Drug intelligence / Profile preview

tucidinostat + tislelizumab

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

Overview

Tucidinostat + tislelizumab is an investigational combination regimen composed of tucidinostat, a selective oral histone deacetylase (HDAC) inhibitor (also known as chidamide), and tislelizumab, a monoclonal antibody immune checkpoint inhibitor against programmed cell death protein 1 (PD-1). Tucidinostat modifies the epigenetic landscape of cancer cells by inhibiting class I and class IIb HDACs, leading to altered gene expression, tumor cell cycle arrest, apoptosis, and immune modulation[1][2][4]. Tislelizumab binds PD-1 on T cells, preventing its interaction with PD-L1/PD-L2, thereby enhancing anti-tumor immune activity[1]. This combination is under clinical investigation for the treatment of advanced malignancies, notably locally advanced or metastatic urothelial carcinoma and non-small cell lung cancer. The rationale is to synergistically promote anti-tumor immunity by both direct HDAC-mediated epigenetic reprogramming and immune checkpoint blockade[1][3][5].

Other names
chidamide + tislelizumab
02

Targets

HDAC11 (Histone Deacetylase 11)PDCD1 (Programmed cell death protein 1 receptor)HDAC10 (Histone Deacetylase 10)HDAC1 (Histone Deacetylase 1)HDAC8 (Histone Deacetylase 8)

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