Contraindicated in:
Use Cautiously in:
Derm: rash.
EENT: nasal congestion, cataracts, rhinitis, rhinorrhea, sinusitis.
GI: ↑ liver enzymes, abdominal pain, diarrhea, HEPATOTOXICITY, hyperbilirubinemia.
MS: ↑ creatine kinase.
Neuro: headache.
Resp: upper respiratory tract infection.
Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), influenza.
Drug-Drug:
Drug-Natural Products:
Drug-Food:
Hepatic Impairment
Hepatic Impairment
Hepatic Impairment
Hepatic Impairment
Hepatic Impairment
Therapeutic Classification: cystic fibrosis therapy adjuncts
Pharmacologic Classification: transmembrane conductance regulator potentiators
Elexacaftor
Absorption: Well absorbed (88%) following oral administration; absorption is enhanced 2-fold by moderate-fat-containing foods.
Distribution: Well distributed to tissues.
Protein Binding: >99%.
Metabolism/Excretion: Primarily metabolized in liver via the CYP3A4 and CYP3A5 isoenzymes; one metabolite (M23) is pharmacologically active; 87% excreted in feces (primarily as metabolite); <1% excreted in urine.
Half-life: 30 hr.
Tezacaftor
Absorption: Some absorption following oral administration.
Distribution: Widely distributed to tissues.
Protein Binding: >99%.
Metabolism/Excretion: Primarily metabolized in liver via the CYP3A4 and CYP3A5 isoenzymes; one metabolite (M1) is pharmacologically active; 72% excreted in feces as unchanged drug or metabolite; 14% excreted in urine (primarily as metabolite).
Half-life: 15 hr.
Ivacaftor
Absorption: Some absorption following oral administration; absorption is enhanced 3-fold by fat-containing foods.
Distribution: Widely distributed to tissues.
Protein Binding: >99%.
Metabolism/Excretion: Primarily metabolized in liver via the CYP3A4 and CYP3A5 isoenzymes; one metabolite (M1) is pharmacologically active; 87.8% eliminated in feces; negligible urinary elimination.
Half-life: 14 hr.
(plasma concentrations)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
Elexacaftor (PO) | unknown | 6 hr | 24 hr |
Tezacaftor (PO) | unknown | 4 hr | 12 hr |
Ivacaftor (PO) | unknown | 6 hr | 12 hr |