Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTE4BSY)

• DTT Name: Bromodomain and extraterminal domain protein (BET)
• Synonyms: Bromodomain and Extra Terminal protein
• Gene Name: BET
• DTT Type: Clinical trial target; [1]
• UniProt ID: NOUNIPROTAC
• TTD ID: T58998
• KEGG Pathway: SNARE interactions in vesicular transport (hsa04130)
• Reactome Pathway: COPII (Coat Protein 2) Mediated Vesicle Transport (R-HSA-204005)

Molecular Interaction Atlas (MIA) of This DTT

21 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CPI-0610	DMPXOYJ	Myelofibrosis	2A20.2	Phase 3	[1]
ZEN-3694	DM6VQTF	Prostate cancer	2C82.0	Phase 2	[2]
BMS-986158	DM6LDI4	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[1]
INCB054329	DM7TZL0	Refractory hematologic malignancy	2A85.5	Phase 1/2	[3]
INCB057643	DMG65CV	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[4]
ODM-207	DMOKVJD	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[5]
OTX-015	DMI8RG1	Acute myeloid leukaemia	2A60	Phase 1/2	[1]
(+)-JQ1	DM1CZSJ	Testicular cancer	2C80	Phase 1	[6]
BAY 1238097	DMYPU8V	Neoplasm	2A00-2F9Z	Phase 1	[7]
BI 894999	DM7W5N2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]
CC-90010	DMKH3Z9	Astrocytoma	2A00.0Y	Phase 1	[1]
CC-95775	DMJCIGN	Non-hodgkin lymphoma	2B33.5	Phase 1	[8]
FT-1101	DMZOAT3	Haematological malignancy	2B33.Y	Phase 1	[1]
GS-5829	DMZVFOQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]
GSK2820151	DMU1X8K	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
GSK525762	DMPAWBN	Haematological malignancy	2B33.Y	Phase 1	[1]
Mivebresib	DMCPF90	Acute myeloid leukaemia	2A60	Phase 1	[1]
PLX51107	DMXLHVW	Haematological malignancy	2B33.Y	Phase 1	[1]
RG6146	DMIHC4R	Haematological malignancy	2B33.Y	Phase 1	[1]
RO6870810	DM7H6XI	Multiple myeloma	2A83	Phase 1	[10]
ZEN003694	DM72GZV	Prostate cancer	2C82.0	Phase 1	[2]

37 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dihydropyrido pyrazinone compound 1	DM8S7NQ	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 1	DM5CXQT	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 10	DMAYKZ9	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 11	DM1G8SM	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 12	DMVA8KL	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 13	DM7OBVT	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 14	DMS3CDT	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 15	DMPXK1C	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 16	DM614F8	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 17	DM2SUCK	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 18	DME8CQA	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 19	DM01FD3	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 2	DMYLR2S	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 3	DMWMRKJ	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 4	DMNI0PH	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 5	DMT46PS	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 6	DMKSNZG	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 7	DM3T840	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 8	DM3IV7K	N. A.	N. A.	Patented	[11]
Isoxazole-based bicyclic compound 9	DMWA7RB	N. A.	N. A.	Patented	[11]
PMID26924192-Compound-50	DMTVZWM	N. A.	N. A.	Patented	[11]
PMID26924192-Compound-51	DMB2MH3	N. A.	N. A.	Patented	[11]
PMID26924192-Compound-52	DMFU6JR	N. A.	N. A.	Patented	[11]
PMID26924192-Compound-53	DMFN1AR	N. A.	N. A.	Patented	[11]
PMID26924192-Compound-54	DMODT8F	N. A.	N. A.	Patented	[11]
PMID26924192-Compound-55	DMGWQVT	N. A.	N. A.	Patented	[11]
PMID26924192-Compound-56	DM6YGLT	N. A.	N. A.	Patented	[11]
PMID26924192-Compound-57	DM3NXP8	N. A.	N. A.	Patented	[11]
Pyrimido-indole derivative 1	DMB5UF7	N. A.	N. A.	Patented	[11]
Pyrimido-indole derivative 2	DM3REN5	N. A.	N. A.	Patented	[11]
Pyrimido-indole derivative 3	DM53LGD	N. A.	N. A.	Patented	[11]
Quinazolinone derivative 3	DMDRIZF	N. A.	N. A.	Patented	[11]
Quinazolinone derivative 4	DM8WH97	N. A.	N. A.	Patented	[11]
Quinazolinone derivative 5	DMXOKH3	N. A.	N. A.	Patented	[11]
Tetra-hydro-quinoline derivative 2	DMEKO71	N. A.	N. A.	Patented	[11]
Tetra-hydro-quinoline derivative 3	DMAWY4L	N. A.	N. A.	Patented	[11]
Tetra-hydro-quinoline derivative 4	DMMC3AG	N. A.	N. A.	Patented	[11]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] Clinical pipeline report, company report or official report of Zenith Epigenetics.
• [3] The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies. Clin Cancer Res. 2019 Jan 1;25(1):300-311.
• [4] Development of 2 Bromodomain and Extraterminal Inhibitors With Distinct Pharmacokinetic and Pharmacodynamic Profiles for the Treatment of Advanced Malignancies. Clin Cancer Res. 2020 Mar 15;26(6):1247-1257.
• [5] First-in-human Phase 1 open label study of the BET inhibitor ODM-207 in patients with selected solid tumours. Br J Cancer. 2020 Dec;123(12):1730-1736.
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma. Br J Haematol. 2017 Sep;178(6):936-948.
• [8] Clinical pipeline report, company report or official report of Bristol-Myers Squibb.
• [9] ClinicalTrials.gov (NCT02630251) Dose Escalation Study of GSK2820151 in Subjects With Advanced or Recurrent Solid Tumors. U.S. National Institutes of Health.
• [10] A Phase 1 study of RO6870810, a novel bromodomain and extra-terminal protein inhibitor, in patients with NUT carcinoma, other solid tumours, or diffuse large B-cell lymphoma. Br J Cancer. 2021 Feb;124(4):744-753.
• [11] BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.