Drug intelligence / Profile preview

quetiapine + topiramate

Development stage
Phase 4
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Quetiapine + topiramate is a combination of two pharmaceutical agents, quetiapine and topiramate, used together primarily in research and off-label clinical settings. Quetiapine is an atypical antipsychotic that acts mainly as an antagonist at dopamine D2 and serotonin 5-HT2A receptors, with additional activity at histamine H1, adrenergic α1, and muscarinic M1 receptors. It is approved for the treatment of schizophrenia, bipolar disorder (including manic and depressive episodes), and as adjunct therapy for major depressive disorder[6]. Topiramate is an anticonvulsant that modulates voltage-dependent sodium channels, enhances GABAergic activity at GABA-A receptors, antagonizes AMPA/kainate glutamate receptors, inhibits carbonic anhydrase isoenzymes, and blocks L-type calcium channels[4][3]. The combination has been studied for potential synergistic effects in conditions such as substance use disorders (e.g., cocaine addiction), mood disorders including bipolar disorder with comorbidities like binge eating or substance abuse[5][3][7]. However, this combination can have additive side effects due to pharmacokinetic interactions—topiramate induces CYP3A4 (the main enzyme metabolizing quetiapine), potentially lowering plasma levels of quetiapine; dose adjustments may be necessary[1][3].

02

Targets

iGluR (Ionotropic receptor 76b (Ir76b))ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)GABRR (GABA-A receptor subunit rho)HRH1 (Histamine H1 Receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2A (Serotonin receptor 5-HT2A)NaV (Voltage-gated sodium channels)CA5A (Carbonic anhydrase VA)LTCC (Voltage-gated calcium channel (L-type))M1 (Muscarinic acetylcholine receptor M1)NET (Norepinephrine Transporter)

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