Lapaquistat acetate

Lapaquistat acetate

Lapaquistat acetate is a pharmacological agent that was developed for the treatment of hypercholesterolemia. It functions as an squalene synthase inhibitor, which is a key enzyme in the cholesterol biosynthesis pathway. However, its development was discontinued due to safety concerns.

History

Lapaquistat acetate, also known as TAK-475, was developed by Takeda Pharmaceutical Company. The drug entered Phase III clinical trials for the treatment of hypercholesterolemia. However, in 2008, Takeda announced that it was discontinuing the development of Lapaquistat acetate due to the occurrence of unexplained liver injuries in some patients.

Mechanism of Action

Lapaquistat acetate is a squalene synthase inhibitor. Squalene synthase is an enzyme that plays a crucial role in the cholesterol biosynthesis pathway. By inhibiting this enzyme, Lapaquistat acetate reduces the production of cholesterol in the body.

Clinical Trials

In clinical trials, Lapaquistat acetate was shown to significantly reduce low-density lipoprotein (LDL) cholesterol levels. However, the drug was also associated with an increased risk of liver injury, leading to its discontinuation.

Safety Concerns

The development of Lapaquistat acetate was discontinued due to safety concerns. During clinical trials, some patients experienced unexplained liver injuries. The exact cause of these injuries is unknown, but they were severe enough to warrant the discontinuation of the drug's development.

See Also

• Squalene synthase inhibitor
• Hypercholesterolemia
• Takeda Pharmaceutical Company