Experience with Regorafenib in the Treatment of Hepatocellular Carcinoma

Overview

Journal Therap Adv Gastroenterol

Publisher Sage Publications

Specialty Gastroenterology

Date 2021 Jun 9

PMID 34104211

Citations 70

Authors

Alessandro Granito

Antonella Forgione

Sara Marinelli

Matteo Renzulli

Luca Ielasi

Vito Sansone

Francesca Benevento

Fabio Piscaglia

Francesco Tovoli

Affiliations

Soon will be listed here.

Abstract

Regorafenib is a diphenylurea oral multikinase inhibitor, structurally comparable to sorafenib, which targets a variety of kinases implicated in angiogenic and tumor growth-promoting pathways. Regorafenib was the first agent to positively show significant survival advantage as a second-line therapy in patients with unresectable hepatocellular carcinoma (HCC) who had previously failed first-line treatment with sorafenib. Recent evidence has shown that its antitumor efficacy is due to a comprehensive spectrum of tumor neo-angiogenesis and proliferation inhibition and immunomodulatory effects on the tumor microenvironment, which plays a crucial role in tumor development. This review addresses the rationale and supporting evidence for regorafenib's efficacy in HCC that led to regorafenib's approval as a second-line therapy. In addition, we review proof from clinical practice studies that validate the RESORCE trial results. We discuss regorafenib's potential role in the newly emerging therapeutic strategy based on combination with immune checkpoint blockade and its possible extensibility to patient categories not enrolled in the registrative study.

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