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Comparator: niacin + laropiprant
Niacin raises HDL cholesterol and lowers triglycerides, while laropiprant blocks the prostaglandin D2 receptor to reduce niacin-induced flushing.
Niacin raises HDL cholesterol and lowers triglycerides, while laropiprant blocks the prostaglandin D2 receptor to reduce niacin-induced flushing. Used for Dyslipidemia in patients at risk for cardiovascular disease.
At a glance
| Generic name | Comparator: niacin + laropiprant |
|---|---|
| Also known as | MK0524A |
| Sponsor | Merck Sharp & Dohme LLC |
| Drug class | Lipid-modifying agent combination |
| Target | Niacin: GPR109A (hydroxycarboxylic acid receptor 2); Laropiprant: DP1 (prostaglandin D2 receptor) |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | Phase 3 |
Mechanism of action
Niacin (vitamin B3) is a lipid-modifying agent that increases HDL cholesterol and decreases triglycerides and LDL cholesterol through multiple pathways including reduced hepatic VLDL production. Laropiprant is a selective antagonist of the prostaglandin D2 receptor (DP1), which mediates the vasodilatory flushing response that limits niacin tolerability. The combination allows higher niacin doses with improved tolerability.
Approved indications
- Dyslipidemia in patients at risk for cardiovascular disease
Common side effects
- Flushing
- Pruritus
- Gastrointestinal upset
- Hyperuricemia
- Hepatotoxicity
Key clinical trials
- A Study to Evaluate the Effects of Extended Release (ER) Niacin/Laropiprant, Laropiprant, ER Niacin, and Placebo on Urinary Prostanoid Metabolites in Subjects With High Cholesterol (0524A-075)(COMPLETED) (PHASE1)
- MK-0524B Lipid Study (MK-0524B-063) (PHASE3)
- MK0524A Clinical Efficacy Study (0524A-026)(COMPLETED) (PHASE2)
- Lipid Efficacy Study (0524B-022)(COMPLETED) (PHASE3)
- An Investigational Drug Study Evaluating a Novel Approach to Treat Dyslipidemia (0524A-032) (PHASE2)
- A Study to Evaluate the Effects of Laropiprant on the Antiplatelet Effects of Clopidogrel and Aspirin in Combination (MK-0524A-114)(COMPLETED) (PHASE1)
- Extended Niacin/Laropiprant in Patients With Type 2 Diabetes (0524A-069) (PHASE3)
- Carotid IMT (Intima Media Thickening) Study (0524A-041)(TERMINATED) (PHASE3)
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 |