Drug intelligence / Profile preview

GNTBM-38

Development stage
Preclinical
Lead developer
GNT Biotech & Medicals
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

GNTBM-38 is a novel, orally administered small molecule drug developed by Great Novel Therapeutics Biotech & Medicals Corp. It acts as a selective class I histone deacetylase (HDAC) inhibitor, specifically targeting HDAC1, HDAC2, and HDAC3. Distinguished from other epigenetic drugs by its dual mechanism of action, GNTBM-38 combines epigenetic regulation of gene expression with immune activation properties. This enables it to remodel the tumor microenvironment (TME), converting immunologically "cold" tumors into "hot" tumors that are more susceptible to immune attack. Mechanistically, it enhances tumor antigen presentation, increases infiltration of activated CD8+ T cells into tumors, induces memory T cell persistence, and inhibits the mobilization of immunosuppressive cells such as TAMs (tumor-associated macrophages), Tregs (regulatory T cells), and MDSCs (myeloid-derived suppressor cells). Preclinical studies have demonstrated significant anti-cancer activity both as monotherapy for hematological malignancies and in combination with tyrosine kinase inhibitors or immune checkpoint inhibitors for solid tumors such as colorectal cancer and metastatic breast cancer[1][2][3][7].

02

Targets

HDAC1 (Histone Deacetylase 1)

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