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

General Information of Drug (ID: DMI69E5)

Drug Name
DS-3201b Drug Info
Synonyms
Valemetostat; 1809336-39-7; UNII-60RD0234VE; 60RD0234VE; 1809336-39-7 (free base); DS-3201; (2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide; Valemetostat 2HCl; Valemetostat [INN]; Valemetostat (DS-3201); CHEMBL4597193; EZH1/2 inhibitor DS-3201; SCHEMBL18393626; SCHEMBL18393627; SCHEMBL18639210; EX-A3423; DS3201; NSC813381; s8926; NSC-813381; HY-109108; CS-0039740; D11551
Indication
Disease Entry ICD 11 Status REF
T-cell leukaemia 2A90 Phase 2 [1]
Small-cell lung cancer 2C25.Y Phase 1/2 [2]
Acute lymphoblastic leukaemia 2A85 Phase 1 [3]
Acute myeloid leukaemia 2A60 Phase 1 [3]
Renal cell carcinoma 2C90 Phase 1 [4]
Urothelial carcinoma 2C92.0 Phase 1 [4]
Cross-matching ID
PubChem CID
126481870
CAS Number
CAS 1809336-39-7
TTD Drug ID
DMI69E5

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Approved Drug(s)
Patented Agent(s)
Download the Complete Related Drug List
Drug(s) Targeting Enhancer of zeste homolog 1 (EZH1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
DS-3201 DMRLPFG Acute lymphoblastic leukaemia 2A85 Phase 1 [6]
HH2853 DMQIE58 Non-hodgkin lymphoma 2B33.5 Phase 1 [7]
GSK343 DM9QU5Y Discovery agent N.A. Investigative [8]
Drug(s) Targeting Enhancer of zeste homolog 2 (EZH2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tazemetostat DMWP1BH Follicular lymphoma 2A80 Approved [9]
CPI-1205 DM3XWJ8 Prostate cancer 2C82.0 Phase 1/2 [6]
SHR2554 DMMUCH0 Prostate cancer 2C82.0 Phase 1/2 [10]
CPI-0209 DMJEXLI Solid tumour/cancer 2A00-2F9Z Phase 1/2 [11]
DS-3201 DMRLPFG Acute lymphoblastic leukaemia 2A85 Phase 1 [6]
HH2853 DMQIE58 Non-hodgkin lymphoma 2B33.5 Phase 1 [7]
GSK2816126 DMJDVW4 Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
PF-06821497 DML3WT6 Diffuse large B-cell lymphoma 2A81 Phase 1 [13]
PMID28394193-Compound-56 DMQRFZK N. A. N. A. Patented [14]
PMID28394193-Compound-46 DMYMPNA N. A. N. A. Patented [14]
⏷ Show the Full List of 10 Drug(s)

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
Enhancer of zeste homolog 1 (EZH1) TTNJA0C EZH1_HUMAN Inhibitor [5]
Enhancer of zeste homolog 2 (EZH2) TT9MZCQ EZH2_HUMAN Inhibitor [5]

References

1 ClinicalTrials.gov (NCT04102150) Valemetostat Tosylate (DS-3201b) Phase 2 Study in Relapsed or Refractory Adult T-cell Leukemia/Lymphoma. U.S. National Institutes of Health.
2 ClinicalTrials.gov (NCT03879798) DS-3201b and Irinotecan for Patients With Recurrent Small Cell Lung Cancer. U.S. National Institutes of Health.
3 ClinicalTrials.gov (NCT03110354) DS-3201b for Acute Myelogenous Leukemia (AML) or Acute Lymphocytic Leukemia (ALL). U.S. National Institutes of Health.
4 ClinicalTrials.gov (NCT04388852) DS3201 and Ipilimumab for the Treatment of Metastatic Prostate, Urothelial and Renal Cell Cancers. U.S. National Institutes of Health.
5 Development of new agents for peripheral T-cell lymphoma. Expert Opin Biol Ther. 2019 Mar;19(3):197-209.
6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7 Clinical pipeline report, company report or official report of HaiHe Biopharma.
8 Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
10 Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286.
11 ClinicalTrials.gov (NCT04104776) A Study of CPI-0209 in Patients With Advanced Tumors. U.S. National Institutes of Health.
12 National Cancer Institute Drug Dictionary (drug id 756211).
13 Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497). J Med Chem. 2018 Feb 8;61(3):650-665.
14 EZH2 inhibitors: a patent review (2014-2016).Expert Opin Ther Pat. 2017 Jul;27(7):797-813.