gfh018

GFH018 is an oral, highly potent and selective small molecule inhibitor of transforming growth factor beta receptor type 1 (TGF-βRI or TGFBR1). It acts as an ATP-competitive antagonist, blocking the TGF-β signaling pathway. This pathway is implicated in tumor progression, metastasis, and immune evasion by suppressing anti-tumor immune responses. By inhibiting TGFBR1 kinase activity, GFH018 downregulates the pro-tumorigenic effects of TGF-β signaling. Preclinical studies have shown that GFH018 inhibits tumor growth both as monotherapy and in combination with anti-PD-1 antibodies. Clinical trials have demonstrated its safety profile and preliminary efficacy in patients with advanced solid tumors who have failed standard treatments. The drug is being developed primarily for various advanced solid tumors including non-small cell lung cancer and hepatocellular carcinoma[1][3][5][6][10].

Other names

TGFBR1 inhibitor (contextual, not a formal synonym)