Details of the Drug Combination

General Information of Drug Combination (ID: DC3DVEO)

Drug Combination Name
TRICIRIBINE Cotellic
Indication
Disease Entry Status REF
Embryonal rhabdomyosarcoma Investigative [1]
Component Drugs TRICIRIBINE   DM8IC5H Cotellic   DMF9M57
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: Rh36
Zero Interaction Potency (ZIP) Score: 19.575
Bliss Independence Score: 18.511
Loewe Additivity Score: 10.483
LHighest Single Agent (HSA) Score: 10.934

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of TRICIRIBINE
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1/2 [2]
TRICIRIBINE Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Human immunodeficiency virus Reverse transcriptase (HIV RT) TT84ETX POL_HV1B1 Inhibitor [6]
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TRICIRIBINE Interacts with 1 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Adenosine kinase (ADK) DE7T5VX ADK_HUMAN Metabolism [7]
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TRICIRIBINE Interacts with 3 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Follitropin subunit beta (FSHB) OTGLS283 FSHB_HUMAN Decreases Activity [8]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Expression [9]
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Increases Expression [9]
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Indication(s) of Cotellic
Disease Entry ICD 11 Status REF
Melanoma 2C30 Phase 3 [3]
Breast cancer 2C60-2C65 Phase 2 [4]
Head and neck cancer 2D42 Phase 1 [4]
Renal cell carcinoma 2C90 Phase 1 [4]
Solid tumour/cancer 2A00-2F9Z Phase 1 [5]
Urothelial carcinoma 2C92.0 Phase 1 [4]

Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Embryonal rhabdomyosarcoma DCPHXGK CTR Investigative [1]
Embryonal rhabdomyosarcoma DCIF4IT RD Investigative [1]
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References

1 CheMBL Affinity Phenotypic Cellular Interaction Assay ID: CHEMBL1125966
2 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: 5920).
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 ClinicalTrials.gov (NCT01106599) A Study Evaluating the Safety, Tolerability, and Pharmacokinetics of GDC-0623 in Patients With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health.
6 Design, synthesis and antiviral activity of novel 4,5-disubstituted 7-(beta-D-ribofuranosyl)pyrrolo[2,3-d][1,2,3]triazines and the novel 3-amino-5-... J Med Chem. 2005 Jun 2;48(11):3840-51.
7 Phosphorylation of triciribine is necessary for activity against HIV type 1. AIDS Res Hum Retroviruses. 1998 Oct 10;14(15):1315-22.
8 Inhibitory roles of prohibitin and chemerin in FSH-induced rat granulosa cell steroidogenesis. Endocrinology. 2013 Feb;154(2):956-67. doi: 10.1210/en.2012-1836. Epub 2012 Dec 18.
9 Metformin and epothilone A treatment up regulate pro-apoptotic PARP-1, Casp-3 and H2AX genes and decrease of AKT kinase level to control cell death of human hepatocellular carcinoma and ovary adenocarcinoma cells. Toxicol In Vitro. 2018 Mar;47:48-62. doi: 10.1016/j.tiv.2017.11.001. Epub 2017 Nov 5.