DGIdb - LUMACAFTOR Drug Record

LUMACAFTOR chembl:CHEMBL2103870 Approved

Alternate Names:

VRT-826809
VX 809
VX-809
VRT 826809
LUMACAFTOR
3-(6-{[1-(2,2-DIFLUORO-2H-1,3-BENZODIOXOL-5-YL)CYCLOPROPANE-1-CARBONYL]AMINO}-3-METHYLPYRIDIN-2-YL)BENZOIC ACID
chembl:CHEMBL2103870
rxcui:1655922
drugbank:09280
pubchem.compound:16678941
chemidplus:936727-05-8

Drug Info:

FDA Approval	not approved
Drug Class	small molecule
Drug Indications	for treatment of cystic fibrosis

(3 More Sources)

Publications:

Hubert D et al., 2017, Real-life initiation of lumacaftor/ivacaftor combination in adults with cystic fibrosis homozygous for the Phe508del CFTR mutation and severe lung disease., J Cyst Fibros
Dekkers JF et al., 2016, Characterizing responses to CFTR-modulating drugs using rectal organoids derived from subjects with cystic fibrosis., Sci Transl Med
Veit G et al., 2016, From CFTR biology toward combinatorial pharmacotherapy: expanded classification of cystic fibrosis mutations., Mol Biol Cell
Awatade NT et al., 2014, Measurements of Functional Responses in Human Primary Lung Cells as a Basis for Personalized Therapy for Cystic Fibrosis., EBioMedicine
Yu et al., 2012, Ivacaftor potentiation of multiple CFTR channels with gating mutations., J. Cyst. Fibros.
Van Goor F et al., 2011, Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809., Proc Natl Acad Sci U S A
Clancy JP et al., 2012, Results of a phase IIa study of VX-809, an investigational CFTR corrector compound, in subjects with cystic fibrosis homozygous for the F508del-CFTR mutation., Thorax
Boyle MP et al., 2014, A CFTR corrector (lumacaftor) and a CFTR potentiator (ivacaftor) for treatment of patients with cystic fibrosis who have a phe508del CFTR mutation: a phase 2 randomised controlled trial., Lancet Respir Med
Kopeikin Z et al., 2014, Combined effects of VX-770 and VX-809 on several functional abnormalities of F508del-CFTR channels., J Cyst Fibros
Ikpa PT et al., 2014, Cystic fibrosis: toward personalized therapies., Int J Biochem Cell Biol
Norman P, 2014, Novel picolinamide-based cystic fibrosis transmembrane regulator modulators: evaluation of WO2013038373, WO2013038376, WO2013038381, WO2013038386 and WO2013038390., Expert Opin Ther Pat
Compain P et al., 2013, Rescue of functional CFTR channels in cystic fibrosis: a dramatic multivalent effect using iminosugar cluster-based correctors., Chembiochem
Van Goor F et al., 2014, Effect of ivacaftor on CFTR forms with missense mutations associated with defects in protein processing or function., J Cyst Fibros
Lubamba B et al., 2012, Cystic fibrosis: insight into CFTR pathophysiology and pharmacotherapy., Clin Biochem
Pesce E et al., 2015, Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis., Eur J Med Chem
Kuk et al., 2015, Lumacaftor and ivacaftor in the management of patients with cystic fibrosis: current evidence and future prospects., Ther Adv Respir Dis

LUMACAFTOR CFTR

Interaction Score: 85.02

Interaction Types & Directionality:

modulator

Interaction Info:

Trial Name VX-809

Novel drug target Established target

Trial Name VX-809 + VX-770

PMIDs:
28325531 27334259 26823392 26137539 22293084 21976485 21825083 24973281 24796242 24561283 24392786 24038832 23891399 22698459 26041577 26416827

Sources:
DTC TdgClinicalTrial ChemblInteractions PharmGKB TTD FDA

TdgClinicalTrial: VX-809
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications for treatment of cystic fibrosis

Drug Class small molecule

FDA Approval not approved

Publications:
DTC: LUMACAFTOR
- Version: 02-September-2020
Alternate Names:

CHEMBL2103870 ChEMBL Drug ID

Drug Info:

Publications:

Pesce E et al., 2015, Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis., Eur J Med Chem

PharmGKB: lumacaftor

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Lubamba B et al., 2012, Cystic fibrosis: insight into CFTR pathophysiology and pharmacotherapy., Clin Biochem

Ikpa PT et al., 2014, Cystic fibrosis: toward personalized therapies., Int J Biochem Cell Biol

Awatade NT et al., 2014, Measurements of Functional Responses in Human Primary Lung Cells as a Basis for Personalized Therapy for Cystic Fibrosis., EBioMedicine

TTD: Lumacaftor
- Version: 2020.06.01
Alternate Names:

D0X0CB TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2103870
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2103870
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
FDA: Lumacaftor
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Trial Name	VX-809
Novel drug target	Established target
Trial Name	VX-809 + VX-770

LUMACAFTOR Drug Record

LUMACAFTOR chembl:CHEMBL2103870 Approved

Alternate Names:

Drug Info:

Publications:

LUMACAFTOR CFTR

Interaction Types & Directionality: modulator

Interaction Info: Trial Name VX-809 Novel drug target Established target Trial Name VX-809 + VX-770

PMIDs: 28325531 27334259 26823392 26137539 22293084 21976485 21825083 24973281 24796242 24561283 24392786 24038832 23891399 22698459 26041577 26416827

Sources: DTC TdgClinicalTrial ChemblInteractions PharmGKB TTD FDA

TdgClinicalTrial: VX-809

Alternate Names:

Drug Info: Drug Indications for treatment of cystic fibrosis Drug Class small molecule FDA Approval not approved

Publications:

DTC: LUMACAFTOR

Alternate Names: CHEMBL2103870 ChEMBL Drug ID

Drug Info:

Publications: Pesce E et al., 2015, Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis., Eur J Med Chem

PharmGKB: lumacaftor

Alternate Names:

Drug Info:

TTD: Lumacaftor

Alternate Names: D0X0CB TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL2103870

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL2103870

Alternate Names:

Drug Info:

Publications:

FDA: Lumacaftor

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

modulator

Interaction Info:

Trial Name VX-809

Novel drug target Established target

Trial Name VX-809 + VX-770

PMIDs:
28325531 27334259 26823392 26137539 22293084 21976485 21825083 24973281 24796242 24561283 24392786 24038832 23891399 22698459 26041577 26416827

Sources:
DTC TdgClinicalTrial ChemblInteractions PharmGKB TTD FDA

Drug Info:

Drug Indications for treatment of cystic fibrosis

Drug Class small molecule

FDA Approval not approved

Alternate Names:

CHEMBL2103870 ChEMBL Drug ID

Publications:

Pesce E et al., 2015, Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis., Eur J Med Chem

Alternate Names:

D0X0CB TTD Drug ID