Comparative Pharmacology
Head-to-head clinical analysis: CAPRELSA versus REGORAFENIB.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CAPRELSA versus REGORAFENIB.
CAPRELSA vs REGORAFENIB
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Inhibits multiple receptor tyrosine kinases involved in tumor angiogenesis and oncogenesis, including VEGFR2, EGFR, and RET.
Regorafenib is a multikinase inhibitor that targets various angiogenic (VEGFR1-3, TIE2), stromal (PDGFR-β, FGFR), and oncogenic kinases (KIT, RET, RAF). It inhibits tumor angiogenesis, growth, and metastasis.
300 mg orally once daily, with or without food.
160 mg orally once daily on days 1-21 of a 28-day cycle until disease progression or unacceptable toxicity.
None Documented
None Documented
Terminal half-life approximately 90 hours (range 30–150 hours), supporting once-daily dosing; steady-state achieved by day 15.
Clinical Note
moderateRegorafenib + Digoxin
"Regorafenib may increase the bradycardic activities of Digoxin."
Clinical Note
moderateRegorafenib + Digitoxin
"Regorafenib may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateRegorafenib + Deslanoside
"Regorafenib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateRegorafenib + Acetyldigitoxin
"Regorafenib may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal half-life is 14–28 hours (mean approximately 20 hours), supporting twice-daily dosing with a 3-weeks-on/1-week-off schedule to allow washout and reduce toxicity accumulation.
Primarily fecal (approximately 75% of administered dose, mainly as unchanged drug and metabolites); renal excretion accounts for about 25% (less than 1% unchanged).
Primarily fecal (approximately 71% of the radiolabeled dose) with renal excretion accounting for 19% (mostly as metabolites). Unchanged regorafenib is minimal in urine.
Category C
Category D/X
Kinase Inhibitor
Kinase Inhibitor