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RX BIN: 015558
RX PCN: HT
Group ID: DDN6600
Card Holder ID: DDN6600

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2018 Price of Lumacaftor

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Lumacaftor volume of distribution

Following oral administration of 200 mg of lumacaftor every 24 hours to cystic fibrosis patients in a fed state for 28 days, the mean (+/-SD) for apparent volumes of distribution was 86.0 (69.8) L. (2)

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What is Lumacaftor

Lumacaftor is an experimental drug for the treatment of cystic fibrosis developed by Vertex Pharmaceuticals. The drug is designed to be effective in patients that have the F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR), the defective protein that causes the disease. F508del, meaning that the amino acid phenylalanine in position 508 is missing, is found in about 60% of cystic fibrosis patients in Europe, and in about 90% of persons with some mutation in the CFTR gene.

Lumacaftor mechanism of action

The CFTR protein is a chloride channel and is found on the surface of epithelial cells in many tissues and organs. Cystic fibrosis involves an F508del mutation which results in a lower amount of properly processed chloride channels and also less which are successfully trafficked to cellular surfaces. Furthermore, the mutated CFTR that are able to reach cell surfaces will not function optimally. Lumacaftor helps stabilize F508del-CFTR, allowing more processing and trafficking to occur which increases the amount of mature protein that will reach cell surfaces. (2)

Dosage forms of Lumacaftor

FormRouteStrength
Tabletoral
Tablet, film coatedoral
Prescription Generics

false

International Brands

Orkambi

Synonyms

3-(6-{[1-(2,2-difluoro-2H-1,3-benzodioxol-5-yl)cyclopropane-1-carbonyl]amino}-3-methylpyridin-2-yl)benzoic acid lumacaftor

Manufacturers

Vertex Pharmaceuticals (Canada) Incorporated

CAS number

936727-05-8

UNII

EGP8L81APK

State

solid

Affected organisms

Indication of Lumacaftor

Cystic fibrosis is a disease that is caused by dysfunction of the ‘cystic fibrosis transmembrane conductance regulator protein’ (CFTR). As a result, cystic fibrosis affects many systems and involves progressive lung disease. Lumacaftor is an effective treatment for cystic fibrosis because it helps correct CFTR as well as the associated functions. (1)

Toxicity of Lumacaftor

Dyspnea, nasopharyngitis, nausea, diarrhea, upper respiratory tract infection, fatigue, respiration abnormal, blood creatine phosphokinase increased, rash, flatulence, rhinorrhea, and influenza are the most common adverse effects reported with the use of ORKAMBI. These adverse effects occurred in 5% of patients with cystic fibrosis homozygous for the F508del mutation in the CFTR gene. Lumacaftor is classified as Pregnancy Category B. (2)

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