Drug intelligence / Profile preview

cilostazol + sertraline

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Cilostazol + sertraline is a combination of two small molecule drugs used together, primarily investigated for the treatment of major depressive disorder (MDD). Cilostazol is a phosphodiesterase-3 (PDE3) inhibitor with antiplatelet and vasodilatory properties, traditionally used for intermittent claudication and secondary stroke prevention. Sertraline is a selective serotonin reuptake inhibitor (SSRI) widely prescribed as an antidepressant. The combination has been studied in clinical trials for its potential to enhance antidepressant efficacy; cilostazol may provide neuroprotective effects and augment the response to sertraline in MDD patients. Both agents act via distinct mechanisms—cilostazol by increasing intracellular cAMP through PDE3 inhibition, leading to vasodilation and reduced platelet aggregation, while sertraline increases synaptic serotonin levels by inhibiting its reuptake at presynaptic neurons[1][4][3].

02

Targets

PDE3B (Phosphodiesterase 3B)PDE3A (Phosphodiesterase 3A)SERT (Sodium-dependent serotonin transporter)

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