Details of the Drug-Related molecule(s) Expression 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(s) Related to This Drug

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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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Histone-lysine N-methyltransferase (HLNM)	DTT	DOT1L	2.406	1.585	1.848	2.138

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Acute myeloid leukaemia

ICD Disease Classification

2A60

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Histone-lysine N-methyltransferase (HLNM)	DTT	DOT1L	7.62E-02	0.08	0.2

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

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.