Drug intelligence / Profile preview

cilostazol + donepezil

Development stage
Preclinical
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral
01

Overview

Cilostazol + donepezil is a combination therapy consisting of two small molecule drugs, cilostazol and donepezil. Donepezil is an acetylcholinesterase inhibitor that increases acetylcholine levels in the brain, thereby enhancing cholinergic neurotransmission and improving cognitive function in Alzheimer's disease. Cilostazol is a phosphodiesterase III inhibitor primarily used for its vasodilatory and antiplatelet effects; it acts by inhibiting PDE3 in vascular smooth muscle cells, leading to increased cAMP levels and vasodilation. The rationale for combining these agents lies in their complementary mechanisms—donepezil targets neurodegenerative aspects by enhancing cholinergic signaling, while cilostazol addresses vascular contributions to dementia by improving cerebral blood flow. This combination has been investigated as an add-on therapy to slow cognitive decline in patients with mild-to-moderate Alzheimer's disease or other dementias[1][2].

02

Targets

ABCG2 (Breast cancer resistance protein)PDE3A (Phosphodiesterase 3A)ABCB1 (P-glycoprotein)Acetylcholinesterase

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