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Lapaquistat acetate and atorvastatin
Lapaquistat acetate and atorvastatin is a ACAT2 inhibitor + HMG-CoA reductase inhibitor (statin combination) Small molecule drug developed by Takeda. It is currently in Phase 3 development for Hypercholesterolemia / dyslipidemia (in combination therapy). Also known as: Lapaquistat acetate, Lipitor, TAK-475, Lapaquistat.
Lapaquistat acetate inhibits ACAT2 (acyl-CoA:cholesterol acyltransferase 2) to reduce intestinal cholesterol absorption, while atorvastatin inhibits HMG-CoA reductase to reduce hepatic cholesterol synthesis.
Lapaquistat acetate inhibits ACAT2 (acyl-CoA:cholesterol acyltransferase 2) to reduce intestinal cholesterol absorption, while atorvastatin inhibits HMG-CoA reductase to reduce hepatic cholesterol synthesis. Used for Hypercholesterolemia / dyslipidemia (in combination therapy).
At a glance
| Generic name | Lapaquistat acetate and atorvastatin |
|---|---|
| Also known as | Lapaquistat acetate, Lipitor, TAK-475, Lapaquistat, TAK475 |
| Sponsor | Takeda |
| Drug class | ACAT2 inhibitor + HMG-CoA reductase inhibitor (statin combination) |
| Target | ACAT2 (acyl-CoA:cholesterol acyltransferase 2) 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 the intestinal enzyme ACAT2, which is responsible for cholesterol esterification and absorption in the gut, thereby reducing dietary cholesterol uptake. Atorvastatin simultaneously inhibits HMG-CoA reductase in the liver, the rate-limiting enzyme in endogenous cholesterol synthesis. Together, these complementary mechanisms provide dual reduction of both exogenous and endogenous cholesterol pathways.
Approved indications
- Hypercholesterolemia / dyslipidemia (in combination therapy)
Common side effects
- Elevated liver transaminases
- Muscle-related adverse events (myalgia, myopathy)
- Gastrointestinal effects
Key clinical trials
- Efficacy of Lapaquistat Acetate Co-Administered With Statins in Subjects With Hypercholesterolemia (PHASE3)
- Safety and Efficacy of Lapaquistat Acetate Taken Alone and With Atorvastatin in Subjects With Primary Dyslipidemia (PHASE3)
- Efficacy of Lapaquistat Acetate in Subjects Currently Treated With Lipid-Lowering Therapy. (PHASE3)
- Safety of Lapaquistat Acetate in Subjects With Hypercholesterolemia (PHASE3)
- Efficacy of Lapaquistat Acetate Alone or Combined With High-Dose Statin Therapy in Subjects With Hypercholesterolemia (PHASE3)
- Efficacy and Safety of Lapaquistat Acetate Coadministered With Atorvastatin in Subjects With Hypercholesterolemia (PHASE2)
- Efficacy of Lapaquistat Acetate and Atorvastatin on Blood Cholesterol Levels in Subjects With Primary 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 atorvastatin CI brief — competitive landscape report
- Lapaquistat acetate and atorvastatin updates RSS · CI watch RSS
- Takeda portfolio CI
Frequently asked questions about Lapaquistat acetate and atorvastatin
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Related
- Drug class: All ACAT2 inhibitor + HMG-CoA reductase inhibitor (statin combination) drugs
- Target: All drugs targeting ACAT2 (acyl-CoA:cholesterol acyltransferase 2) and HMG-CoA reductase
- Manufacturer: Takeda — full pipeline
- Therapeutic area: All drugs in Cardiovascular
- Indication: Drugs for Hypercholesterolemia / dyslipidemia (in combination therapy)
- Also known as: Lapaquistat acetate, Lipitor, TAK-475, Lapaquistat, TAK475
- Compare: Lapaquistat acetate and atorvastatin vs similar drugs
- Pricing: Lapaquistat acetate and atorvastatin cost, discount & access