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gptkbp:instance_of
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gptkb:pharmaceuticals
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gptkbp:approves
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gptkb:FDA
October 2019
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gptkbp:atccode
|
R07 AX03
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gptkbp:availability
|
prescription only
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gptkbp:can_be_combined_with
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gptkb:Ivacaftor
gptkb:Tezacaftor
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gptkbp:casnumber
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1394640-80-0
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gptkbp:chemical_formula
|
C22 H26 F2 N4 O3 S
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gptkbp:clinical_trial
|
Phase 3
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gptkbp:clinical_use
|
in patients aged 12 years and older
in patients with at least one F508del mutation
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gptkbp:contraindication
|
severe liver impairment
hypersensitivity to elexacaftor
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gptkbp:developed_by
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gptkb:Vertex_Pharmaceuticals
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gptkbp:dissolved
|
soluble in DMSO
slightly soluble in water
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gptkbp:dosage_form
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gptkb:tablet
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gptkbp:drug_interactions
|
with strong CYP3 A inducers
with strong CYP3 A inhibitors
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gptkbp:excretion
|
urine
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|
https://www.w3.org/2000/01/rdf-schema#label
|
Elexacaftor
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gptkbp:indication
|
homozygous F508del mutation in CFTR gene
other mutations in CFTR gene
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gptkbp:invention
|
patented
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gptkbp:is_monitored_by
|
pulmonary function tests
liver function tests
|
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gptkbp:lifespan
|
approximately 12 hours
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gptkbp:marketed_as
|
gptkb:Trikafta
|
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gptkbp:mechanism_of_action
|
CFTR modulator
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gptkbp:metabolism
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gptkb:CYP3_A4
|
|
gptkbp:monitors
|
3 F1 B1 D1 F1 D
|
|
gptkbp:pharmacokinetics
|
improves CFTR function
oral bioavailability around 80%
|
|
gptkbp:price
|
high cost
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|
gptkbp:research
|
ongoing for additional mutations
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gptkbp:route_of_administration
|
oral
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gptkbp:safety_features
|
generally well tolerated
|
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gptkbp:side_effect
|
fatigue
headache
nausea
diarrhea
elevated liver enzymes
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gptkbp:targets
|
CFTR protein
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gptkbp:treatment
|
with Tezacaftor and Ivacaftor
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gptkbp:type_of_care
|
important for treatment efficacy
|
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gptkbp:used_for
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gptkb:cystic_fibrosis
|
|
gptkbp:weight
|
452.53 g/mol
|
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gptkbp:bfsParent
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gptkb:CFTR_modulators
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gptkbp:bfsLayer
|
5
|