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RO6870810 + venetoclax
- Development stage
- Phase 1
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Subcutaneous, Oral
01
Overview
RO6870810 + venetoclax is a combination therapy investigated primarily for the treatment of relapsed/refractory diffuse large B-cell lymphoma (DLBCL). **RO6870810** is a novel, small-molecule, non-covalent inhibitor of the bromodomain and extra-terminal (BET) family of proteins, which act as epigenetic readers and regulate transcription of oncogenic drivers such as MYC, BCL2, and E2F. **Venetoclax** is a selective, orally available small molecule antagonist of B-cell lymphoma 2 (BCL-2) protein, leading to apoptosis in cancer cells dependent on BCL-2 for survival. This combination disrupts oncogenic transcriptional programs and simultaneously induces apoptosis through BCL-2 inhibition. RO6870810 is administered subcutaneously for 14 days of a 21-day cycle, while venetoclax is given orally once daily. Clinical studies have shown manageable safety and preliminary antitumor activity in heavily pretreated DLBCL patients[3][5][1].
- Other names
- RO-6870810 + venetoclaxRO + venetoclax
02
Targets
BCL-2 (BCL-2 family)BRD4 (Bromodomain-containing protein 4)
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