Details of the Drug Combination

General Information of Drug Combination (ID: DCRKG08)

• Drug Combination Name: PAC1 + BIIB-021
• Indication: Glioblastoma; Status: Investigative [1]
• Component Drugs:
  PAC1 (DMYQUIP): Small molecular drug
  BIIB-021 (DMPAJ41): Small molecular drug
• High-throughput Screening Result:
  Testing Cell Line: JHH-136
  Zero Interaction Potency (ZIP) Score: 56.535
  Bliss Independence Score: 50.945
  Loewe Additivity Score: 1.177
  LHighest Single Agent (HSA) Score: 5.348

Molecular Interaction Atlas of This Drug Combination

Indication(s) of PAC1

Disease Entry	ICD 11	Status	REF
Anaplastic astrocytoma	2A00.0	Phase 1	[2]
Recurrent glioblastoma	2A00.00	Phase 1	[2]

PAC1 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Caspase-3 (CASP3)	TTPF2QI	CASP3_HUMAN	Activator	[4]

Indication(s) of BIIB-021

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 2	[3]

BIIB-021 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Heat shock protein 90 alpha (HSP90A)	TT78R5H	HS90A_HUMAN	Inhibitor	[5]

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 (NCT00618319) An Open-Label, 18FDG-PET Pharmacodynamic Assessment of the Effect of BIIB021 in Subjects With Gastrointestinal Stromal Tumors (GIST). U.S. National Institutes of Health.
• [4] Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50.
• [5] BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol Cancer Ther. 2009 Apr;8(4):921-9.