FGFR4 Inhibitor

Liver cancer, most often called hepatocellular carcinoma (HCC), is the second leading cause of cancer death worldwide with over 794,000 people affected. The incidence of HCC is highest in Asia and Africa, where the high endemic prevalence of hepatitis B and hepatitis C strongly predisposes to the development of chronic liver disease and subsequent development of HCC. It occurs predominantly in patients with underlying chronic liver disease and cirrhosis. Tumors progress with local expansion, intrahepatic spread, and distant metastases.
Sorafenib is only approved small molecule drug, and there is no approved 2nd line therapy. Up to 30% of HCC patients have abnormally active FGFR4 pathway, a validated oncogenic driver. Unfortunately, there are no FGFR4 targeted therapies available. Therefore, FGFR4 is an emerging therapeutic target for HCC.
Genosco’s proprietary know-how can generate selective and potent FGFR4 sparing FGFR1-3. Partially selective FGFR inhibitors (ex, AZD4547 & BGJ398) in the clinical stage are predominantly FGFR1-3 selective inhibitors. Current FGFR inhibitors are not suitable for treating FGF19/ FGFR4 mediated cancer. FGFR4 selective inhibitor (ex, Blu9931) has shown efficacy in HCC xenografts. The selective FGFR4 inhibitor is a novel therapeutic strategy for HCC. The diagram below is representing our selective FGFR4 inhibitor in comparison with known FGFR inhibitor.
This program is partnering to collaborate with Yuhan Co to generate lead candidates. It is in lead optimization stage.