Avatrombopag (maleate)

Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC₅₀: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A ^[1][2][3]. In Vitro:Avatrombopag (AKR-501) maleate (0.001-1000 nM) promotes the proliferation of Ba/F3 cells expressing TPO receptor in a concentration-dependent manner (EC₅₀: 3.3 nM)^[1].
Avatrombopag (AKR-501) maleate (0.003-3 μM, 15 min) induces the phosphorylation of STAT3, STAT5 and ERK in Ba/F3 cells in a concentration-dependent manner^[1].
Avatrombopag (AKR-501) maleate (0.01-1000 nM) promotes megakaryocyte colony formation from human CB CD34+ cells in a concentration-dependent manner (EC₅₀: 3.3 nM)^[1].
In Vivo:Avatrombopag (AKR-501) maleate (0.3-3 mg/kg, p.o., once per day for 14 d) increases the number of human platelets in non-obese diabetic/severe combined immunodeficiency (NOD/SCID) mice transplanted with human fetal liver (FL) CD34+ cells in dose-dependent manner^[1].