LY2157299, a specific and potent TGF-β receptor (TβR) inhibitor that competitively binds to the active site of its kinase domain¹, inhibiting TGF-β-mediated SMAD2 phosphorylation/activation and down streaming signaling.

LY2157299 inhibited hematopoetic suppression in primary hematopoietic stem cells, such that it improved anemia in a TGF-β overexpressing transgenic mouse model, and stimulated hematopoiesis from primary MDS bone marrow specimens². Daily oral administration of LY2157299 in patients with advanced/metastatic cancer was tolerated well with an expected pharmacokinetic profile^3,4.