Statements (50)
Predicate | Object |
---|---|
gptkbp:instance_of |
gptkb:drug
|
gptkbp:bfsLayer |
4
|
gptkbp:bfsParent |
gptkb:CFTR_modulators
|
gptkbp:activities |
CFTR modulator
|
gptkbp:approves |
gptkb:FDA
October 2019 |
gptkbp:availability |
prescription only
|
gptkbp:can_be_used_with |
gptkb:Ivacaftor
gptkb:Tezacaftor |
gptkbp:clinical_trial |
Phase 3
in patients aged 12 years and older in patients with at least one F508del mutation |
gptkbp:contraindication |
severe liver impairment
hypersensitivity to elexacaftor |
gptkbp:developed_by |
gptkb:Vertex_Pharmaceuticals
|
gptkbp:dissolved |
soluble in DMSO
slightly soluble in water |
gptkbp:dosage_form |
gptkb:tablet
|
gptkbp:excretion |
urine
|
https://www.w3.org/2000/01/rdf-schema#label |
Elexacaftor
|
gptkbp:indication |
homozygous F508del mutation in CFTR gene
other mutations in CFTR gene |
gptkbp:ingredients |
C22 H26 F2 N4 O3 S
|
gptkbp:interacts_with |
with strong CY P3 A inducers
with strong CY P3 A inhibitors |
gptkbp:invention |
patented
|
gptkbp:is_atype_of |
R07 A X03
|
gptkbp:is_monitored_by |
pulmonary function tests
liver function tests |
gptkbp:is_used_for |
gptkb:cystic_fibrosis
|
gptkbp:lifespan |
approximately 12 hours
|
gptkbp:manager |
oral
|
gptkbp:marketed_as |
gptkb:Trikafta
|
gptkbp:metabolism |
CY P3 A4
|
gptkbp:monitors |
3 F1 B1 D1 F1 D
|
gptkbp:pharmacokinetics |
improves CFTR function
oral bioavailability around 80% |
gptkbp:price |
high cost
|
gptkbp:research |
ongoing for additional mutations
|
gptkbp:safety_features |
generally well tolerated
|
gptkbp:side_effect |
fatigue
headache nausea diarrhea elevated liver enzymes |
gptkbp:targets |
CFTR protein
|
gptkbp:treatment |
with Tezacaftor and Ivacaftor
|
gptkbp:type_of |
1394640-80-0
|
gptkbp:type_of_care |
important for treatment efficacy
|
gptkbp:weight |
452.53 g/mol
|