Betrixaban activates cGAS and ERVs to promote dual nucleic-sensing antiviral immunity

Broad-spectrum host-directed antivirals are urgently needed, as virus-targeted drugs often suffer from narrow specificity and rapid resistance. Here, we reported that Betrixaban (BT), an FDA-approved oral Factor Xa inhibitor, induced a robust antiviral state through dual innate immune pathways. Mechanistically, we identified BT as the first small molecule to directly bind and activate the DNA sensor cGAS to induce cGAMP production. Concurrently, BT inhibited histone deacetylases (HDACs), leading to chromatin de-repression of endogenous retroviruses (ERVs) and production of immunostimulatory double-stranded RNA (dsRNA) that engaged RIG-I/MDA5. These combined signal cascades triggered strong type I interferon responses and conferred broad-spectrum antiviral protection against RNA and DNA viruses in vitro and in vivo. These findings unveil a unique host-directed antiviral strategy wherein a small-molecule drug engages dual nucleic acid-sensing pathway, and suggest repurposing BT as an orally broad-spectrum antiviral.

Authors

Publication Details

Journal
EMBO Molecular Medicine
Published
2026-03-23
DOI
https://doi.org/10.1038/s44321-025-00356-7
Primary Topic
interferon and immune responses
Type
article
Field-Weighted Citation Impact
0.00
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article

Betrixaban activates cGAS and ERVs to promote dual nucleic-sensing antiviral immunity

Yang Zhao, Xingyu Chen, Yunfei Xie, Haocheng Wang et al.
EMBO Molecular Medicine
interferon and immune responses
article

Betrixaban activates cGAS and ERVs to promote dual nucleic-sensing antiviral immunity

Yang Zhao, Xingyu Chen, Yunfei Xie, Haocheng Wang, Xuefei Guo, Tianyi Liu, Xiao Renshaw Wang, Fuping You
article en

Abstract

Broad-spectrum host-directed antivirals are urgently needed, as virus-targeted drugs often suffer from narrow specificity and rapid resistance. Here, we reported that Betrixaban (BT), an FDA-approved oral Factor Xa inhibitor, induced a robust antiviral state through dual innate immune pathways. Mechanistically, we identified BT as the first small molecule to directly bind and activate the DNA sensor cGAS to induce cGAMP production. Concurrently, BT inhibited histone deacetylases (HDACs), leading to chromatin de-repression of endogenous retroviruses (ERVs) and production of immunostimulatory double-stranded RNA (dsRNA) that engaged RIG-I/MDA5. These combined signal cascades triggered strong type I interferon responses and conferred broad-spectrum antiviral protection against RNA and DNA viruses in vitro and in vivo. These findings unveil a unique host-directed antiviral strategy wherein a small-molecule drug engages dual nucleic acid-sensing pathway, and suggest repurposing BT as an orally broad-spectrum antiviral.

EMBO Molecular Medicine
Good health and well-being
Openalex Percentile: Top 11%
interferon and immune responses
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