LY2157299 is a small molecule inhibitor that targets the transforming growth factor-beta (TGF-β) receptor I kinase. It is primarily investigated for its potential in cancer therapy, especially in tumors where the TGF-β signaling pathway contributes to progression, metastasis, and immune evasion. By inhibiting this pathway, LY2157299 can suppress tumor growth and enhance the body’s immune response against cancer cells.

It has been studied in clinical trials for advanced solid tumors, including glioblastoma and hepatocellular carcinoma. Research also suggests it may help reduce fibrosis in certain disease models, expanding its potential use to fibrotic disorders. Due to its ability to modulate the tumor microenvironment, it is being explored in combination with immunotherapies and other targeted agents to improve treatment outcomes.