Drug intelligence / Profile preview

esketamine + ticlopidine

Development stage
Unknown
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral, Intranasal
01

Overview

Esketamine + ticlopidine refers to the concomitant administration of **esketamine**, the S-enantiomer of ketamine primarily used in treatment-resistant depression, together with **ticlopidine**, an antiplatelet agent acting as a CYP2B6 inhibitor. This combination is not marketed as a fixed-dose product, but the interaction has been studied for its pharmacokinetic effects. Esketamine acts as a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist, producing rapid antidepressant effects by modulating glutamatergic neurotransmission in the brain[6]. Ticlopidine primarily inhibits adenosine diphosphate (ADP)-mediated platelet aggregation via antagonism of the P2Y12 receptor. When administered with esketamine, ticlopidine increases esketamine plasma exposure (AUC) by inhibiting the CYP2B6 enzyme responsible for its metabolism, but this increase is not considered clinically significant and does not require esketamine dose adjustment[1][2][5]. No therapeutic indication exists specifically for this combination; the interaction is relevant to pharmacokinetic safety and dose considerations in clinical practice.

02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)P2Y12 (Purinergic P2Y12 receptor)

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