Details of the Drug Combination

General Information of Drug Combination (ID: DCD6K9J)

Drug Combination Name
Lumacaftor Ivacaftor
Indication
Disease Entry Status REF
Cystic Fibrosis Phase 1 [1]
Component Drugs Lumacaftor   DMCLWDJ Ivacaftor   DMZC1HS
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Lumacaftor
Disease Entry ICD 11 Status REF
Cystic fibrosis CA25 Phase 2 [2]
Lumacaftor Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
cAMP-dependent chloride channel (CFTR) TTRLZHP CFTR_HUMAN Regulator [4]
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Indication(s) of Ivacaftor
Disease Entry ICD 11 Status REF
Cystic fibrosis CA25 Approved [3]
Ivacaftor Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
cAMP-dependent chloride channel (CFTR) TTRLZHP CFTR_HUMAN Modulator [5]
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Ivacaftor Interacts with 1 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [6]
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Ivacaftor Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [7]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [7]
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Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Cystic fibrosis; Acute lung injury DCEIVC9 N. A. Approved [8]
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References

1 ClinicalTrials.gov (NCT01768663) A Phase 1 Study to Examine the Drug-Drug Interaction of Ciprofloxacin, Itraconazole, and Rifampin on the Combination of Lumacaftor With Ivacaftor in Healthy Adult Subjects
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7481).
3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4342).
4 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. 2014 Jul;2(7):527-38.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
6 Investigation of the effects of the CFTR potentiator ivacaftor on human P-glycoprotein (ABCB1). Sci Rep. 2017 Dec 13;7(1):17481.
7 Sensitivity of ivacaftor to drug-drug interactions with rifampin, a cytochrome P450 3A4 inducer. Pediatr Pulmonol. 2018 May;53(5):E6-E8.
8 FDA Drug Development and Drug Interactions