galunisertib

Galunisertib is an orally available, small molecule inhibitor of the transforming growth factor-beta receptor type 1 (TGFBR1), also known as TGF-betaRI kinase. It was developed as an antineoplastic agent with potential to inhibit tumor growth by blocking TGF-beta-mediated signaling pathways, which are implicated in cancer cell proliferation, migration, invasion, and immune evasion. Galunisertib specifically binds to the kinase domain of TGFBR1 and downregulates phosphorylation of SMAD2, thereby abrogating activation of the canonical TGF-beta pathway. Preclinical studies demonstrated its activity against various cancers including glioblastoma, breast cancer, colon cancer, lung cancer, hepatocellular carcinoma, pancreatic cancer, rectal cancer and prostate cancer. Clinical development included trials for glioma/glioblastoma and hepatocellular carcinoma among others; however, development was discontinued by Eli Lilly in January 2020.

Brand names

galunisertib

Other names

galunisertib700874-72-2