Ezobresib

Ezobresib
Clinical data
Other names	BMS-986158
Identifiers
	IUPAC name 2-[3-(3,5-dimethyltriazol-4-yl)-5-[(S)-oxan-4-yl(phenyl)methyl]pyrido[3,2-b]indol-7-yl]propan-2-ol;
CAS Number	1800340-40-2;
PubChem CID	118196485;
DrugBank	DB15435;
ChemSpider	58828664;
UNII	X8BW0MQ5PI;
KEGG	D12710;
ChEMBL	ChEMBL4297458;
Chemical and physical data
Formula	C30H33N5O2
Molar mass	495.627 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(N(N=N1)C)C2=CC3=C(C4=C(N3[C@@H](C5CCOCC5)C6=CC=CC=C6)C=C(C=C4)C(C)(C)O)N=C2;
	InChI InChI=InChI=1S/C30H33N5O2/c1-19-28(34(4)33-32-19)22-16-26-27(31-18-22)24-11-10-23(30(2,3)36)17-25(24)35(26)29(20-8-6-5-7-9-20)21-12-14-37-15-13-21/h5-11,16-18,21,29,36H,12-15H2,1-4H3/t29-/m1/s1; Key:KGERZPVQIRYWRK-GDLZYMKVSA-N;

Ezobresib is an investigational new drug that has been evaluated for the treatment of cancer. It inhibits Bromodomain and Extra-Terminal domain (BET) proteins, with potential antineoplastic activity.^[1] Developed by Bristol Myers Squibb, this therapeutic agent has been studied for its efficacy in treating various cancers, including solid tumors and hematological malignancies.^[2] Despite showing promise in early-phase clinical trials, recent developments suggest that Bristol Myers Squibb has decided to discontinue further development of ezobresib.^[3]

References

↑ Ma Z, Zhang C, Bolinger AA, Zhou J (October 2024). "An updated patent review of BRD4 degraders". Expert Opinion on Therapeutic Patents. 34 (10): 929–951. doi:10.1080/13543776.2024.2400166. PMC 11427152. PMID 39219068.
↑ "Clinical Trials Using Ezobresib". National Cancer Institute.
↑ Brown A. "Bristol backs out of BET inhibition". ApexOnco.

[pmid39219068-1] Ma Z, Zhang C, Bolinger AA, Zhou J (October 2024). "An updated patent review of BRD4 degraders". Expert Opinion on Therapeutic Patents. 34 (10): 929–951. doi:10.1080/13543776.2024.2400166. PMC 11427152. PMID 39219068.

[2] "Clinical Trials Using Ezobresib". National Cancer Institute.

[3] Brown A. "Bristol backs out of BET inhibition". ApexOnco.

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