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CAS NO:
571170-77-9
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Basic Info
CAS Number
571170-77-9
Pharmacopoeia
ChP,USP,BP,EP,JP,ChP
Product Keywords
Laropiprant,,Intermediates
Is Manufacturer
No
Samples Provided
NO
Packaging & Delivery
Packaging Specification
packaging : Length x Width x Height
shipping_port :
shipping_port :
Product Description
AI Product Description
*The following content is generated by AI and is for reference only.
Laropiprant, chemically known as 4-[2-[(5-chloro-1H-indol-3-yl)methyl]-6-methoxy-1-benzofuran-7-yloxy]butan-2-one, is a selective antagonist of the prostaglandin D2 receptor DP1. Its molecular formula is C25H28ClNO4, and it carries the CAS Registry Number 939990-89-5. Originally developed by Takeda Pharmaceutical Company Limited, this compound gained significant attention primarily for its role in combination therapy with niacin (nicotinic acid) to treat dyslipidemia.
The primary clinical utility of laropiprant stems from its ability to mitigate cutaneous flushing, a common and often dose-limiting side effect associated with high-dose niacin supplementation. Niacin is effective in raising high-density lipoprotein (HDL) cholesterol levels and lowering triglycerides, but the intense skin flushing can severely impact patient compliance and quality of life. By selectively blocking the DP1 receptor on sensory nerve endings in the skin, laropiprant inhibits the vasodilation caused by prostaglandin D2 released during niacin administration, thereby allowing patients to tolerate higher therapeutic doses of niacin without discomfort.
Although laropiprant was successfully formulated into a fixed-dose combination product named Advicor or similar variants in various markets, its development trajectory faced challenges due to mixed results in large-scale cardiovascular outcome trials. While the drug effectively managed the side effects of niacin, subsequent studies failed to demonstrate that adding laropiprant to standard lipid-lowering regimens significantly reduced major adverse cardiovascular events compared to placebo. Consequently, despite its pharmacological success in solving the flushing issue, the commercial adoption of laropiprant has been limited in recent years as newer, more potent lipid-modifying agents have emerged. Nevertheless, laropiprant remains a scientifically important molecule in pharmacology, serving as a prime example of targeted receptor antagonism improving the tolerability profile of established therapies. It continues to be studied for potential applications in other inflammatory conditions where PGD2 signaling plays a critical pathogenic role.
![4-[[[[6-[(Diethylamino)methyl]-2-naphthalenylmethoxy]carbonyllaminolbenzoic acid](https://eimg.pharmasources.com/image/20241206/xJCFsdgfMrHzqjtgeOixhGQHgVbKi7kAcoEqemzE.jpg)
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