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Lapaquistat acetate and simvastatin
Lapaquistat acetate inhibits ACAT (acyl-CoA:cholesterol acyltransferase) to reduce cholesterol absorption, while simvastatin inhibits HMG-CoA reductase to decrease cholesterol synthesis, providing dual lipid-lowering effects.
Lapaquistat acetate inhibits ACAT (acyl-CoA:cholesterol acyltransferase) to reduce cholesterol absorption, while simvastatin inhibits HMG-CoA reductase to decrease cholesterol synthesis, providing dual lipid-lowering effects. Used for Hypercholesterolemia / dyslipidemia (LDL cholesterol reduction).
At a glance
| Generic name | Lapaquistat acetate and simvastatin |
|---|---|
| Also known as | TAK-475, Zocor, Lapaquistat |
| Sponsor | Takeda |
| Drug class | ACAT inhibitor + HMG-CoA reductase inhibitor (statin combination) |
| Target | ACAT (acyl-CoA:cholesterol acyltransferase) and HMG-CoA reductase |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | Phase 3 |
Mechanism of action
This combination targets two key steps in cholesterol metabolism. Lapaquistat acetate blocks ACAT, an enzyme that esterifies cholesterol in the intestine, reducing dietary cholesterol absorption. Simvastatin simultaneously inhibits HMG-CoA reductase in the liver, suppressing endogenous cholesterol synthesis. Together, these complementary mechanisms produce additive reductions in LDL cholesterol and total cholesterol levels.
Approved indications
- Hypercholesterolemia / dyslipidemia (LDL cholesterol reduction)
Common side effects
- Elevated liver transaminases
- Myalgia
- Gastrointestinal disturbances
- Headache
Key clinical trials
- Efficacy of Lapaquistat Acetate Co-Administered With Statins in Subjects With Hypercholesterolemia (PHASE3)
- Efficacy of Lapaquistat Acetate in Subjects Currently Treated With Lipid-Lowering Therapy. (PHASE3)
- Efficacy of Lapaquistat Acetate Alone or Combined With Simvastatin in Subjects With Hypercholesterolemia (PHASE3)
- Efficacy of Lapaquistat Acetate and Simvastatin in Subjects With Primary Dyslipidemia. (PHASE3)
- Efficacy of Lapaquistat Acetate Alone or Combined With High-Dose Statin Therapy in Subjects With Hypercholesterolemia (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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Lapaquistat acetate and simvastatin CI brief — competitive landscape report
- Lapaquistat acetate and simvastatin updates RSS · CI watch RSS
- Takeda portfolio CI