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eprenetapopt + venetoclax + rituximab

Development stage
Unknown
Lead developer
Aprea Therapeutics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

**eprenetapopt + venetoclax + rituximab** is a combination therapy studied primarily for relapsed or refractory hematologic malignancies, particularly chronic lymphocytic leukemia (CLL) and other lymphoid cancers. - **Eprenetapopt (APR-246, PRIMA-1MET)** is a small molecule that restores the normal function of mutant p53 protein, inducing cancer cell apoptosis. - **Venetoclax (ABT-199, Venclexta)** is a small molecule inhibitor of B-cell lymphoma-2 (BCL-2), promoting programmed cell death in malignant lymphocytes. - **Rituximab (IDEC-C2B8, Rituxan)** is a monoclonal antibody targeting CD20 on B cells, leading to immune-mediated B cell depletion. This combination aims to synergistically induce apoptosis in malignant B cells by targeting different apoptotic pathways and surface antigens. Eprenetapopt is being developed by Aprea Therapeutics, venetoclax by AbbVie/Genentech, and rituximab by Roche/Genentech/Biogen. The combination is under clinical investigation, and current development in the US is on *clinical hold* due to pending data and safety review by the FDA. In at least one reported CLL patient treated with this combination, a complete remission was achieved[2][7].

Other names
APR-246 + ABT-199 + IDEC-C2B8
02

Targets

TP53 (Cellular Tumor Antigen p53 R175H)BCL-2 (BCL-2 family)CD20 (B-lymphocyte antigen CD20)

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