Birabresib

also known as OTX015 · MK-8628 · OTX-015 ANHYDROUS · Y-803 anhydrous

Small molecule targets BRD2, BRD3, BRD4 via inhibition

Developed for: acute myeloid leukemia · castration-resistant prostate carcinoma · diffuse large B-cell lymphoma · nut midline carcinoma · triple-negative breast carcinoma · acute lymphoblastic leukemia · glioblastoma · lung cancer
+3 more
· non-small cell lung carcinoma · pancreatic ductal adenocarcinoma · plasma cell myeloma
Investigated by: Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA) · Merck Sharp & Dohme LLC

Trials 6

today NCT02698189 · Ph 1 NCT02698176 · Ph 1 NCT02303782 · Ph 1/2 NCT02296476 · Ph 2 NCT02259114 · Ph 1 NCT01713582 · Ph 1

201320142015201620172018201920202021202220232024202520262027

Phase	Registry id	Dates	Indication	Sponsor	Status	Outcome
Phase 14 trials
Phase 1	NCT02698189	May 2016 → Jan 2018	acute myeloid leukemia, diffuse large B-cell lymphoma	Merck Sharp & Dohme LLC	Terminated	No outcome recorded
Phase 1	NCT02698176	May 2016 → Apr 2017	castration-resistant prostate carcinoma, non-small cell lung carcinoma, nut midline carcinoma, triple-negative breast carcinoma	Merck Sharp & Dohme LLC	Terminated	No outcome recorded
Phase 1	NCT02259114	Oct 2014 → Mar 2017	castration-resistant prostate carcinoma, lung cancer, nut midline carcinoma, pancreatic ductal adenocarcinoma +1	Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)	Completed	No outcome recorded
Phase 1	NCT01713582	Dec 2012 → Jan 2017	acute lymphoblastic leukemia, acute myeloid leukemia, diffuse large B-cell lymphoma, plasma cell myeloma	Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)	Completed	No outcome recorded
Phase 1/21 trial
Phase 1/2	NCT02303782	Jan 2015 → Mar 2016	acute myeloid leukemia	Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)	Withdrawn	No outcome recorded
Phase 21 trial
Phase 2	NCT02296476	Oct 2014 → Oct 2015	glioblastoma	Oncoethix GmbH, a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)	Terminated	No outcome recorded

Evidence & citations 11 cited values

Every value below carries the sentence it was read from. 9 sources stand behind the page.

Field	Value	Cited text
Known as	Birabresib	“The primary purpose of this study was to determine the recommended dose (RD) of birabresib (MK-8628) /OTX015 for further phase II studies, in participants with acute leukemia...” NCT01713582 ↗ 4 NCT02259114 ↗ NCT02698189 ↗ NCT02698176 ↗ NCT02296476 ↗
Known as	MK-8628	ChEMBL registry synonym — accepted as the source's own label CHEMBL3581647 ↗
Known as	OTX-015 ANHYDROUS	ChEMBL registry synonym — accepted as the source's own label CHEMBL3581647 ↗
Known as	OTX015	ClinicalTrials.gov intervention name — accepted as the source's own label NCT02303782 ↗ 1 NCT01713582 ↗
Known as	Y-803 anhydrous	ChEMBL registry synonym — accepted as the source's own label CHEMBL3581647 ↗
Action	Inhibit	“OTX015 (MK-8628) specifically binds to BRD2, BRD3, and BRD4, preventing BET proteins from binding to the chromatin, thus inhibiting gene transcription.” PMID 27063977 ↗ Mar 2016
Modality	Small molecule	“The first-in-class small molecule inhibitor OTX015 (MK-8628)” PMID 27063978 ↗ Mar 2016
Route	Oral	“Birabresib 10, 20 and/or 40 mg oral capsules” NCT02259114 ↗
Target	BRD2	“OTX015 (MK-8628) specifically binds to BRD2, BRD3, and BRD4, preventing BET proteins from binding to the chromatin, thus inhibiting gene transcription.” PMID 27063977 ↗ Mar 2016
Target	BRD3	“OTX015 (MK-8628) specifically binds to BRD2, BRD3, and BRD4, preventing BET proteins from binding to the chromatin, thus inhibiting gene transcription.” PMID 27063977 ↗ Mar 2016
Target	BRD4	“OTX015 (MK-8628) specifically binds to BRD2, BRD3, and BRD4, preventing BET proteins from binding to the chromatin, thus inhibiting gene transcription.” PMID 27063977 ↗ Mar 2016