Details of the Drug Combination

General Information of Drug Combination (ID: DC4O3K4)

Drug Combination Name
ARRY-162 Alpelisib
Indication
Disease Entry Status REF
Advanced and Selected Solid Tumors Phase 1 [1]
Component Drugs ARRY-162   DM1P6FR Alpelisib   DMEXMYK
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 ARRY-162
Disease Entry ICD 11 Status REF
Melanoma 2C30 Approved [2]
ARRY-162 Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
MAPK/ERK kinase kinase (MAP3K) TTROQ37 NOUNIPROTAC Modulator [5]
ERK activator kinase (MEK) TTZCRP3 NOUNIPROTAC Inhibitor [2]
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ARRY-162 Interacts with 2 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [6]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [6]
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ARRY-162 Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [7]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Metabolism [8]
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Indication(s) of Alpelisib
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Approved [3]
Solid tumour/cancer 2A00-2F9Z Phase 2 [4]
Alpelisib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
PI3-kinase alpha (PIK3CA) TTEUNMR PK3CA_HUMAN Inhibitor [3]
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Alpelisib Interacts with 1 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [9]
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References

1 ClinicalTrials.gov (NCT01449058) A Phase Ib Study of MEK162 Plus BYL719 in Adult Patients With Selected Advanced Solid Tumors
2 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
4 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: 7955).
5 MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013; 6: 27.
6 The impact of P-glycoprotein and breast cancer resistance protein on the brain pharmacokinetics and pharmacodynamics of a panel of MEK inhibitors. Int J Cancer. 2018 Jan 15;142(2):381-391.
7 FDA Label of Binimetinib. The 2020 official website of the U.S. Food and Drug Administration.
8 Binimetinib - European Medicines Agency - European Union
9 Comparison of 19F NMR and 14C measurements for the assessment of ADME of BYL719 (Alpelisib) in humans. Drug Metab Dispos. 2017 Aug;45(8):900-907.