Comparative Pharmacology
Head-to-head clinical analysis: IVACAFTOR versus KALYDECO.
Peer-Reviewed Evidence
Head-to-head clinical analysis: IVACAFTOR versus KALYDECO.
IVACAFTOR vs KALYDECO
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.
Potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) protein; increases the probability of CFTR channel opening by binding to the nucleotide-binding domain, thereby enhancing chloride transport in cells with defective CFTR gating mutations.
150 mg orally every 12 hours with fat-containing food.
150 mg orally every 12 hours 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
12 hours (terminal); supports twice-daily dosing; steady-state reached in 2-3 days.
Primarily fecal (87%) as unchanged drug and metabolites; renal excretion accounts for <1%
Primarily hepatic metabolism (CYP3A4), then biliary/fecal elimination; 88% in feces, <1% in urine as unchanged drug.
Category A/B
Category C
CFTR Potentiator
CFTR Potentiator
"The serum concentration of Fluconazole can be increased when it is combined with Ivacaftor."