Aptose Biosciences Inc. announced a clinical poster presentation and a preclinical e-poster at the European Hematology Association (EHA) 2024 Hybrid Congress in Madrid, Spain. Tuspetinib (TUS) is being developed as a TUS + venetoclax (VEN) + hypomethylating agent (HMA) triple drug combination (or TUS+VEN+HMA triplet) as frontline therapy for newly diagnosed AML patients. Aptose's poster presentation illustrates the safety and breadth of activity of TUS monotherapy and the TUS+VEN doublet combination in relapsed or refractory (R/R) AML patients from the APTIVATE Phase 1/2 trial and supports the launch of the TUS+ven+HMA (using azacitidine, AZA, as the HMA) triplet frontline therapy in newly diagnosed AML patients.

The study demonstrated that TUS targets known venetoclax (VEN") resistance mechanisms, retaining nanomolar potential against AML cells engineered to express the NRAS-G12D mutation or selected for resistance to VEN, and in combination with VEN, could prevent emergence of resistance to both agents. TUS resistant cells showed sensitivity to VEN such that treatment with both drugs could also interfere with the emergence of TUS resistance.