Regorafenib in the treatment of metastatic colorectal cancer.

What is it about?

It is a review about regorafenib (Stivarga®; Bayer HealthCare Pharmaceuticals Inc.), an orally available multikinase inhibitor, and its use in metastatic colorectal cancer (mCRC) patients who have been pretreated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, anti-VEGF and anti-EGFR therapy if RAS wild-type.

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Why is it important?

Regorafenib is an inhibitor of several key angiogenic and tumorigenic kinases. Its metabolism is essentially based on the hepatic route. Two randomized phase III studies have established its superiority over placebo in chemorefractory CRC pts, one in an international study (CORRECT) and in an Asiatic one (CONCUR). Both have shown an increase of progression-free and overall survival with regorafenib, the overall response rate being low. Regorafenib is available in tablets of 40 mg and is prescribed at the initial dose of 160 mg once daily for 21 days in 28 day cycles, continued until tumor progression or unacceptable toxicity. Severe adverse events (grade ≥3) were observed in half of the patients in both phase III studies and were mostly represented by hand-foot skin reaction, fatigue, diarrhea and hypertension.

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