lumacaftor indications/contra

Stem definitionDrug idCAS RN
cystic fibrosis transmembrane regulator (CFTR) protein modulators 5010 936727-05-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lumacaftor
  • VX-809
  • VRT-826809
a corrector of CF transmembrane conductance regulator (CTFR)
  • Molecular weight: 452.41
  • Formula: C24H18F2N2O5
  • CLOGP: 6.05
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 2
  • TPSA: 97.75
  • ALOGS: -5.08
  • RINGS: 5
  • ROTB: 5

Drug dosage:

DoseUnitRoute
400 mg O

Approvals:

DateAgencyCompanyOrphan
July 2, 2015 FDA VERTEX PHARMS INC

Pharmacologic Action:

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SourceCodeDescription
ATC R07AX30 RESPIRATORY SYSTEM
OTHER RESPIRATORY SYSTEM PRODUCTS
OTHER RESPIRATORY SYSTEM PRODUCTS
Other respiratory system products
FDA EPC N0000184146 Cystic Fibrosis Transmembrane Conductance Regulator Potentiator
FDA MoA N0000184145 Chloride Channel Activation Potentiators
FDA MoA N0000190118 Cytochrome P450 3A Inducers
FDA MoA N0000187064 Cytochrome P450 2B6 Inducers
FDA MoA N0000187063 Cytochrome P450 2C8 Inducers
FDA MoA N0000185507 Cytochrome P450 2C9 Inducers
FDA MoA N0000185607 Cytochrome P450 2C19 Inducers
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000185504 Cytochrome P450 2C9 Inhibitors
CHEBI has role CHEBI:71031 orphan drug

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Cystic fibrosis of the lung indication 86555001

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Cystic fibrosis transmembrane conductance regulator Ion channel POSITIVE MODULATOR EC50 6.46 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

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IDSource
4034600 VANDF
N0000191736 NDFRT
016231 NDDF
1655922 RXNORM
31119 MMSL
d08371 MMSL
716073005 SNOMEDCT_US
DB09280 DRUGBANK_ID
C569105 MESH_SUPPLEMENTAL_RECORD_UI
D10134 KEGG_DRUG
9449 INN_ID
EGP8L81APK UNII
CHEBI:90951 CHEBI
16678941 PUBCHEM_CID
7481 IUPHAR_LIGAND_ID
CHEMBL2103870 ChEMBL_ID
N0000191736 NUI
C3852684 UMLSCUI
4034600 VUID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
ORKAMBI HUMAN PRESCRIPTION DRUG LABEL 2 51167-700 TABLET, FILM COATED 100 mg ORAL NDA 19 sections
ORKAMBI HUMAN PRESCRIPTION DRUG LABEL 2 51167-809 TABLET, FILM COATED 200 mg ORAL NDA 19 sections