Elexacaftor tezacaftor ivacaftor Brand Name– Trikafta
What is Elexacaftor tezacaftor ivacaftor
Elexacaftor tezacaftor ivacaftor is an oral combination ion channel modulator approved for the treatment of cystic fibrosis (CF) in patients 12 years of age and older who have at least 1 F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR) gene.
Although there are approximately 2,000 known mutations of the CFTR gene, the F508del mutation is the most frequent genotype in patients with CF. In the United States, 90% of the population with CF, or roughly 27,000 people, have at least 1 F508del mutation.
CFTR modulators, such as elexacaftor; tezacaftor; ivacaftor, target specific defects caused by mutations in CFTR, thereby helping the protein made by the CFTR gene mutation function more effectively.
Clinical trials have demonstrated that combination corrector and potentiator treatment enhance CFTR function and improve lung function.
During a Phase 3 trial in patients 12 years and older, mean ppFEV1 increased 13.9% from baseline compared to placebo. Improvements were also noted in sweat chloride, number of pulmonary exacerbations, and body mass index.
In another trial, mean ppFEV1 increased 10% from baseline compared to tezacaftor; ivacaftor. Adverse reactions related to elevated liver transaminases have been reported in patients receiving elexacaftor; tezacaftor; ivacaftor and, in pediatric patients, ivacaftor has been associated with the development of cataracts.
Hence, liver function monitoring and eye exams are required at baseline and periodically throughout therapy.
Indications
- cystic fibrosis
Side Effects
- abdominal pain
- conjunctivitis
- diarrhea
- dizziness
- dysmenorrhea
- elevated hepatic enzymes
- flatulence
- headache
- hyperbilirubinemia
- hypoglycemia
- infection
- influenza
- nasal congestion
- pharyngitis
- pruritus
- rash
- rhinitis
- rhinorrhea
- sinusitis
Monitoring Parameters
- LFTs
- ophthalmologic exam
Contraindications
- breast-feeding
- cataracts
- children
- hepatic disease
- pregnancy
- renal disease
- renal failure
- renal impairment
Interactions
- Acetaminophen; Caffeine; Dihydrocodeine
- Acetaminophen; Diphenhydramine
- Acetaminophen; Hydrocodone
- Acetaminophen; Oxycodone
- Acetaminophen; Tramadol
- Afatinib
- Alfentanil
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- Alprazolam
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- Amlodipine; Valsartan
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- Amoxicillin; Clarithromycin; Omeprazole
- Apalutamide
- Aprepitant, Fosaprepitant
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- Aspirin, ASA; Oxycodone
- Aspirin, ASA; Pravastatin
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- Emtricitabine; Rilpivirine; Tenofovir alafenamide
- Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
- Emtricitabine; Tenofovir alafenamide
- Emtricitabine; Tenofovir disoproxil fumarate
- Enalapril; Felodipine
- Encorafenib
- Enzalutamide
- Ergotamine
- Erythromycin
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- Glimepiride; Rosiglitazone
- Glipizide
- Glipizide; Metformin
- Glyburide
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- grapefruit juice
- Guaifenesin; Hydrocodone
- Guaifenesin; Hydrocodone; Pseudoephedrine
- Homatropine; Hydrocodone
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- Hydrocodone
- Hydrocodone; Ibuprofen
- Hydrocodone; Phenylephrine
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