#最小單位貼紙

Gastrointestinal stromal tumor, Locally advanced, unresectable, or metastatic disease, after treatment with imatinib and sunitinib.
Liver carcinoma, In patients previously treated with sorafenib.
Metastatic colorectal cancer, In patients previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-containing chemotherapy, and anti-VEGF therapy, and if RAS wild type, an anti-EGFR therapy.

Regorafenib is an oral kinase inhibitor acting on various membrane-bound and intracellular kinases involved in cellular functions and processes, including oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment.

Absorption:
Bioavailability, Oral tablet: 69%
Metabolism:
Metabolized by CYP3A4 and UGT1A9
Excretion:
Renal: 19%
Elimination Half Life
Regorafenib: 28 hours

Specific contraindications have not been determined.

Fetal risk cannot be ruled out. (TH)

Infant risk cannot be ruled out.(MDX)

Common:
Cardiovascular: Hypertension, All grades (30% to 59% )
Dermatologic: Acral erythema, All grades (47% to 71% )
Endocrine metabolic: Hypocalcemia (17% to 59% ), Hyponatremia (30% ), Hypophosphatemia (55% to 57% ), Weight loss (14% to 32% )
Gastrointestinal: Decrease in appetite (31% to 47% ), Diarrhea (43% to 47% ), Inflammatory disease of mucous membrane (33% to 40% ), Nausea (20% ), Vomiting (17% )
Hematologic: Anemia (79% ), Lymphocytopenia (30% to 54% ), Thrombocytopenia (13% to 41% )
Hepatic: ALT/SGPT level raised, All grades (39% to 45% ), AST/SGOT level raised, All grades (58% to 65% ), Hyperbilirubinemia (33% to 45% ), Increased serum lipase level (14% to 46% )
Neurologic: Asthenia, Difficulty speaking (30% to 39% )
Renal: Proteinuria (33% to 60% )
Other: Fatigue, Fever (21% to 28% ), Infectious disease (31% to 32% ), Pain (29% )
Serious:
Cardiovascular: Hypertension, Grade 3 or 4 (8% to 28% ), Hypertensive crisis (0.25% ), Myocardial infarction, Myocardial ischemia
Dermatologic: Acral erythema, Grade 3 or 4 (17% to 22% ), Erythema multiforme (0.2% ), Stevens-Johnson syndrome (0.2% ), Toxic epidermal necrolysis (0.17% )
Gastrointestinal: Gastrointestinal fistula, Gastrointestinal perforation
Hematologic: Hemorrhage (11% to 21% )
Hepatic: ALT/SGPT level raised, Grades 3 and 4 (Grade 3, 4% to 5%; grade 4, 1% ), AST/SGOT level raised, Grades 3 and 4 (Grade 3, 3% to 5%; grade 4, 1% ), Hepatotoxicity, Liver failure (0.8% to 1.6% )

Gastrointestinal stromal tumor, Locally advanced, unresectable, or metastatic disease, after treatment with imatinib and sunitinib
160 mg orally once daily with a low-fat breakfast on days 1 through 21 of each 28-day cycle until disease progression or unacceptable toxicity
Liver carcinoma, In patients previously treated with sorafenib
160 mg orally once daily after a low-fat breakfast on days 1 through 21 of each 28-day cycle until disease progression or unacceptable toxicity
Metastatic colorectal cancer, In patients previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-containing chemotherapy, and anti-VEGF therapy, and if RAS wild type, an anti-EGFR therapy
160 mg orally once daily with a low-fat breakfast on days 1 through 21 of each 28-day cycle until disease progression or unacceptable toxicity .

Safety and efficacy in pediatric patients have not been established.

Preexisting mild (total bilirubin ? ULN and AST > ULN or total bilirubin > ULN to ?1.5 times ULN) or moderate (total bilirubin >1.5 times to ?3 times ULN and any AST) impairment: No dosage adjustment necessary; closely monitor for adverse effects.
Preexisting severe impairment (total bilirubin >3 times ULN): Use is not recommended (has not been studied).
Hepatotoxicity during treatment:
Grade 3 AST and/or ALT elevation: Withhold dose until recovery. If benefit of treatment outweighs toxicity risk, resume therapy at a reduced dose of 120 mg once daily.
AST or ALT >20 times ULN: Discontinue permanently.
AST or ALT >3 times ULN and bilirubin >2 times ULN: Discontinue permanently.
Recurrence of AST or ALT >5 times ULN despite dose reduction to 120 mg: Discontinue permanently.