Details of the Drug Combination

General Information of Drug Combination (ID: DCX00PF)

Drug Combination Name
GDC-0084 CP-868596
Indication
Disease Entry Status REF
Ewing sarcoma Investigative [1]
Component Drugs GDC-0084   DMA9SEY CP-868596   DMZIM37
N.A. Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: TC-71
Zero Interaction Potency (ZIP) Score: 38.166
Bliss Independence Score: 35.161
Loewe Additivity Score: 20.355
LHighest Single Agent (HSA) Score: 9.059

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of GDC-0084
Disease Entry ICD 11 Status REF
Glioblastoma of brain 2A00.00 Phase 2 [2]
GDC-0084 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Inhibitor [6]
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Indication(s) of CP-868596
Disease Entry ICD 11 Status REF
Gastrointestinal cancer 2C11 Phase 3 [3]
Gastrointestinal stromal tumour 2B5B Phase 3 [4]
Acute myelogenous leukaemia 2A41 Phase 2 [5]
Acute myeloid leukaemia 2A60 Phase 2 [4]
Malignant glioma 2A00.0 Phase 1 [5]
CP-868596 Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Platelet-derived growth factor receptor alpha (PDGFRA) TT8FYO9 PGFRA_HUMAN Modulator [7]
Proto-oncogene c-Src (SRC) TT6PKBN SRC_HUMAN Inhibitor [4]
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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 ClinicalTrials.gov (NCT03522298) Safety, Pharmacokinetics and Efficacy of Paxalisib (GDC-0084) in Newly-diagnosed Glioblastoma. U.S. National Institutes of Health.
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: 7882).
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
6 Current clinical development of PI3K pathway inhibitors in glioblastoma. Neuro Oncol. 2012 July; 14(7): 819-829.
7 The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.