Details of the Drug Combination

General Information of Drug Combination (ID: DC8PGIS)

Drug Combination Name
Abexinostat AG-881
Indication
Disease Entry Status REF
Diffuse intrinsic pontine glioma Investigative [1]
Component Drugs Abexinostat   DM91LGU AG-881   DMIE1WY
Small molecular drug N.A.
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: DIPG25
Zero Interaction Potency (ZIP) Score: 17.452
Bliss Independence Score: 18.311
Loewe Additivity Score: 18.515
LHighest Single Agent (HSA) Score: 12.28

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Abexinostat
Disease Entry ICD 11 Status REF
Follicular lymphoma 2A80 Phase 3 [2]
Renal cell carcinoma 2C90 Phase 3 [3]
Acute myeloid leukaemia 2A60 Phase 2 [2]
Breast cancer 2C60-2C65 Phase 2 [2]
Diffuse large B-cell lymphoma 2A81 Phase 2 [2]
Gynecologic cancer 2F33-2F76 Phase 2 [2]
Peripheral T-cell lymphoma 2A90.C Phase 2 [2]
Solid tumour/cancer 2A00-2F9Z Phase 2 [2]
Abexinostat Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Histone deacetylase (HDAC) TTBH0VX NOUNIPROTAC Modulator [6]
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Abexinostat Interacts with 15 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 [5]
Growth arrest and DNA damage-inducible protein GADD45 gamma (GADD45G) OT8V1J4M GA45G_HUMAN Increases Expression [7]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [5]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Increases Expression [5]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [7]
C-C motif chemokine 3 (CCL3) OTW2H3ND CCL3_HUMAN Decreases Expression [5]
Nuclear factor NF-kappa-B p105 subunit (NFKB1) OTNRRD8I NFKB1_HUMAN Decreases Expression [5]
Heme oxygenase 2 (HMOX2) OTG40XBT HMOX2_HUMAN Decreases Expression [5]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Increases Expression [5]
Breast cancer type 2 susceptibility protein (BRCA2) OTF1XSV1 BRCA2_HUMAN Decreases Expression [7]
Caspase-9 (CASP9) OTD4RFFG CASP9_HUMAN Increases Cleavage [5]
C-C motif chemokine 7 (CCL7) OTDIS99H CCL7_HUMAN Decreases Expression [5]
Transcription factor RelB (RELB) OTU3QYEF RELB_HUMAN Decreases Expression [5]
DNA repair protein RAD51 homolog 1 (RAD51) OTNVWGC1 RAD51_HUMAN Decreases Expression [7]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Increases Cleavage [5]
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⏷ Show the Full List of 15 DOT(s)
Indication(s) of AG-881
Disease Entry ICD 11 Status REF
Glioma 2A00.0 Phase 3 [4]
Acute myeloid leukaemia 2A60 Phase 1 [2]
AG-881 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Isocitrate dehydrogenase (IDH) TTDTWV0 IDHC_HUMAN; IDHP_HUMAN; IDH3A_HUMAN; IDH3B_HUMAN; IDH3G_HUMAN Inhibitor [2]
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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 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 ClinicalTrials.gov (NCT03592472) A Study of Pazopanib With or Without Abexinostat in Patients With Locally Advanced or Metastatic Renal Cell Carcinoma (RENAVIV). U.S. National Institutes of Health.
4 ClinicalTrials.gov (NCT04164901) Study of Vorasidenib (AG-881) in Participants With Residual or Recurrent Grade 2 Glioma With an IDH1 or IDH2 Mutation (INDIGO). U.S. National Institutes of Health.
5 PCI-24781 induces caspase and reactive oxygen species-dependent apoptosis through NF-kappaB mechanisms and is synergistic with bortezomib in lymphoma cells. Clin Cancer Res. 2009 May 15;15(10):3354-65. doi: 10.1158/1078-0432.CCR-08-2365. Epub 2009 May 5.
6 Phase 1 study of the oral histone deacetylase inhibitor abexinostat in patients with Hodgkin lymphoma, non-Hodgkin lymphoma, or chronic lymphocytic leukaemia. Invest New Drugs. 2015 Apr;33(2):423-31.
7 HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19482-7. doi: 10.1073/pnas.0707828104. Epub 2007 Nov 27.