Lapaquistat

Lapaquistat (also known as TAK-475) is a lipid-lowering agent that was under development by Takeda Pharmaceutical Company for the treatment of hypercholesterolemia. It is an inhibitor of squalene synthase, an enzyme involved in the biosynthesis of cholesterol.

History

Lapaquistat was first synthesized by Takeda Pharmaceutical Company in the late 1990s as part of their research into lipid-lowering agents. The drug entered clinical trials in the early 2000s, but development was discontinued in 2007 due to concerns about potential liver toxicity.

Mechanism of Action

Lapaquistat works by inhibiting the enzyme squalene synthase, which is involved in the biosynthesis of cholesterol. By blocking this enzyme, the drug reduces the amount of cholesterol produced by the body, thereby lowering blood cholesterol levels.

Clinical Trials

Several clinical trials were conducted to assess the efficacy and safety of Lapaquistat. These trials showed that the drug was effective in lowering cholesterol levels, but there were concerns about potential liver toxicity. In 2007, Takeda announced that it was discontinuing the development of Lapaquistat due to these safety concerns.

Potential Side Effects

The most significant potential side effect of Lapaquistat is liver toxicity. Other potential side effects include gastrointestinal symptoms such as nausea and diarrhea, and musculoskeletal symptoms such as muscle pain and weakness.

See Also

• Lipid-lowering agent
• Squalene synthase
• Hypercholesterolemia

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