General Information of Drug (ID: DMTNQB0)

Drug Name
CC-486 Drug Info
Synonyms
AG-14361; AG14361; 328543-09-5; UNII-48N0U0K50I; AG 14361; CHEMBL65892; 48N0U0K50I; Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-; AG-014361; 1-(4-((dimethylamino)methyl)phenyl)-8,9-dihydro-2,7,9a-triazabenzo[cd]azulen-6(7H)-one; Imidazo(4,5,1-jk)(1,4)benzodiazepin-7(4H)-one, 2-(4-((dimethylamino)methyl)phenyl)-5,6-dihydro-; 2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one; SMR000486393; MLS006011157; MLS001065917; Nucleoside analogue
Indication
Disease Entry ICD 11 Status REF
Acute myeloid leukaemia 2A60 Phase 3 [1]
Myelodysplastic syndrome 2A37 Phase 3 [2]
Diffuse large B-cell lymphoma 2A81 Phase 1 [1]
Cross-matching ID
PubChem CID
9840076
ChEBI ID
CHEBI:92015
CAS Number
CAS 328543-09-5
TTD Drug ID
DMTNQB0

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
DNA [cytosine-5]-methyltransferase 1 (DNMT1) TT6S2FE DNMT1_HUMAN Inhibitor [3]
Poly [ADP-ribose] polymerase 1 (PARP1) TTVDSZ0 PARP1_HUMAN Inhibitor [4]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Poly [ADP-ribose] polymerase 1 (PARP1) DTT PARP1 7.871 7.105 7.62 7.33
DNA [cytosine-5]-methyltransferase 1 (DNMT1) DTT DNMT1 6.508 6.687 6.296 6.565
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
Poly [ADP-ribose] polymerase 1 (PARP1) DTT PARP1 1.62E-122 0.77 3
DNA [cytosine-5]-methyltransferase 1 (DNMT1) DTT DNMT1 1.56E-81 0.73 2.22
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 J Clin Oncol 33, 2015 (suppl, abstr TPS7097).
3 Efficacy and safety of extended dosing schedules of CC-486 (oral azacitidine) in patients with lower-risk myelodysplastic syndromes. Leukemia. 2016 Apr;30(4):889-96.
4 Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J Med Chem. 2003 Jan 16;46(2):210-3.