What is Regorafenib
Regorafenib is an oral multikinase inhibitor.
It works by inhibiting tyrosine kinases that promote angiogenesis and tumor growth such as vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-alpha, PDGFR-beta, and TIE2 and oncogenic kinases c-KIT, REF, and BRAF.
Regorafenib is indicated for the treatment of metastatic colorectal cancer (mCRC), locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST), and hepatocellular cancer.
Brand Name
Stivarga
Indications
- colorectal cancer
- gastrointestinal stromal tumors (GIST)
- hepatocellular cancer
For the treatment of metastatic colorectal cancer in patients who have previously received fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy; an anti-VEGF therapy; and an anti-EGFR therapy if RAS wild type
Side Effects
- abdominal pain
- abdominal pain
- alopecia
- alopecia
- anemia
- anemia
- anorexia
- anorexia
- asthenia
- asthenia
- bleeding
- bleeding
- diarrhea
- diarrhea
- dysphonia
- elevated hepatic enzymes
- elevated hepatic enzymes
- erythema multiforme
- exfoliative dermatitis
- fatigue
- fatigue
- fever
- fever
- gastrointestinal fistula
- GI bleeding
- GI perforation
- headache
- headache
- heart failure
- hepatic failure
- hepatotoxicity
- hyperamylasemia
- hyperamylasemia
- hyperbilirubinemia
- hyperbilirubinemia
- hypertension
- hypertension
- hypertensive crisis
- hypocalcemia
- hypocalcemia
- hypokalemia
- hypokalemia
- hyponatremia
- hyponatremia
- hypophosphatemia
- hypophosphatemia
- hypothyroidism
- infection
- infection
- leukoencephalopathy
- lymphopenia
- lymphopenia
- maculopapular rash
- muscle cramps
- myocardial infarction
- nausea
- nausea
- nephrotic syndrome
- neutropenia
- neutropenia
- palmar-plantar erythrodysesthesia (hand and foot syndrome)
- palmar-plantar erythrodysesthesia (hand and foot syndrome)
- pancreatitis
- pharyngitis
- prolonged bleeding time
- prolonged bleeding time
- proteinuria
- proteinuria
- pruritus
- rash
- rash
- Stevens-Johnson syndrome
- stomatitis
- stomatitis
- thrombocytopenia
- thrombocytopenia
- toxic epidermal necrolysis
- tremor
- vomiting
- vomiting
- weight loss
- weight loss
Monitoring Parameters
- blood pressure
- LFTs
Contraindications
- acute myocardial infarction
- anticoagulant therapy
- Asian patients
- bleeding
- breast-feeding
- cardiac disease
- contraception requirements
- encephalopathy
- fistula
- geriatric
- GI bleeding
- GI perforation
- hepatic disease
- hepatotoxicity
- hypertension
- impaired wound healing
- infertility
- pregnancy
- reproductive risk
- skin disease
- surgery
Interactions
- Abacavir; Dolutegravir; Lamivudine
- Alpelisib
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Apalutamide
- Atazanavir
- Atazanavir; Cobicistat
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Carbamazepine
- Ceritinib
- Chloramphenicol
- Clarithromycin
- Cobicistat
- Conivaptan
- Darunavir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Delavirdine
- Dolutegravir
- Dolutegravir; Lamivudine
- Dolutegravir; Rilpivirine
- Doravirine; Lamivudine; Tenofovir disoproxil fumarate
- Efavirenz; Emtricitabine; Tenofovir
- Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
- Emtricitabine; Tenofovir disoproxil fumarate
- Enzalutamide
- Fluvastatin
- Fosamprenavir
- Fosphenytoin
- Glecaprevir; Pibrentasvir
- grapefruit juice
- Idelalisib
- Indinavir
- Irinotecan
- Irinotecan Liposomal
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Itraconazole
- Ketoconazole
- Lamivudine; Tenofovir Disoproxil Fumarate
- Letermovir
- Lopinavir; Ritonavir
- Lumacaftor; Ivacaftor
- Lumacaftor; Ivacaftor
- Meloxicam
- Mephobarbital
- Methotrexate
- Mifepristone
- Mitotane
- Nefazodone
- Nelfinavir
- Neomycin
- Ombitasvir; Paritaprevir; Ritonavir
- Ozanimod
- Pazopanib
- Phenobarbital
- Phenytoin
- Posaconazole
- Primidone
- Ribociclib
- Ribociclib; Letrozole
- Rifampin
- Rimegepant
- Ritonavir
- Rosuvastatin
- Saquinavir
- St. John’s Wort, Hypericum perforatum
- Sulfasalazine
- Talazoparib
- Telithromycin
- Tenofovir Alafenamide
- Tenofovir, PMPA
- Tipranavir
- Topotecan
- Tucatinib
- Ubrogepant
- Voriconazole
- Warfarin
