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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).
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|Molibresib||I-BET762|GSK525762||BET Inhibitor (Pan) 27||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, PMID: 30906568, PMID: 32328561).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|ARID1A dec exp||ovarian clear cell carcinoma||predicted - sensitive||Molibresib||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|
|Unknown unknown||NUT midline carcinoma||not applicable||Molibresib||Phase Ib/II||Actionable||In a Phase I/II trial, Molibresib (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...|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status|
|NCT01943851||Phase I||Molibresib||A Dose Escalation Study to Investigate the Safety, Pharmacokinetics (PK), Pharmacodynamics (PD) and Clinical Activity of GSK525762 in Subjects With Relapsed, Refractory Hematologic Malignancies||Completed|
|NCT01587703||Phase I||Molibresib||A Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics, and Clinical Activity of GSK525762 in Subjects With NUT Midline Carcinoma (NMC) and Other Cancers||Completed|