Therapy Detail

Therapy Name GSK525762
Therapy Description

Molibresib (GSK525762) is a JQ1 derivative which binds to the bromodomain of BET proteins preventing their interaction with acetylated histone peptides, thus disrupting chromatin remodeling, gene expression, and cell proliferation (PMID: 24015967).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
GSK525762 Molibresib I-BET762 BET Inhibitor (Pan) 25 Molibresib (GSK525762) is a JQ1 derivative which binds to the bromodomain of BET proteins preventing their interaction with acetylated histone peptides, thus disrupting chromatin remodeling, gene expression, and cell proliferation (PMID: 24015967).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown NUT midline carcinoma not applicable GSK525762 Phase Ib/II Actionable In a Phase I/II trial, GSK525762 treatment resulted in partial response in 20% (2/10) and stable disease in 40% (4/10) of NUT midline carcinoma patients (Cancer Res 2016;76(14 Suppl): Abstract nr CT014). detail...
ARID1A dec exp ovarian clear cell carcinoma predicted - sensitive GSK525762 Preclinical - Cell culture Actionable In a preclinical study, knockdown of ARID1A resulted in increased sensitivity to Molibresib (GSK525762) in ovarian clear cell carcinoma cell lines in culture (PMID: 29760405). 29760405
Clinical Trial Phase Therapies Title Recruitment Status
NCT01943851 Phase I GSK525762 A Dose Escalation Study to Investigate the Safety, Pharmacokinetics (PK), Pharmacodynamics (PD) and Clinical Activity of GSK525762 in Subjects With Relapsed, Refractory Hematologic Malignancies Recruiting
NCT01587703 Phase I GSK525762 A Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics, and Clinical Activity of GSK525762 in Subjects With NUT Midline Carcinoma (NMC) and Other Cancers Active, not recruiting