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Therapy Name | Molibresib |
Synonyms | |
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, PMID: 30906568, PMID: 32328561). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Molibresib | I-BET762|GSK525762|GSK-525762|GSK 525762 | BET Inhibitor (Pan) 32 | 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 |
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Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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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 | USA | NLD | GBR | FRA | ESP | AUS | 1 |
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 | USA | GBR | ESP | AUS | 1 |