Seletracetam
UCB 44212 (CAS 357336-74-4)
Seletracetam is a potent investigational racetam and SV2A ligand with N-type Ca2+ channel blocking activity, intended for epilepsy but never marketed. Structurally related to levetiracetam and brivaracetam, it showed robust preclinical anticonvulsant effects and advanced to Phase II clinical trials.
Also known as:
Formula
C₁₀H₁₄F₂N₂O
Category
Racetam / Anticonvulsant
Molar Mass
216.23 g/mol
Legal Status
AU S4; research only US/EU
Chemical Profile
Mechanism of Action
Seletracetam acts as a potent, high-affinity ligand at synaptic vesicle glycoprotein 2A (SV2A)—tenfold higher affinity than levetiracetam—and selectively inhibits N-type Ca2+ channels, reducing pathologic neuronal hyperexcitation and seizure spread in models of acquired and genetic epilepsy.
Preclinical and Early Clinical Evidence
Potent SV2A Target Engagement, Ca2+ Channel Inhibition, Seizure Control
Seletracetam shows robust anti-seizure efficacy in acquired/genetic animal and in vitro epilepsy models, with favorable tolerability and linear PK. It suppresses spike-and-wave discharges and is highly active in kindled and audiogenic seizure models. Phase I/II studies: mild, CNS-predominant side effects.
Safety & Side Effects
In healthy volunteers, seletracetam was well tolerated at a wide oral dose range. Mild-to-moderate, transient CNS effects (dizziness, euphoria, somnolence) most common; low risk of serious toxicity in animals/early clinical.
Regulatory & Legal Status
Australia / US / Intl.
- AU: S4 prescription only
- Not FDA/EMA approved, not marketed globally
- Research/academic use only
Note: Not marketed anywhere as of 2024; research only.
History
Developed by UCB Pharma in the 2000s as a high-potency successor to levetiracetam. Phase II trials showed efficacy but were discontinued in favor of brivaracetam. Remains a research reference for SV2A/N-type Ca2+ mediated seizure control.
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Benefits
- SV2A ligand—10x affinity of levetiracetam
- N-type Ca2+ channel inhibition
- Robust anti-epileptic effect in animal models
Considerations
- Not approved or marketed
- Best data: animal, Phase I/II volunteers
- Not for human clinical use
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Scientific References
- Matagne, A., et al. "Profile of the new pyrrolidone derivative seletracetam (UCB 44212) in animal models of epilepsy." Eur J Pharmacol, vol. 614, 2009, pp. 30–37. https://doi.org/10.1016/j.ejphar.2009.04.024.
- Bennett, B., et al. "Seletracetam (UCB 44212)." Neurotherapeutics, vol. 4, no. 1, 2007, pp. 117–122. https://doi.org/10.1016/j.nurt.2006.11.014.
- Pollard, J.R. "Seletracetam, a small molecule SV2A modulator for the treatment of epilepsy." Curr Opin Investig Drugs, vol. 9, no. 1, 2008, pp. 101–107.
- "Seletracetam." PubChem Compound Summary, NCBI, CID 9856063, 2024. https://pubchem.ncbi.nlm.nih.gov/compound/9856063
For research/education only. Not for human or supplement use. Last updated: 4/12/2025.