Drug intelligence / Profile preview

vadimezan + fluvoxamine

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

vadimezan + fluvoxamine is a pharmacological combination consisting of the vascular disrupting agent (VDA) and STING agonist vadimezan (also known as DMXAA or ASA404) and the selective serotonin reuptake inhibitor (SSRI) and Sigma-1 receptor (S1R) agonist fluvoxamine. Vadimezan was originally developed as a tumor-vascular disrupting agent that induces cytokine production and was later identified as a potent agonist of the murine Stimulator of Interferon Genes (STING) protein, though it lacks significant activity against the human STING variant. Fluvoxamine is an approved antidepressant that also acts as a high-affinity agonist for the Sigma-1 receptor, an endoplasmic reticulum-resident chaperone protein. This specific combination is primarily utilized in preclinical research to investigate the cross-talk between S1R and the STING pathway; specifically, studies have demonstrated that S1R activation by fluvoxamine can suppress STING-mediated induction of type I interferons and pro-inflammatory cytokines, suggesting a potential therapeutic strategy for STING-associated autoinflammatory diseases. While the individual components have undergone extensive clinical testing, the combination itself is not currently part of a formal clinical development program.

Brand names
Favarin
Other names
5,6-dimethylxanthenone-4-acetic acidfluvoxamine maleate
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)SERT (Sodium-dependent serotonin transporter)

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