Anacetrapib is a member of a class of cholesterol-lowering medications called CETP (Cholesteryl Ester Transfer Protein) inhibitors. Its primary function is to inhibit the transfer of cholesteryl esters between lipoproteins, which ultimately leads to a reduction in the level of LDL cholesterol, otherwise known as “bad cholesterol.” Here, we will cover the important properties of this drugin detail, including its chemical formula, CAS number, health benefits, potential effects, mechanism of action, safety, side effects, and dosing information.
The chemical name of Anacetrapib is (R)-1-(3-(4-((4-fluorobenzyl)carbamoyl)-1,2,5-oxadiazol-3-yl)phenyl)-3-(4-fluorophenyl)urea. The molecular formula of this drug is C30H25F2N5O2, and its formula weight is 558.55 g/mol. The CAS number of Anacetrapib is 875446-37-0.
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Synonyms include MK-0859 and R-130535.
Health Benefits of Anacetrapib
Anacetrapib has unique potential health benefits related to cardiovascular health. Such health benefits primarily stem from the activity of Anacetrapib on reducing the levels of LDL cholesterol, as high level of LDL cholesterol is deemed as a major risk factor for heart-related ailments. By inhibiting the CETP protein, Anacetrapib reduces the transfer of cholesteryl esters, hence decreasing the levels of LDL (low-density lipoprotein) cholesterol while increasing the levels of HDL (high-density lipoprotein) cholesterol, which is considered as 'good cholesterol.'
There have been several preclinical trials and randomized clinical trials (REVEAL trial) that showcase the potential effects of Anacetrapib on reducing the LDL cholesterol levels and other heart-related diseases. The observation made was that the medication showed up to 40% reduction in LDL levels, as well as a slight increase in HDL cholesterol. Furthermore, REVEAL trial demonstrated that this medication potentially reduces the risk of cardiovascular events.
Anacetrapib is a CETP inhibitor that targets the CETP protein. CETP protein is responsible for facilitating the transfer of cholesteryl esters between lipoproteins, including HDL and LDL. Anabolic cholesterol moves from the liver to peripheral tissue particles. High-density lipoprotein (HDL) and LDL particles transfer cholesteryl esters bi-directionally under CETP control. CETP inhibition simultaneously blocks the transfer of peripheral tissue cholesteryl esters to LDL and hepatic cholesterol esters to HDL.
The safety profile of Anacetrapib has been studied extensively in randomized clinical trials. Doses of up to 300mg daily had shown no significant adverse effects, and the medication was well-tolerated by patients. However, further research is needed to determine the safety of long-term use of Anacetrapib.
The most commonly reported adverse effects associated with Anacetrapib include gastrointestinal symptoms such as diarrhea and nausea. Other reported side effects include headache, back pain, fatigue, and dizziness. It is essential to contact a qualified healthcare professional if experiencing any of these side effects or other changes in health while taking the medication.
Anacetrapib dosing regimen is prescribed by health professionals based on the individual's health status and weight. Anacetrapib is usually administered orally as a tablet, and the dose ranges typically between 20 - 100mg per day.
Anacetrapib is a CETP inhibitor medication that functions to reduce LDL cholesterol levels while increasing HDL cholesterol levels. Through its unique mechanism of action, it inhibits CETP protein, blocking the transfer of cholesterol esters between lipoproteins. Published preclinical and randomized clinical trials (REVEAL trial) have demonstrated the potential of Anacetrapib in reducing the risk of cardiovascular events. Although Anacetrapib appears to be safe and well-tolerated without significant adverse effects, there remains a need for further research on the medication's long-term safety and efficacy. As with any medication, Anacetrapib should only be taken under the guidance of a qualified healthcare professional.