Drug intelligence / Profile preview

DF-006

Development stage
Phase 1
Lead developer
Drug Farm
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

DF-006 is a first-in-class, orally administered small molecule prodrug and serum-stable derivative of ADP-heptose that acts as an agonist of alpha-kinase 1 (ALPK1), a pattern recognition receptor involved in innate immunity. Upon oral administration, DF-006 is rapidly converted to its active form (DF-006A) in target tissues such as the liver. Activation of ALPK1 by DF-006 leads to phosphorylation of TIFA and subsequent activation of the NF-kB pathway, stimulating local innate immune responses and inflammation. Preclinical studies have demonstrated potent anti-hepatitis B virus (HBV) efficacy in mouse models and primary human hepatocytes, with significant reductions in HBV DNA, hepatitis B surface antigen (HBsAg), and hepatitis B e antigen (HBeAg). In clinical trials, DF-006 has shown safety and tolerability at various doses in both healthy volunteers and patients with chronic hepatitis B infection. The drug is being developed primarily for chronic hepatitis B but has also been investigated for hepatocellular carcinoma[1][2][3][4][5][7][9].

02

Targets

ALPK1 (Alpha-protein kinase 1)NF-κB

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