Drug intelligence / Profile preview

citalopram + pipamperone

Development stage
Phase 3
Lead developer
PharmaNeuroBoost
Modality
Small Molecules
Administration
Oral
01

Overview

Citalopram + pipamperone is a fixed-dose combination of two drugs: citalopram, a selective serotonin reuptake inhibitor (SSRI) antidepressant, and low-dose pipamperone, an antipsychotic. The combination was developed to treat major depressive disorder. Citalopram works by inhibiting the reuptake of serotonin in the central nervous system, thereby increasing serotonergic activity. Pipamperone at low doses acts as a highly selective antagonist at serotonin 5-HT2A receptor and dopamine D4 receptor; it also has antagonistic effects on other receptors such as dopamine D2 and D3, and adrenergic α1/α2 receptors but with lower affinity. The rationale for this combination is that pipamperone may accelerate or augment the antidepressant effect of citalopram by blocking post-synaptic 5-HT2A receptor activation, which is thought to contribute to the delayed onset of SSRI efficacy[1][5][8]. Developed by PharmaNeuroBoost N.V., this drug reached phase 3 clinical trials for major depressive disorder but no recent development has been reported since 2015[1][3].

Other names
Pipamperone/citalopram
02

Targets

HTR2A (Serotonin receptor 5-HT2A)DRD2 (Dopamine D2 Receptor)DRD4 (Dopamine D4 Receptor)SERT allosteric site (Serotonin transporter allosteric site)SERT (Sodium-dependent serotonin transporter)

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