Details of the Drug Combination

General Information of Drug Combination (ID: DCYIX8I)

• Drug Combination Name: C646 + AG-881
• Indication: Diffuse intrinsic pontine glioma; Status: Investigative [1]
• Component Drugs:
  C646 (DMCOQKH): Small molecular drug
  AG-881 (DMIE1WY): N.A.
• High-throughput Screening Result:
  Testing Cell Line: DIPG25
  Zero Interaction Potency (ZIP) Score: 21.402
  Bliss Independence Score: 32.127
  Loewe Additivity Score: 4.854
  LHighest Single Agent (HSA) Score: 1.653

Molecular Interaction Atlas of This Drug Combination

Indication(s) of C646

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[2]

C646 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Histone acetyltransferase KAT6B (KAT6B)	TTH4VJL	KAT6B_HUMAN	Inhibitor	[5]

Indication(s) of AG-881

Disease Entry	ICD 11	Status	REF
Glioma	2A00.0	Phase 3	[3]
Acute myeloid leukaemia	2A60	Phase 1	[4]

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	[4]

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] Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases. Drug Discov Today. 2014 May;19(5):654-60.
• [3] 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.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol. 2010 May 28;17(5):471-82.