Details of the Drug Combination

General Information of Drug Combination (ID: DCRFU87)

Drug Combination Name
BIX-01294 Piperaquine
Indication
Disease Entry Status REF
DD2 Investigative [1]
Component Drugs BIX-01294   DM5CBNY Piperaquine   DMT70RC
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL is unavailable 3D MOL
High-throughput Screening Result Testing Cell Line: DD2
Zero Interaction Potency (ZIP) Score: 9.239
Bliss Independence Score: 6.725
Loewe Additivity Score: 5.475
LHighest Single Agent (HSA) Score: 6.778

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of BIX-01294
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Preclinical [2]
BIX-01294 Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Euchromatic histone-lysine N-methyltransferase 1 (EHMT1) TTOFXD7 EHMT1_HUMAN Inhibitor [4]
Histone-lysine N-methyltransferase EHMT2 (EHMT2) TTS6RZT EHMT2_HUMAN Inhibitor [4]
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BIX-01294 Interacts with 2 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Interferon alpha-2 (IFNA2) OT4GII73 IFNA2_HUMAN Increases Response To Substance [5]
Interferon regulatory factor 7 (IRF7) OTC1A2PQ IRF7_HUMAN Increases Expression [5]
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Indication(s) of Piperaquine
Disease Entry ICD 11 Status REF
Malaria 1F40-1F45 Approved [3]
Piperaquine Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Sarcoplasmic/endoplasmic reticulum calcium ATPase (ATP2A) TTZVSJ2 NOUNIPROTAC Inhibitor [3]
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Piperaquine Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Metabolism [6]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Metabolism [7]
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References

1 Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
2 Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286.
3 The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71.
4 Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81.
5 Inhibition of euchromatic histone methyltransferase 1 and 2 sensitizes chronic myeloid leukemia cells to interferon treatment. PLoS One. 2014 Jul 31;9(7):e103915. doi: 10.1371/journal.pone.0103915. eCollection 2014.
6 Eurartesim - European Medicines Agency
7 Open-label crossover study of primaquine and dihydroartemisinin-piperaquine pharmacokinetics in healthy adult thai subjects. Antimicrob Agents Chemother. 2014 Dec;58(12):7340-6.