Details of the Drug Combination

General Information of Drug Combination (ID: DC6MNHW)

Drug Combination Name
Pelitinib Ispinesib
Indication
Disease Entry Status REF
Ewing sarcoma Investigative [1]
Component Drugs Pelitinib   DMIW453 Ispinesib   DMP2BWX
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: 39.786
Bliss Independence Score: 36.664
Loewe Additivity Score: 6.106
LHighest Single Agent (HSA) Score: 10.835

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Pelitinib
Disease Entry ICD 11 Status REF
Lymphoma 2A80-2A86 Phase 2 [2]
Pelitinib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Modulator [4]
------------------------------------------------------------------------------------
Pelitinib Interacts with 7 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [5]
B-cell lymphoma/leukemia 10 (BCL10) OT47MCLI BCL10_HUMAN Decreases Expression [5]
Cyclic AMP-dependent transcription factor ATF-1 (ATF1) OT251CI0 ATF1_HUMAN Decreases Expression [5]
B-cell lymphoma 3 protein (BCL3) OT1M5B95 BCL3_HUMAN Decreases Expression [5]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [5]
Baculoviral IAP repeat-containing protein 1 (NAIP) OTLA925F BIRC1_HUMAN Decreases Expression [5]
Baculoviral IAP repeat-containing protein 2 (BIRC2) OTFXFREP BIRC2_HUMAN Decreases Expression [5]
------------------------------------------------------------------------------------
⏷ Show the Full List of 7 DOT(s)
Indication(s) of Ispinesib
Disease Entry ICD 11 Status REF
Head and neck cancer 2D42 Phase 2 [3]
Ovarian cancer 2C73 Phase 2 [3]
Renal cell carcinoma 2C90 Phase 2 [3]
Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
Ispinesib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Kinesin-like protein KIF11 (KIF11) TTTRP0H KIF11_HUMAN Inhibitor [6]
------------------------------------------------------------------------------------

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: 7644).
3 ClinicalTrials.gov (NCT00095628) SB-715992 in Treating Patients With Recurrent or Metastatic Head and Neck Cancer. U.S. National Institutes of Health.
4 EGFR tyrosine kinase inhibitor pelitinib regulates radiation-induced p65-dependent telomerase activation in squamous cell carcinoma.Radiat Res.2013 Mar;179(3):304-12.
5 Irreversible EGFR inhibitor EKB-569 targets low-LET -radiation-triggered rel orchestration and potentiates cell death in squamous cell carcinoma. PLoS One. 2011;6(12):e29705. doi: 10.1371/journal.pone.0029705. Epub 2011 Dec 29.
6 Initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program. Pediatr Blood Cancer. 2009 Dec 15;53(7):1255-63.