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Probucol and Cilostazol
This combination of probucol (an antioxidant lipid-lowering agent) and cilostazol (a phosphodiesterase-3 inhibitor with antiplatelet and vasodilatory properties) works synergistically to reduce lipid oxidation, improve blood flow, and inhibit platelet aggregation.
This combination of probucol (an antioxidant lipid-lowering agent) and cilostazol (a phosphodiesterase-3 inhibitor with antiplatelet and vasodilatory properties) works synergistically to reduce lipid oxidation, improve blood flow, and inhibit platelet aggregation. Used for Hyperlipidemia and atherosclerotic cardiovascular disease, Peripheral arterial disease.
At a glance
| Generic name | Probucol and Cilostazol |
|---|---|
| Sponsor | Otsuka Beijing Research Institute |
| Drug class | Antioxidant/lipid-lowering agent combined with phosphodiesterase-3 inhibitor |
| Target | Probucol: lipid peroxidation inhibitor; Cilostazol: phosphodiesterase-3 (PDE-3) |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
Mechanism of action
Probucol acts as a potent antioxidant that reduces LDL cholesterol oxidation and improves HDL cholesterol levels, while cilostazol inhibits phosphodiesterase-3 to increase cAMP levels in platelets and vascular smooth muscle, resulting in antiplatelet effects, vasodilation, and improved blood viscosity. Together, they address multiple pathways in atherosclerotic cardiovascular disease and peripheral arterial disease.
Approved indications
- Hyperlipidemia and atherosclerotic cardiovascular disease
- Peripheral arterial disease
Common side effects
- Headache
- Diarrhea
- Palpitations
- Dizziness
- Tachycardia
Key clinical trials
- To Compare the Effect of Concomitant Administration of Probucol and Cilostazol With Probucol Single Treatment on the Atherosclerosis Related Markers (Including the Thickness of the Achilles Tendon) and Evaluate Safety (Based on Atorvastatin Treatment) in Severe Hypercholesterolemia Subject (PHASE4)
- Study of Cilostazol and Probucol to Assess Their Effects on Atherosclerosis Related Biomarker (PHASE4)
- Evaluation of Concomitant Administration of Cilostazol and Probucol on Biomarkers, Endothelial Function and Safety (PHASE2)
- Safety and Pharmacokinetics of Probucol and Cilostazol (PHASE4)
- Effect of Probucol and/or Cilostazol on Mean IMT in Patients With Coronary Heart dIsease (PHASE4)
- PreventIon of IMT Progression in iSchemic Stroke Patients With High Risk of Cerebral HemOrrhage-IMT Study (PHASE4)
- PreventIon of CArdiovascular Events in iSchemic Stroke Patients With High Risk of Cerebral HemOrrhage (PHASE4)
- A Clinical Study to Evaluate the Efficacy and Safety of Cilostazol and Probucol in Combination on Patients With Diabetic Nephropathy (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Probucol and Cilostazol CI brief — competitive landscape report
- Probucol and Cilostazol updates RSS · CI watch RSS
- Otsuka Beijing Research Institute portfolio CI