Drug intelligence / Profile preview

cilostazol + rosuvastatin

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

Overview

Cilostazol + rosuvastatin is a combination drug comprised of cilostazol, a phosphodiesterase III inhibitor, and rosuvastatin, an HMG-CoA reductase inhibitor (statin). Cilostazol is primarily used for its antiplatelet, vasodilator, and anti-inflammatory properties, often in the management of peripheral arterial disease. Rosuvastatin is used to lower lipid levels and reduce cardiovascular risk by inhibiting cholesterol synthesis in the liver. The combination has been studied for synergistic anti-inflammatory and cytoprotective effects, including reduced TNF signaling and protection against kidney ischemia/reperfusion and cardiac injury in animal models. Mechanistically, cilostazol increases cyclic adenosine monophosphate (cAMP), activates protein kinase A, and upregulates endothelial nitric oxide synthase, while rosuvastatin suppresses cholesterol biosynthesis and upregulates nitric oxide synthase, thus enhancing endothelial function and reducing inflammatory responses. In combination, these drugs have shown improved anti-inflammatory efficacy and survival benefits compared to monotherapies in preclinical studies[1][4][6].

Brand names
Artostazol
Other names
cilostazol + rosuvastatinCilostazol/Rosuvastatin FDC
02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)NOS3 (eNOS)PDE3TNFA (Tumor necrosis factor alpha (soluble))

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