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temozolomide + trotabresib
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Temozolomide + trotabresib is an investigational combination therapy for the treatment of glioblastoma and other high-grade gliomas. Temozolomide is an oral alkylating agent that induces DNA damage in tumor cells, while trotabresib (CC-90010, BMS-986378) is a potent oral small molecule inhibitor of bromodomain and extraterminal (BET) proteins. BET proteins regulate gene expression involved in cancer cell proliferation and survival; inhibition leads to antitumor activity. Trotabresib has demonstrated the ability to penetrate the blood–brain barrier and engage its target within brain tumor tissue. The combination aims to enhance antitumor efficacy by targeting both DNA integrity (temozolomide) and epigenetic regulation (trotabresib). Clinical trials have evaluated this regimen with or without radiotherapy in newly diagnosed glioblastoma patients[2][3][4][5].
- Brand names
- trotabresib
- Other names
- temozolomide + CC-90010temozolomide + BMS-986378
02
Targets
BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)DNABRD4 (Bromodomain-containing protein 4)BRDT (Bromodomain testis-specific protein)
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