RESEARCH MONOGRAPH · KDC-MN-206
Fluvoxamine
Fluvoxamine (Luvox) is an SSRI with a structural backbone unlike the others in its class, developed by Solvay and approved in the US in 1994. It is a first-line drug for OCD and also useful in social anxiety. The pharmacological wrinkle that makes researchers care about it is high-affinity activation of the sigma-1 receptor, an unusual cellular target involved in stress response, neuroprotection, and possibly viral defense. That sigma-1 hook briefly made fluvoxamine a topic of pandemic-era research after small trials suggested it might reduce hospitalization risk in early COVID-19, although larger follow-up trials have been mixed. It also strongly blocks the liver enzyme CYP1A2, which raises blood levels of caffeine, theophylline, and several other common drugs. Not stocked by Kodiac. This monograph is provided for research and educational reference.
Intrigue 0–100 blends mechanism novelty, evidence strength, and translational potential. Kodiac editorial, not peer-reviewed.
Selective serotonin reuptake inhibitor / sigma-1 agonist
A monocyclic SSRI with notable sigma-1 receptor agonism; first-line for OCD and a pharmacological tool for sigma-1 research.
Abstract
Fluvoxamine (5-methoxy-1-[4-(trifluoromethyl)phenyl]pentan-1-one O-(2-aminoethyl)oxime; CAS 54739-18-3; molecular formula C15H21F3N2O2; molecular weight 318.34) is a monocyclic 2-aminoethyl oxime ether SSRI developed at Solvay, approved in Europe in 1983 and by the FDA in 1994 under the trade name Luvox. SERT affinity is approximately 2 nM; the structural class is distinct from the bicyclic SSRIs and produces a different selectivity profile, including high-affinity sigma-1 agonism (Ki approximately 36 nM). The sigma-1 component is unique among SSRIs and has been investigated for neuroprotective and anti-inflammatory applications, including the much-discussed COVID-19 trials in 2020 to 2021 where fluvoxamine reduced clinical deterioration in outpatients. Plasma half-life is 13 to 22 hours; hepatic metabolism via CYP2D6 and CYP1A2, with the compound itself being a potent CYP1A2 and CYP2C19 inhibitor and producing significant interactions with caffeine, theophylline, clozapine, and numerous other CYP1A2 substrates. Approved primarily for OCD; widely used off-label for social anxiety disorder. Used as the reference SSRI for sigma-1 receptor pharmacology studies.
Mechanism of action
SERT inhibition combined with high-affinity sigma-1 receptor agonism. Potent CYP1A2 inhibitor.
Reported research dose ranges
Reported research dose ranges in the literature.
References
- Hashimoto K. Sigma-1 receptor chaperone and brain-derived neurotrophic factor: emerging links between cardiovascular disease and depression. Prog Neurobiol 2013.
- Lenze EJ, et al. Fluvoxamine vs placebo and clinical deterioration in outpatients with symptomatic COVID-19. JAMA 2020.
- Wagner W, et al. Fluvoxamine. A review of its pharmacology and use in psychiatry. CNS Drugs 1994.
Read the full monograph
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The full reference document is provided strictly for research use only. It reports research dose ranges from the published literature, not instructions for use in humans or animals.
FOR RESEARCH USE ONLY. Not for medical, diagnostic, or therapeutic purposes. Not for human consumption. All information is provided for research and educational purposes only.