Details of the Drug Combination

General Information of Drug Combination (ID: DC47IF5)

Drug Combination Name
ARRY-162 Pexidartinib
Indication
Disease Entry Status REF
Gastrointestinal Stromal Tumor (GIST) Phase 1 [1]
Component Drugs ARRY-162   DM1P6FR Pexidartinib   DMS2J0Z
Small molecular drug N.A.
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 [7]
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 [8]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [8]
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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 [9]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Metabolism [10]
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Indication(s) of Pexidartinib
Disease Entry ICD 11 Status REF
Tenosynovial giant cell tumour 2F7B Approved [3]
Alzheimer disease 8A20 Phase 3 [4]
Pigmented villonodular synovitis FA27.1 Phase 3 [5]
Neurofibromatosis type 1 LD2D.10 Phase 1/2 [6]
Pexidartinib Interacts with 3 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Macrophage colony-stimulating factor 1 receptor (CSF1R) TT7MRDV CSF1R_HUMAN Inhibitor [3]
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Inhibitor [3]
Fms-like tyrosine kinase 3 (FLT-3) TTGJCWZ FLT3_HUMAN Inhibitor [3]
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Pexidartinib Interacts with 1 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Macrophage colony-stimulating factor 1 (CSF1) OT68M7RD CSF1_HUMAN Decreases Secretion [11]
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References

1 ClinicalTrials.gov (NCT03158103) A Study of MEK162 (Binimetinib) in Combination With Pexidartinib in Patients With Advanced Gastrointestinal Stromal Tumor (GIST)
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 ClinicalTrials.gov (NCT02371369) PLX3397 Phase 3 Study for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS). U.S. National Institutes of Health.
5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7 MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013; 6: 27.
8 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.
9 FDA Label of Binimetinib. The 2020 official website of the U.S. Food and Drug Administration.
10 Binimetinib - European Medicines Agency - European Union
11 Antitumor activity of a pexidartinib bioisostere inhibiting CSF1 production and CSF1R kinase activity in human hepatocellular carcinoma. Chem Biol Interact. 2023 Jan 5;369:110255. doi: 10.1016/j.cbi.2022.110255. Epub 2022 Nov 9.