Laropiprant

Laropiprant is a drug that was used in combination with niacin to reduce blood cholesterol. It was developed by Merck & Co and was sold under the trade name Tredaptive. Laropiprant acts by inhibiting the action of prostaglandin D2 (PGD2) on the DP1 receptor (also known as DP1), which mediates flushing. The combination of laropiprant and niacin was withdrawn from the market worldwide in 2013, due to its association with an increased risk of side effects, including non-fatal but serious skin and gastrointestinal problems.

History

Laropiprant was developed by Merck & Co and was approved by the European Medicines Agency (EMA) in 2008 for use in combination with niacin to reduce blood cholesterol. The combination was sold under the trade name Tredaptive. However, in 2013, the EMA recommended the withdrawal of the combination from the market worldwide due to its association with an increased risk of side effects, including non-fatal but serious skin and gastrointestinal problems.

Pharmacology

Laropiprant is a selective antagonist of the DP1 receptor, which is a receptor for prostaglandin D2 (PGD2). PGD2 mediates flushing, a common side effect of niacin therapy. By inhibiting the action of PGD2 on the DP1 receptor, laropiprant reduces the incidence and severity of niacin-induced flushing.

Side Effects

The combination of laropiprant and niacin has been associated with an increased risk of side effects, including non-fatal but serious skin and gastrointestinal problems. Other side effects may include diarrhea, nausea, vomiting, dyspepsia, and pruritus.

See Also

• Niacin
• Prostaglandin D2
• DP1 receptor
• Merck & Co

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