Infigratinib (BGJ398): An investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma.

Infigratinib (BGJ398): An investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma. Expert Opin Investig Drugs. 2020 Dec 12;: Authors: Botrus G, Raman P, Oliver T, Bekaii-Saab T Abstract INTRODUCTION: The fibroblast growth factor receptor (FGFR) pathway is essential in cell proliferation, differentiation, migration and survival. Cancers such as intrahepatic cholangiocarcinoma (IHCA) have demonstrated alterations of FGFR allowing unregulated growth and spread. Infigratinib (BGJ398) is a potent ATP-competitive inhibitor of all four FGFR receptors as demonstrated by the consistent high prevalence of hyperphosphatemia, indicating disruption of FGFR-related phosphate homeostasis. AREAS COVERED: In this article, the authors discuss preclinical studies and the biological characterization of BGJ398 that inspired its investigation for cancer treatment. They summarize the results from phase I and II studies and comment on ongoing phase III clinical trials primarily focusing on its role in treating IHCA. EXPERT OPINION: Infigratinib was established to exhibit high potency FGFR1-3 inhibition in preclinical studies. FGFR alterations and more specifically FGFR2 fusions have been established as main drivers in intrahepatic cholangiocarcinoma (IHCA). Clinically, a group of agents targeting FGFR including infigratinib have been found to show promising anti-tumor activity in various targeted trials. Addit...
Source: Expert Opinion on Investigational Drugs - Category: Drugs & Pharmacology Tags: Expert Opin Investig Drugs Source Type: research