Lowers cetp. Medical search. Frequent questions

Moreover, although anacetrapib "showed that LDL lowering via CETP inhibition worked," retention of the drug in fat tissue meant it had an extended half-life. (medscape.com)
Recent developments in biologic cardiovascular drugs such as Pfizer's PCSK9 inhibitor, Esperion Therapeutics' novel LDL-lowering drug ETC-1002 and Merck's CETP inhibitor anacetrapib, uncovers the potential of these drugs. (ipsnews.net)
The next set of cholesterol guidelines will likely be published in the next few years after results from ongoing trials with PCSK9 inhibitors and the CETP inhibitor anacetrapib are completed. (cardiometabolichealth.org)
Two more CETP inhibitors are still in development, Merck's anacetrapib and evacetrapib from Eli Lilly. (chemistryworld.com)
My suspicion is that anacetrapib and evacetrapib will probably reduce the risk of disease, but largely because of their LDL-lowering properties. (chemistryworld.com)
The positive top-line results for Merck & Co's cardiovascular outcomes trial for its CETP inhibitor anacetrapib may not be enough to de-risk the class, and questions remain about the level of clinical benefit and the regulatory options. (citeline.com)

Two other drugs in the same class as evacetrapib, known as CETP inhibitors, have also failed: One, which lowered LDL levels by only 20 percent, had toxic side effects. (healthimpactnews.com)
Over the past decade, five different experimental drugs known as CETP inhibitors have been tested in large clinical trials in people with low HDL. (harvard.edu)

FOURIER (Further Cardiovascular Outcomes Research with PCSK9 Inhibition in Subjects with Elevated Risk) provided definitive evidence of the outcomes benefits of lowering plasma levels of low-density lipoprotein cholesterol (LDL-C) beyond current goals. (eas-society.org)
Genetic and pharmacological studies support the hypothesis that CETP inhibition reduces cardiovascular risk by lowering LDL, which, by extension, may also lower VCID. (biomedcentral.com)
Learn more about CETP inhibition for lipid management. (medscape.com)
Inhibition of miR-33a/b in non-human primates raises plasma HDL and lowers VLDL triglycerides. (skanestugan.se)

Elaidic acid increases plasma cholesterylester transfer protein (CETP) activity which lowers HDL cholesterol. (wikipedia.org)
The launch of antidyslipidemic agents from two novel drug classes - proprotein convertase subtilisin/kexin type 9 (PCSK9) and cholesterylester transfer protein (CETP) inhibitors - will be the primary drivers of market growth during this period, and will offset the strong generalisation that has and will continue to impact this market to 2022, says the study, from Decision Resources. (pharmatimes.com)

The plasma cholesteryl ester transfer protein (CETP) activity in fish oil fed hamsters was lower compared to the MIX diet fed hamsters, thus this increase in LDL-cholesterol concentration and decrease in HDL-cholesterol concentration in fish oil fed hamsters are not a result of increased CETP activity. (mun.ca)

MILAN - Adding the cholesteryl ester transfer protein (CETP) inhibitor obicetrapib to high-intensity statins significantly lowers cholesterol levels and substantially increases the number of patients achieving cholesterol targets, suggest data from the ROSE trial. (medscape.com)
The latest results are something of a reversal for the CETP inhibitor, after a series of disappointments led to many writing them off, and the original developer of obicetrapib, Amgen, discontinuing development in 2017. (medscape.com)
Still, another new CETP inhibitor called obicetrapib looks promising. (harvard.edu)
We look forward to sharing topline data from BROADWAY and BROOKLYN in the second half of 2024, as we work to establish obicetrapib as a next-generation CETP inhibitor for some of the world's most prevalent and debilitating diseases. (pawtuckettimes.com)
NewAmsterdam is developing obicetrapib, an oral, low-dose and once-daily cholesteryl ester transfer protein ("CETP") inhibitor, as the preferred LDL-C lowering therapy to be used as an adjunct to maximally tolerated statin therapy for high-risk cardiovascular disease patients. (pawtuckettimes.com)
In a phase 2 study by Nicholls and colleagues , the CETP inhibitor obicetrapib, when added to high-intensity statin therapy, significantly increased levels of HDL-C by 135% using a 5-mg dose and 165% with a 10-mg dose. (medscape.com)

After that," Catapano said, there will be combination therapy, starting with bempedoic acid and ezetimibe, followed by PCSK9 inhibitors, siRNA drugs, and CETP inhibitors, all competing for the same space. (medscape.com)
Positive data from IMPROVE-IT will have a significant effect on physician prescribing and provide further validation of the LDL-C hypothesis, which will impact emerging LDL-C-lowering agents such as the PCSK9 inhibitors, agents which will initially target the most high-risk patients, it forecasts. (pharmatimes.com)
Two different algorithms were created for patients with familial hypercholesterolemia (FH) and recommend a lower threshold for the use of PCSK9 inhibitors. (cardiometabolichealth.org)
In these patients, the addition of the PCSK9 (proprotein convertase subtilisin/kexin type 9) inhibitor evolocumab to intensive statin therapy lowered LDL-C levels by 59% and led to a 15% reduction in major cardiovascular events and 20% reduction in the secondary 'hard outcomes' endpoint, a composite of cardiovascular death, MI and stroke. (eas-society.org)
That receptor clears LDL from circulation, making PCSK9 an appealing drug target: Blocking PCSK9 lowers blood LDL concentration, thereby reducing risk for cardiovascular disease. (asbmb.org)

