Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMN2FS3)

Drug Name

EPZ-5676 Drug Info

Synonyms

pinometostat; EPZ-5676; 1380288-87-8; EPZ5676; UNII-8V9YR09EF3; UNII-F66X4M38G5; 8V9YR09EF3; CHEMBL3087499; CHEMBL3414626; F66X4M38G5; 1380288-88-9; (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol; Pinometostat, trans-; 5'-[{cis-3-[2-(5-Tert-Butyl-1h-Benzimidazol-2-Yl)ethyl]cyclobutyl}(Propan-2-Yl)amino]-5'-Deoxyadenosine

Indication

Disease Entry	ICD 11	Status	REF
Acute myeloid leukaemia	2A60	Phase 1/2	[1]
Acute lymphoblastic leukaemia	2A85	Phase 1	[2]
Acute lymphocytic leukaemia	2B33.3	Phase 1	[3]

Cross-matching ID

PubChem CID: 57345410
ChEBI ID: CHEBI:124919
CAS Number: CAS 1380288-87-8
TTD Drug ID: DMN2FS3

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Investigative Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Histone-lysine N-methyltransferase (HLNM)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
EPZ-004777	DMLN4V5	leukaemia	2A60-2B33	Investigative	[5]
bromo-deaza-SAH	DMX2U7G	Discovery agent	N.A.	Investigative	[6]
SGC0946	DMP35VS	Discovery agent	N.A.	Investigative	[7]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histone-lysine N-methyltransferase (HLNM)	TTSZ8T1	DOT1L_HUMAN	Modulator	[4]

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References

1	ClinicalTrials.gov (NCT03701295) Pinometostat and Azacitidine in Treating Patients With Relapsed, Refractory, or Newly Diagnosed Acute Myeloid Leukemia With 11q23 Rearrangement. U.S. National Institutes of Health.
2	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Blood. 2013 August 8; 122(6): 1017-1025.
5	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: 7377).
6	Bromo-deaza-SAH: a potent and selective DOT1L inhibitor. Bioorg Med Chem. 2013 Apr 1;21(7):1787-94.
7	Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288.