ly3200882

LY3200882 is an orally bioavailable, small molecule inhibitor developed by Eli Lilly that selectively targets transforming growth factor-beta receptor type 1 (TGFβR1, also known as ALK5), acting as an ATP-competitive antagonist. By binding to TGFβR1, it blocks the binding and signal transduction of TGFβ ligands (TGFβ1, TGFβ2, and TGFβ3), thereby inhibiting downstream SMAD phosphorylation and associated pro-tumorigenic activities. This mechanism leads to reduced proliferation of cancer cells and modulation of the tumor microenvironment. Preclinical studies have shown antitumor activity in models such as triple-negative breast cancer, with evidence for immune modulation including enhanced tumor-infiltrating lymphocytes and reversal of immune suppression. Clinical trials have evaluated its safety and preliminary efficacy both as monotherapy and in combination with other anticancer agents (e.g., pembrolizumab or chemotherapy) in advanced cancers such as pancreatic cancer.

Other names

1898283-02-7