Drug intelligence / Profile preview

fimepinostat + rituximab

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

Overview

**Fimepinostat + rituximab** is an investigational combination regimen evaluated in clinical trials for relapsed or refractory diffuse large B-cell lymphoma (DLBCL) and other lymphomas. \n- **Fimepinostat** is a synthetic, orally available small molecule that acts as a dual inhibitor of *histone deacetylase (HDAC, class I and II)* and *phosphatidylinositol 3-kinase (PI3K, α, β, and δ)* enzymes. It downregulates MYC protein and MYC-associated genes via HDAC and PI3K inhibition, showing activity in MYC-altered DLBCL[1][3][4][5]. \n- **Rituximab** is a chimeric monoclonal antibody targeting *CD20* on B lymphocytes, mediating B-cell lysis via mechanisms such as antibody-dependent cellular cytotoxicity, complement activation, and direct induction of apoptosis[5]. \nTogether, these agents are combined to exploit potential synergy in B-cell lymphomas, especially in relapsed/refractory settings or MYC-altered cases, with fimepinostat targeting tumor epigenetics and survival pathways, and rituximab targeting malignant B-cells directly[1][5]. \nPreclinical, Phase 1, and Phase 2 clinical data suggest activity for the combination, but the regimen is still under clinical investigation and is not yet approved for routine clinical use[1][3][5].

02

Targets

CD20 (B-lymphocyte antigen CD20)PIK3CA (Phosphoinositide 3-kinase alpha)HDAC10 (Histone Deacetylase 10)HDAC1 (Histone Deacetylase 1)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)

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