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Lapaquistat acetate and rosuvastatin
Lapaquistat acetate and rosuvastatin is a ACAT2 inhibitor combined with statin Small molecule drug developed by Takeda. It is currently in Phase 3 development for Hypercholesterolemia / elevated LDL cholesterol. Also known as: TAK-475, Crestor.
Lapaquistat acetate inhibits ACAT2 (acyl-CoA:cholesterol acyltransferase 2) to reduce intestinal cholesterol absorption, while rosuvastatin inhibits HMG-CoA reductase to reduce hepatic cholesterol synthesis.
Lapaquistat acetate inhibits ACAT2 (acyl-CoA:cholesterol acyltransferase 2) to reduce intestinal cholesterol absorption, while rosuvastatin inhibits HMG-CoA reductase to reduce hepatic cholesterol synthesis. Used for Hypercholesterolemia / elevated LDL cholesterol.
At a glance
| Generic name | Lapaquistat acetate and rosuvastatin |
|---|---|
| Also known as | TAK-475, Crestor |
| Sponsor | Takeda |
| Drug class | ACAT2 inhibitor combined with statin |
| Target | ACAT2 and HMG-CoA reductase |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | Phase 3 |
Mechanism of action
This combination targets two distinct steps in cholesterol metabolism: lapaquistat acetate blocks the enzyme responsible for cholesterol esterification in the intestine, reducing dietary cholesterol uptake, while rosuvastatin inhibits the rate-limiting enzyme in hepatic cholesterol production. Together, they provide complementary mechanisms to lower LDL cholesterol through both reduced absorption and decreased synthesis.
Approved indications
- Hypercholesterolemia / elevated LDL cholesterol
Common side effects
- Elevated liver enzymes
- Muscle-related adverse events
- Gastrointestinal effects
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 Rosuvastatin in Subjects With Hypercholesterolemia (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 rosuvastatin CI brief — competitive landscape report
- Lapaquistat acetate and rosuvastatin updates RSS · CI watch RSS
- Takeda portfolio CI
Frequently asked questions about Lapaquistat acetate and rosuvastatin
What is Lapaquistat acetate and rosuvastatin?
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Related
- Drug class: All ACAT2 inhibitor combined with statin drugs
- Target: All drugs targeting ACAT2 and HMG-CoA reductase
- Manufacturer: Takeda — full pipeline
- Therapeutic area: All drugs in Cardiovascular
- Indication: Drugs for Hypercholesterolemia / elevated LDL cholesterol
- Also known as: TAK-475, Crestor
- Compare: Lapaquistat acetate and rosuvastatin vs similar drugs
- Pricing: Lapaquistat acetate and rosuvastatin cost, discount & access