Welcome to “A to Z: Drugs in Highlight: N is for NILEMDO®
This series is designed to delve into the intricate realm of pharmaceutical drugs. As the world of pharmaceuticals continues to evolve with new discoveries and emerging challenges, we aim to shed light on the diverse array of medications available today, ranging from blockbuster medications to those that may not be as familiar. Whether you’re a healthcare professional, a student, or simply someone with a curious mind, “A to Z: Drugs in Highlight” promises to be an enlightening and engaging series.
N is for NILEMDO®
NILEMDO® (from Esperion Therapeutics, Inc and Daiichi Sankyo Europe GmbH), also sold under the brand name NEXLETOL®, uses bempedoic acid to reduce blood cholesterol levels in the blood. It is used to treat adults with adults with primary hypercholesterolaemia (a condition that causes high levels of cholesterol in the blood) or mixed dyslipidaemia (a conditions where there are high levels of LDL cholesterol and triglycerides).
How it works:
Bempedoic acid is a prodrug that is metabolized in the liver by long-chain acyl-CoA synthetase I into its active form, bempedoyl coenzyme A. This active form inhibits the enzyme adenosine triphosphate citrate lyase (ACL) in the liver. By blocking ACL, bempedoyl coenzyme A reduces cholesterol production and enhances the removal of LDL-cholesterol from the blood.
NILEMDO® can be used alone or in combination with other cholesterol-lowering medication. For example, bempedoic acid can been administered in combination with ezetimibe, which inhibits the intestinal absorption of cholesterol. The combination of bempedoic acid and ezetimibe is sold under the brand names NUSTENDI® and NEXLIZET®.
Patients taking NILEMDO® are required to be on a low-fat diet.
Marketing approval:
NILEMDO® is approved for marketing in both the United States (approved by the FDA in February 2020) and Europe (approved by the EMA in April 2020).
Patent protection:
There are patent rights protecting various aspects of the NILEMDO® technology.
The original European patents for bempedoic acid (for example, EP1597223B1, EP2402300B1 and EP2404890B1) have expired. However, bempedoic acid remains protected in Europe by Supplementary Protection Certificates, which are set to expire December 2028.
EP4438114A2 is a pending European patent application filed by Esperion Therapeutics, Inc. The claims on file relate to a pharmaceutical material comprising a crystalline form of the compound of formula (V):
or a pharmaceutically acceptable salt thereof; wherein the pharmaceutical material comprises the compound of formula (V), or a pharmaceutically acceptable salt thereof, in an amount greater than 98% by weight based on the total weight of the pharmaceutical material; and the pharmaceutical material comprises at least one of the following: 0.0001% to 0.15% of a compound of formula (VI):
or a pharmaceutically acceptable salt thereof, based on the total weight of the pharmaceutical material; and 0.001% to 0.15% of a compound of formula (VIII):
or a pharmaceutically acceptable salt thereof, based on the total weight of the pharmaceutical material.
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