Drug intelligence / Profile preview

RO6870810 + venetoclax + rituximab

Development stage
Preclinical
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Subcutaneous, Intravenous, Oral
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Overview

RO6870810 + venetoclax + rituximab is a combination of three drugs under investigation primarily for hematologic malignancies: - **RO6870810** is a small molecule BET (bromodomain and extra-terminal motif) inhibitor that disrupts transcription of oncogenes such as MYC by inhibiting BET family proteins (BRD2, BRD3, BRD4, BRDT), thereby modulating epigenetic control and reducing abnormal proliferation in cancer cells. - **Venetoclax** is an orally administered small molecule inhibitor targeting BCL-2, an anti-apoptotic protein, to restore apoptosis in cancer cells, particularly those of lymphoid origin. - **Rituximab** is a monoclonal antibody directed against CD20, a surface antigen found on B lymphocytes, leading to cell lysis via immune-mediated mechanisms. This combination is designed to synergistically induce apoptosis, modulate key oncogenic pathways, and facilitate B-cell depletion in aggressive B-cell malignancies such as diffuse large B-cell lymphoma (DLBCL). The combination is not an approved regimen but is of current research interest.

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Targets

BCL-2 (BCL-2 family)CD20 (B-lymphocyte antigen CD20)BRD4 (Bromodomain-containing protein 4)BRDT (Bromodomain testis-specific protein)BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)

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