Drug intelligence / Profile preview

diABZI

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Intranasal, Endotracheal, Intravenous (preclinical/in Vivo), Unspecified Experimental / Research
01

Overview

diABZI is a **potent non-nucleotide small molecule STING agonist** from the amidobenzimidazole (ABZI) family, engineered as a dimeric ligand to exploit the symmetrical nature of the STING protein for enhanced activation[1][3][5][11]. It binds and activates the STING pathway, leading to phosphorylation and dimerization of STING, activation of TBK1 and IRF3, and subsequent induction of **type-I interferons**, pro-inflammatory cytokines (including IFN-α, IFN-β, CXCL10, IL-6, TNF-α), and NF-κB/IRF3-dependent signaling[1][4][5]. diABZI promotes antitumor immunity, suppresses tumor growth (as shown in vivo in colorectal cancer models), and has demonstrated efficacy in antiviral models (notably SARS-CoV-2), both in vitro and in vivo[1][4][5][14]. It also overcomes NRF2-driven therapy resistance in cancers (like melanoma) and synergizes with BRAF inhibitors to prevent tumor proliferation and migration[4][12]. diABZI shows improved physicochemical and pharmacokinetic properties compared to classical STING agonists (e.g., cyclic dinucleotides such as cGAMP), with water solubility and increased systemic bioavailability[1]. It is primarily being investigated for oncology and anti-viral indications.

Brand names
diABZI
Other names
diABZI (compound 3)diABZI STING agonist-1 trihydrochlorideDiamidobenzimidazole STING Agonist-1STING agonist diABZISTING agonist 3
02

Targets

STING (Stimulator of interferon genes protein)

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