Regorafenib(CAS: 755037-03-7)

Regorafenib (BAY 73-4506, commercial name Stivarga) is an oral

multi-kinase inhibitor developed by Bayer which targets angiogenic,

stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib

shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2

tyrosine kinase inhibition. It is currently being studied as a potential treatment

option in multiple tumor types.

Approvals and indications

Metastatic colorectal cancer

Regorafenib demonstrated to increase the overall survival of patients with

metastatic colorectal cancer and has been approved by the US FDA on September 27, 2012.

Advanced gastrointestinal stromal tumours

On February 25, 2013 the US FDA expanded the approved use to treat patients

with advanced gastrointestinal stromal tumors that cannot be surgically removed

and no longer respond to other FDA-approved treatments for this disease. In a

clinical study with 199 patients regorafenib treated patients had a delay in tumor

growth (progression-free survival) that was, on average, 3.9 months longer than

patients who were given placebo.