Comparative Pharmacology
Head-to-head clinical analysis: IVACAFTOR versus SYMDEKO COPACKAGED.
Peer-Reviewed Evidence
Head-to-head clinical analysis: IVACAFTOR versus SYMDEKO COPACKAGED.
IVACAFTOR vs SYMDEKO (COPACKAGED)
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Ivacaftor is a CFTR potentiator that increases the open probability of the cystic fibrosis transmembrane conductance regulator (CFTR) protein at the cell surface, enhancing chloride transport in epithelial cells. It is effective in CFTR mutations with residual function or responsive to potentiators.
Symdeko is a combination of tezacaftor and ivacaftor. Tezacaftor is a CFTR corrector that facilitates the cellular processing and trafficking of the F508del-CFTR protein to the cell surface, while ivacaftor is a CFTR potentiator that increases the open probability of CFTR channels at the cell surface, thereby enhancing chloride transport in epithelial cells.
150 mg orally every 12 hours with fat-containing food.
Two tablets orally every 12 hours: one tablet tezacaftor 50mg/ivacaftor 75mg and one tablet ivacaftor 150mg, taken with fat-containing food.
None Documented
None Documented
Clinical Note
moderateIvacaftor + Sulfisoxazole
"The serum concentration of Sulfisoxazole can be increased when it is combined with Ivacaftor."
Clinical Note
moderateIvacaftor + Erythromycin
"The serum concentration of Erythromycin can be increased when it is combined with Ivacaftor."
Clinical Note
moderateIvacaftor + Cyclosporine
"The serum concentration of Cyclosporine can be increased when it is combined with Ivacaftor."
Clinical Note
moderateIvacaftor + Fluconazole
12-14 hours in healthy subjects; steady state achieved in 3-5 days
Tezacaftor: terminal half-life approximately 15 hours; ivacaftor: terminal half-life approximately 12 hours (range 9–15 hours). The half-lives support twice-daily dosing (every 12 hours) for steady state.
Primarily fecal (87%) as unchanged drug and metabolites; renal excretion accounts for <1%
Tezacaftor is primarily metabolized, with <1% excreted unchanged in urine and 72% of the dose recovered in feces (mainly as metabolites). Ivacaftor is extensively metabolized; 87% of the dose is excreted in feces (mostly as metabolites) and <1% in urine. Biliary/fecal elimination is the major route for both.
Category A/B
Category C
CFTR Potentiator
CFTR Potentiator/Corrector
"The serum concentration of Fluconazole can be increased when it is combined with Ivacaftor."