Details of the Drug Combination

General Information of Drug Combination (ID: DCKHUVA)

Drug Combination Name
Pelitinib Sapanisertib
Indication
Disease Entry Status REF
Hodgkin lymphoma Investigative [1]
Component Drugs Pelitinib   DMIW453 Sapanisertib   DMYZFNH
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: L-1236
Zero Interaction Potency (ZIP) Score: 7.81
Bliss Independence Score: 10.386
Loewe Additivity Score: 5.422
LHighest Single Agent (HSA) Score: 6.952

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 [5]
------------------------------------------------------------------------------------
Pelitinib Interacts with 14 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Inhibitor of nuclear factor kappa-B kinase subunit beta (IKBKB) OT9RDS3H IKKB_HUMAN Decreases Expression [6]
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [6]
B-cell lymphoma/leukemia 10 (BCL10) OT47MCLI BCL10_HUMAN Decreases Expression [6]
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Decreases Activity [7]
Transcription factor Sp1 (SP1) OTISPT4X SP1_HUMAN Decreases Activity [6]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [6]
Cyclic AMP-dependent transcription factor ATF-1 (ATF1) OT251CI0 ATF1_HUMAN Decreases Expression [6]
B-cell lymphoma 3 protein (BCL3) OT1M5B95 BCL3_HUMAN Decreases Expression [6]
NF-kappa-B inhibitor alpha (NFKBIA) OTFT924M IKBA_HUMAN Increases Expression [6]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Expression [6]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [6]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [6]
Baculoviral IAP repeat-containing protein 1 (NAIP) OTLA925F BIRC1_HUMAN Decreases Expression [6]
Baculoviral IAP repeat-containing protein 2 (BIRC2) OTFXFREP BIRC2_HUMAN Decreases Expression [6]
------------------------------------------------------------------------------------
⏷ Show the Full List of 14 DOT(s)
Indication(s) of Sapanisertib
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Phase 2 [3]
Coronavirus Disease 2019 (COVID-19) 1D6Y Investigative [4]
Sapanisertib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
HUMAN mammalian target of rapamycin (mTOR) TT7HQAF MTOR_HUMAN Inhibitor [4]
------------------------------------------------------------------------------------

References

1 Loss of function mutations in VARS encoding cytoplasmic valyl-tRNA synthetase cause microcephaly, seizures, and progressive cerebral atrophy.Hum Genet. 2018 Apr;137(4):293-303. doi: 10.1007/s00439-018-1882-3. Epub 2018 Apr 24.
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 (NCT02049957) Safety and Efficacy Study of Sapanisertib in Combination With Exemestane or Fulvestrant in Postmenopausal Women With Estrogen Receptor Positive/Human Epidermal Growth Factor Receptor 2 Negative (ER+/HER2-) Metastatic Breast Cancer. U.S. National Institutes of Health.
4 Prevent COVID-19 Severity by Repurposing mTOR Inhibitors. 2 April 2020
5 EGFR tyrosine kinase inhibitor pelitinib regulates radiation-induced p65-dependent telomerase activation in squamous cell carcinoma.Radiat Res.2013 Mar;179(3):304-12.
6 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.
7 Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. J Med Chem. 2011 Mar 10;54(5):1347-55. doi: 10.1021/jm101396q. Epub 2011 Feb 15.