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

General Information of DTT (ID: TT9MZCQ)

• DTT Name: Enhancer of zeste homolog 2 (EZH2) DTT Info
• Gene Name: EZH2

Molecule-Related Drug & Molecule List

1 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tazemetostat	DMWP1BH	Follicular lymphoma	2A80	Approved	[1]

8 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DS-3201b	DMI69E5	T-cell leukaemia	2A90	Phase 2	[2]
CPI-0209	DMJEXLI	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[3]
CPI-1205	DM3XWJ8	Prostate cancer	2C82.0	Phase 1/2	[4]
SHR2554	DMMUCH0	Prostate cancer	2C82.0	Phase 1/2	[5]
DS-3201	DMRLPFG	Acute lymphoblastic leukaemia	2A85	Phase 1	[4]
GSK2816126	DMJDVW4	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
HH2853	DMQIE58	Non-hodgkin lymphoma	2B33.5	Phase 1	[7]
PF-06821497	DML3WT6	Diffuse large B-cell lymphoma	2A81	Phase 1	[8]

49 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID26882240-Compound-1	DMPAE8N	N. A.	N. A.	Patented	[9]
PMID28394193-Compound-12	DMA7H9T	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-13	DMGZ9MW	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-14	DM6T2FM	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-15	DMXMP92	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-16	DMQDRUT	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-17	DMPR9GA	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-18	DMIBZ2H	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-19	DM4ZAE8	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-20	DMC5NR0	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-21	DMLD8K3	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-22	DM8PJ3F	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-23	DMNHCMY	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-24	DMYCVWZ	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-25	DMPIXAO	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-26	DMNWCUJ	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-27	DM2KVDH	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-28	DMC24OL	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-29	DMBVI7L	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-30	DMGEZT8	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-31	DMJ02N1	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-32	DM628MP	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-33	DMEOHX2	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-34	DMB7WNP	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-36	DM658HJ	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-37	DM73CA5	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-38	DM25PMQ	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-39	DM2NS5T	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-40	DMO5479	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-41	DMYLVTQ	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-42	DMLI7TG	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-43	DMASV8I	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-44	DME6FWY	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-45	DMZJXPF	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-46	DMYMPNA	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-47	DM7UDIM	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-49	DMEU4Y1	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-50	DM4NVTB	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-51	DM0KPQ9	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-52	DM2I9HY	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-53	DMXMRQP	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-54	DMMQ3UG	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-55	DM2FPHZ	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-56	DMQRFZK	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-57	DM4Y3US	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-Figure3bI	DMXK2GA	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-Figure3bII	DML6PE0	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-Figure3bIII	DMUI385	N. A.	N. A.	Patented	[10]
PMID28394193-Compound-Figure5aVIII	DMKVRTM	N. A.	N. A.	Patented	[10]

1 #N/A Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
#N/A	DMV1AGC	N. A.	N. A.	#N/A	[10]

5 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
EI1	DMBQCMU	Discovery agent	N.A.	Investigative	[11]
EPZ005687	DMYISTE	Discovery agent	N.A.	Investigative	[12]
GSK343	DM9QU5Y	Discovery agent	N.A.	Investigative	[13]
MS1943	DMTPGQ3	Breast cancer	2C60-2C65	Investigative	[5]
UNC1999	DMOPCBD	Discovery agent	N.A.	Investigative	[14]

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [2] Development of new agents for peripheral T-cell lymphoma. Expert Opin Biol Ther. 2019 Mar;19(3):197-209.
• [3] ClinicalTrials.gov (NCT04104776) A Study of CPI-0209 in Patients With Advanced Tumors. U.S. National Institutes of Health.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286.
• [6] National Cancer Institute Drug Dictionary (drug id 756211).
• [7] Clinical pipeline report, company report or official report of HaiHe Biopharma.
• [8] 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.
• [9] Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2011-2015).Expert Opin Ther Pat. 2016;26(3):309-22.
• [10] EZH2 inhibitors: a patent review (2014-2016).Expert Opin Ther Pat. 2017 Jul;27(7):797-813.
• [11] Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5.
• [12] A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012 Nov;8(11):890-6.
• [13] Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6.
• [14] An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34.