General Information of Drug Combination (ID: DC3NBGU)

Drug Combination Name
Exherin CP-868596
Indication
Disease Entry Status REF
Ewing sarcoma Investigative [1]
Component Drugs Exherin   DMC1I56 CP-868596   DMZIM37
Small molecular drug 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: 14.067
Bliss Independence Score: 12.748
Loewe Additivity Score: 1.721
LHighest Single Agent (HSA) Score: 6.046

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Exherin
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 2 [2]
Exherin Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Neural cadherin (CDH2) TT1WS0T CADH2_HUMAN Binder [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 (NCT00264433) A Study of the Safety and Effects of ADH-1 Given Intravenously as a Single Agent. 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 Clinical and pharmacological phase I evaluation of Exherin (ADH-1), a selective anti-N-cadherin peptide in patients with N-cadherin-expressing soli... Ann Oncol. 2009 Apr;20(4):741-5.
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.