Difference between revisions of "Regorafenib (Stivarga)"
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==Diseases for which it is used== | ==Diseases for which it is used== | ||
*[[Cholangiocarcinoma]] | *[[Cholangiocarcinoma]] | ||
| − | *[[ | + | *[[Colorectal cancer]] |
| + | *[[Gallbladder cancer]] | ||
*[[Gastric cancer]] | *[[Gastric cancer]] | ||
*[[Gastrointestinal stromal tumor]] | *[[Gastrointestinal stromal tumor]] | ||
| Line 24: | Line 25: | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| + | |||
| + | ===[[Colorectal cancer]]=== | ||
*9/27/2012: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm321378.htm Approved] for patients with metastatic [[colorectal cancer]] (mCRC) who have been previously treated with [[Regimen_classes#Fluoropyrimidine-based_regimen|fluoropyrimidine-]], [[Regimen_classes#Oxaliplatin-based_regimen|oxaliplatin-]], and [[Regimen_classes#Irinotecan-based_regimen|irinotecan-based]] chemotherapy, an [[Regimen_classes#VEGFR_inhibitor_therapy|anti-VEGF therapy]], and, if KRAS wild type, an [[Regimen_classes#EGFR_TKI_therapy|anti-EGFR therapy]]. ''(Based on CORRECT)'' | *9/27/2012: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm321378.htm Approved] for patients with metastatic [[colorectal cancer]] (mCRC) who have been previously treated with [[Regimen_classes#Fluoropyrimidine-based_regimen|fluoropyrimidine-]], [[Regimen_classes#Oxaliplatin-based_regimen|oxaliplatin-]], and [[Regimen_classes#Irinotecan-based_regimen|irinotecan-based]] chemotherapy, an [[Regimen_classes#VEGFR_inhibitor_therapy|anti-VEGF therapy]], and, if KRAS wild type, an [[Regimen_classes#EGFR_TKI_therapy|anti-EGFR therapy]]. ''(Based on CORRECT)'' | ||
| + | |||
| + | ===[[Gastrointestinal stromal tumor]]=== | ||
*2/25/2013: [http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm340958.htm Approved] for patients with advanced [[Gastrointestinal stromal tumor|gastrointestinal stromal tumors (GIST)]] that cannot be surgically removed and no longer respond to other FDA-approved treatments for this disease. ''(Based on GRID)'' | *2/25/2013: [http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm340958.htm Approved] for patients with advanced [[Gastrointestinal stromal tumor|gastrointestinal stromal tumors (GIST)]] that cannot be surgically removed and no longer respond to other FDA-approved treatments for this disease. ''(Based on GRID)'' | ||
| + | |||
| + | ===[[Hepatocellular carcinoma]]=== | ||
*4/27/2017: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm555548.htm Approved] for the treatment of patients with [[Hepatocellular carcinoma|hepatocellular carcinoma (HCC)]] who have been previously treated with [[Sorafenib (Nexavar)|sorafenib]]. ''(Based on RESORCE)'' | *4/27/2017: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm555548.htm Approved] for the treatment of patients with [[Hepatocellular carcinoma|hepatocellular carcinoma (HCC)]] who have been previously treated with [[Sorafenib (Nexavar)|sorafenib]]. ''(Based on RESORCE)'' | ||
| Line 50: | Line 57: | ||
[[Category:Cholangiocarcinoma medications]] | [[Category:Cholangiocarcinoma medications]] | ||
| − | [[Category: | + | [[Category:Colorectal cancer medications]] |
| + | [[Category:Gallbladder cancer medications]] | ||
[[Category:Gastric cancer medications]] | [[Category:Gastric cancer medications]] | ||
[[Category:Gastrointestinal stromal tumor medications]] | [[Category:Gastrointestinal stromal tumor medications]] | ||
Revision as of 13:45, 1 May 2022
General information
Class/mechanism: Small molecule inhibitor of multiple tyrosine kinases, such as: VEGFR1, VEGFR2, VEGFR3, KIT, RET, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, Trk2A, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Abl, which are involved in tumor cell proliferation, survival, and angiogenesis. Its major active metabolites are M-2 and M-5.[1][2][3]
Route: PO
Extravasation: n/a
Black Box Warning: Severe and sometimes fatal hepatotoxicity has been observed in clinical trials. Monitor hepatic function prior to and during treatment. Interrupt and then reduce or discontinue regorafenib for hepatotoxicity as manifested by elevated liver function tests (LFTs) or hepatocellular necrosis, depending upon severity and persistence.
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the package insert.[1]
Diseases for which it is used
- Cholangiocarcinoma
- Colorectal cancer
- Gallbladder cancer
- Gastric cancer
- Gastrointestinal stromal tumor
- Hepatocellular carcinoma
- Leiomyosarcoma
- Osteosarcoma
- Renal cell carcinoma
- Soft tissue sarcoma
Patient drug information
- Regorafenib (Stivarga) package insert[1]
- Regorafenib (Stivarga) patient drug information (Chemocare)[4]
- Regorafenib (Stivarga) patient drug information (UpToDate)[5]
History of changes in FDA indication
Colorectal cancer
- 9/27/2012: Approved for patients with metastatic colorectal cancer (mCRC) who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy. (Based on CORRECT)
Gastrointestinal stromal tumor
- 2/25/2013: Approved for patients with advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed and no longer respond to other FDA-approved treatments for this disease. (Based on GRID)
Hepatocellular carcinoma
- 4/27/2017: Approved for the treatment of patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib. (Based on RESORCE)
History of changes in EMA indication
- 8/26/2013: Initial marketing authorization as Stivarga.
Also known as
- Code name: BAY 73-4506
- Brand names: Nublexa, Regonix, Renib, Resihance, Stivarga
References
Categories:
- Drugs
- Oral medications
- BRAF inhibitors
- FGFR inhibitors
- KIT inhibitors
- PDGFR inhibitors
- RET inhibitors
- TEK inhibitors
- VEGFR inhibitors
- Cholangiocarcinoma medications
- Colorectal cancer medications
- Gallbladder cancer medications
- Gastric cancer medications
- Gastrointestinal stromal tumor medications
- Hepatocellular carcinoma medications
- Leiomyosarcoma medications
- Osteosarcoma medications
- Renal cell carcinoma medications
- Soft tissue sarcoma medications
- EMA approved in 2013
- FDA approved in 2012