PMID- 29943375 OWN - NLM STAT- MEDLINE DCOM- 20190516 LR - 20190516 IS - 1179-1950 (Electronic) IS - 0012-6667 (Linking) VI - 78 IP - 11 DP - 2018 Jul TI - Regorafenib: A Review in Metastatic Colorectal Cancer. PG - 1133-1144 LID - 10.1007/s40265-018-0938-y [doi] AB - Regorafenib (Stivarga((R))) is an oral small-molecule multiple kinase inhibitor. It is indicated worldwide for patients with metastatic colorectal cancer (mCRC). In the EU and USA it is indicated for patients with mCRC who have been previously treated with, or are not considered candidates for available therapies, including fluoropyrimidine-based chemotherapy, an anti-VEGF therapy and, if RAS wild-type, an anti-EGFR therapy. In Japan, it is indicated for the treatment of unresectable, advanced/recurrent CRC. The addition of regorafenib to best supportive care prolonged median overall survival (OS; by up to 2.5 months) and progression-free survival (PFS; by up to 1.5 months) relative to the addition of placebo in double-blind phase 3 studies (CORRECT and CONCUR) in patients with mCRC who had progressed after failure of standard therapy. Health-related quality of life was not adversely affected with regorafenib relative to placebo. A large open-label phase 3 study (CONSIGN) and several large real-world studies supported the efficacy of regorafenib in this setting. Regorafenib had a generally manageable tolerability profile, which was consistent with the profile of a typical small-molecule multiple kinase inhibitor. Treatment-related adverse events (AEs), mostly of mild or moderate severity, were reported in the majority of patients receiving regorafenib, with dermatological toxicities and liver enzyme elevations among the most common AEs. Although identification of biomarkers/parameters predicting efficacy outcomes with regorafenib will help to individualize therapy, current evidence indicates that regorafenib is a valuable treatment option for patients with refractory mCRC who have a very poor prognosis. FAU - Dhillon, Sohita AU - Dhillon S AD - Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. demail@springer.com. LA - eng PT - Journal Article PT - Review PL - New Zealand TA - Drugs JT - Drugs JID - 7600076 RN - 0 (Antineoplastic Agents) RN - 0 (Phenylurea Compounds) RN - 0 (Pyridines) RN - 24T2A1DOYB (regorafenib) SB - IM MH - Antineoplastic Agents/administration & dosage/pharmacokinetics/pharmacology/*therapeutic use MH - Clinical Trials, Phase III as Topic MH - Colorectal Neoplasms/*drug therapy/pathology MH - Dose-Response Relationship, Drug MH - Humans MH - Neoplasm Metastasis MH - Phenylurea Compounds/administration & dosage/pharmacokinetics/pharmacology/*therapeutic use MH - Pyridines/administration & dosage/pharmacokinetics/pharmacology/*therapeutic use MH - Quality of Life EDAT- 2018/06/27 06:00 MHDA- 2019/05/17 06:00 CRDT- 2018/06/27 06:00 PHST- 2018/06/27 06:00 [pubmed] PHST- 2019/05/17 06:00 [medline] PHST- 2018/06/27 06:00 [entrez] AID - 10.1007/s40265-018-0938-y [pii] AID - 10.1007/s40265-018-0938-y [doi] PST - ppublish SO - Drugs. 2018 Jul;78(11):1133-1144. doi: 10.1007/s40265-018-0938-y.