Details of the Drug Combination

General Information of Drug Combination (ID: DCB5LYJ)

• Drug Combination Name: PFK-158 + Metyrosine
• Indication: Chronic myelogenous leukemia; Status: Investigative [1]
• Component Drugs:
  PFK-158 (DMIR21F): N.A.
  Metyrosine (DMBYCU0): Small molecular drug
• High-throughput Screening Result:
  Testing Cell Line: KBM-7
  Zero Interaction Potency (ZIP) Score: 14.39
  Bliss Independence Score: 14.39
  Loewe Additivity Score: 17.3
  LHighest Single Agent (HSA) Score: 17.31

Molecular Interaction Atlas of This Drug Combination

Indication(s) of PFK-158

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

PFK-158 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Renal carcinoma antigen NY-REN-56 (PFKFB3)	TTTHMQJ	F263_HUMAN	Inhibitor	[4]

Indication(s) of Metyrosine

Disease Entry	ICD 11	Status	REF
Pheochromocytoma	5A75	Approved	[3]

Metyrosine Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Tyrosine 3-monooxygenase (TH)	TTUHP71	TY3H_HUMAN	Binder	[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] ClinicalTrials.gov (NCT02044861) Phase 1 Safety Study of ACT-PFK-158, 2HCl in Patients With Advanced Solid Malignancies. U.S. National Institutes of Health.
• [3] 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: 6956).
• [4] Discovery of a PFKFB3 inhibitor for phase I trial testing that synergizes with the B-Raf inhibitor vemurafenib. Cancer Metab. 2014; 2(Suppl 1): P14.
• [5] Dopamine beta-hydroxylase deficiency. A genetic disorder of cardiovascular regulation. Hypertension. 1991 Jul;18(1):1-8.