Drug intelligence / Profile preview

fimepinostat + venetoclax + rituximab

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

Overview

**Fimepinostat + venetoclax + rituximab** is a three-drug investigational combination used primarily in early-phase clinical trials for hematologic malignancies, particularly high-grade B-cell lymphomas such as diffuse large B-cell lymphoma (DLBCL) or high-grade B-cell lymphoma (HGBL) with dual MYC and BCL2 alterations. Fimepinostat is a dual inhibitor of histone deacetylase (HDAC) and phosphoinositide 3-kinase (PI3K), disrupting transcription and proliferation. Venetoclax is a selective small molecule inhibitor of B-cell lymphoma 2 (BCL2), promoting apoptosis of malignant cells. Rituximab is a monoclonal antibody targeting CD20 on B lymphocytes, mediating cell death via immune effector mechanisms. The primary action of this triple combination is to synergistically induce apoptosis and disrupt growth signals in malignant B cells, leveraging distinct and complementary mechanisms. This combination is currently being tested in clinical trials and is not approved for routine clinical use[2][5].

Other names
fimepinostat + venetoclax + rituximab
02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)BCL-2 (BCL-2 family)CD20 (B-lymphocyte antigen CD20)HDAC (HDAC family)

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