was investigated in early-phase clinical trials for its ability to promote leukemic cell differentiation and cell death. The rationale for the combination is that GSK2879552 impairs maintenance of differentiation block in leukemic cells, thereby enhancing the differentiation- and apoptosis-promoting effects of ATRA[4][1][5]. The combination resulted in increased cell differentiation, upregulation of differentiation markers (e.g., CD11b), and synergistic growth inhibition and cell death in AML models[4][5]. GSK2879552 was developed by GSK and evaluated in combination with ATRA in Phase I clinical studies in AML and high-risk MDS[5][1].

Other names

all-trans retinoic acidATRA