galunisertib

Overview

Galunisertib (LY2157299) is an oral small-molecule inhibitor of TGF-β receptor I (TGFBR1/ALK5). It blocks TGF-β signaling, which drives immune exclusion in the HCC “exhausted” immune subclass and contributes to tumor progression. It has been investigated in combination with sorafenib in HCC.

Evidence in the corpus

• Cited in HCC in the context of TGF-β pathway targeting, relevant to the immune-excluded HCC subclass overexpressing TGFβ-regulated genes; combination with sorafenib under evaluation PMID:24798001.

Resistance mechanisms

Cancer types (linked)

• HCC

Sources

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