Comparative Pharmacology
Head-to-head clinical analysis: EXKIVITY versus STIVARGA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EXKIVITY versus STIVARGA.
EXKIVITY vs STIVARGA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Irreversible tyrosine kinase inhibitor that selectively targets epidermal growth factor receptor (EGFR) exon 19 deletion or exon 21 L858R substitution mutations, and specifically inhibits EGFR T790M and C797S resistance mutations, with less activity against wild-type EGFR.
Multikinase inhibitor that inhibits VEGFR-1, -2, -3, PDGFR-α, PDGFR-β, FGFR-1, -2, TIE2, KIT, RET, RAF-1, and B-RAF.
150 mg orally once daily with or without food.
160 mg orally once daily for 3 weeks, followed by 1 week off (28-day cycle).
None Documented
None Documented
Terminal elimination half-life is approximately 48 hours, supporting once-daily dosing for systemic exposure.
Terminal elimination half-life is approximately 30 hours (range 15-42 h) for regorafenib and 25-60 h for its active metabolites M-2 and M-5. Steady-state is reached within 2-3 weeks.
Primarily hepatic metabolism with biliary excretion; 91% of total recovered in feces (30% as unchanged drug), <1% in urine.
Approximately 51% fecal (as unchanged drug and metabolites), 19% renal (as metabolites, <1% unchanged).
Category C
Category C
Tyrosine Kinase Inhibitor
Tyrosine Kinase Inhibitor