NCIt definition : An orally available, small molecule antagonist of the tyrosine kinase transforming
growth factor-beta (TGF-b) receptor type 1 (TGFBR1), with potential antineoplastic
activity. Upon administration, galunisertib specifically targets and binds to the
kinase domain of TGFBR1, thereby preventing the activation of TGF-b-mediated signaling
pathways. This may inhibit the proliferation of TGF-b-overexpressing tumor cells.
Dysregulation of the TGF-b signaling pathway is seen in a number of cancers and is
associated with increased cancer cell proliferation, migration, invasion and tumor
progression.;