The LDL:HDL ratio in humans is set mainly by CETP activity, which exchanges cholesteryl esters for triglycerides across lipoprotein fractions to raise LDL and lower HDL as CETP activity increases. (biomedcentral.com)
Three-dimensional illustration of cholesteryl ester transfer protein (CETP), which facilitates the transport of cholesteryl esters and triglycerides between lipoproteins. (citeline.com)
Genetic predisposition to higher HDL-C levels was associated with lower risk of small vessel stroke [odds ratio (OR) per standard deviation = 0.85, 95% confidence interval (CI) = 0.78-0.92] and lower WMH volume (β = -0.07, 95% CI = -0.12 to -0.02), which in multivariable Mendelian randomization remained stable after adjustments for LDL-C and triglycerides. (ox.ac.uk)
Moreover, thyroid hormones stimulate the cholesteryl ester transfer protein (CETP), an enzyme which transports cholesteryl esters from HDL2 to the very low density lipoproteins (VLDL) and triglycerides in the opposite direction 9 (figure). (hormones.gr)

Amgen (NASDAQ:AMGN) has announced new data from three separate analyses of Phase 2 and 3 studies evaluating evolocumab, a novel investigational low-density lipoprotein cholesterol (LDL-C)-lowering medication. (europeanpharmaceuticalreview.com)
Proof of benefit is strongest for lowering elevated low-density lipoprotein cholesterol (LDL-C) levels. (msdmanuals.com)
In the general population, evidence is less strong for a benefit from lowering elevated TG and increasing low high-density lipoprotein cholesterol (HDL-C) levels. (msdmanuals.com)
The reciprocal increase in HDL cholesterol (HDL-C) and decrease in low-density lipoprotein cholesterol (LDL-C) associated with CETP deficiency has led to the search for synthetic CETP inhibitors over the past 15 years. (cims-ops.cz)

CETP Inhibitors (cholesteryl ester transfer protein inhibitors) are still under development. (wikidoc.org)
Dalcetrapib is a cholesteryl ester transfer protein (CETP) inhibitor - the first CETP inhibitor, Pfizer's torcetrapib, was a high-profile failure back in 2006, with trials stopped because the drug raised blood pressure. (chemistryworld.com)
This narrative review focuses on the role of cholesteryl ester transfer protein (CETP) and peripheral lipoproteins in the vascular contributions to cognitive impairment and dementia (VCID). (biomedcentral.com)
and 3) describing the functions of cholesteryl ester transfer protein (CETP) in regulating the LDL:HDL ratio in humans, including therapeutic strategies targeting CETP. (biomedcentral.com)
Within the dal- Final results trial from the cholesteryl ester transfer proteins (CETP) inhibitor dalcetrapib sufferers received dalcetrapib furthermore to other realtors that lower LDL-C. Though a substantial elevation in HDL-C amounts was observed in sufferers treated with dalcetrapib the trial was terminated because of futility from the research6. (ampkpathway.com)
Despite success in REVEAL outcomes trial, Merck will not submit the for the cholesteryl ester transfer protein (CETP) inhibitor for regulatory approval. (citeline.com)
Aloïs Dusuel and colleagues at the University of Burgundy recently published findings in the Journal of Lipid Research that a protein tightly related to key players of the RLT pathway, cholesteryl ester transfer protein, or CETP, does not contribute to the binding and transfer of LPS in plasma. (asbmb.org)
Cholesteryl ester transfer protein (CETP) catalyzes the transfer of cholesteryl ester from high-density lipoprotein (HDL) to apolipoprotein B-containing lipoproteins in exchange for triglyceride, and thereby plays a major role in lipoprotein metabolism. (cims-ops.cz)
The cholesteryl ester transfer protein (CETP) has a central role in the lipid metabolism and therefore may alter the susceptibility to atherosclerosis. (biomedcentral.com)
Since the discovery of cholesteryl ester transfer protein (CETP) and its identification as a modulator of HDL-C levels (mediates the exchange of lipids between lipoproteins), there has been much speculation about its role in CAD [ 17 ]. (biomedcentral.com)

Analysis of CETP gene included additional cases and controls from the Secondary Manifestations of Arterial Diseases (SMART) study. (jamanetwork.com)
The scientists found that those who completed the test successfully (by correctly answering 25 of thirty questions) were two to three times more likely to possess the W variant of the CETP gene than those who did not. (cognitivelabs.com)
In this study they found that the ones who did not develop dementia on follow up were five times more likely to have the CETP W gene than those who did not. (cognitivelabs.com)
This research comes on top of earlier studies, also by Dr. Barzilai and his team where they first showed that CETP W helps people live longer and also pass this gene onto their descendants. (cognitivelabs.com)
HDL-C raising genetic variants in the gene locus of the target of CETP inhibitors were associated with lower risk of small vessel stroke (OR: 0.82, 95% CI = 0.75-0.89) and lower WMH volume (β = -0.08, 95% CI = -0.13 to -0.02), but a higher risk of intracerebral haemorrhage (OR: 1.64, 95% CI = 1.26-2.13). (ox.ac.uk)
The DNA of 471 subjects [133 subjects with angiographically documented left main coronary artery disease (LMCAD), 241 subjects with more peripheral coronary artery disease (MPCAD) and 97 subjects self reported healthy (Controls)] was analyzed for the frequency of TaqIB and I405V polymorphisms in the gene coding CETP. (biomedcentral.com)
Thus the studies evaluating the influence of CETP gene polymorphisms in humans are essential. (biomedcentral.com)
The CETP gene is located on chromosome 16q21. (biomedcentral.com)
Widely studied CETP variants is a silent base change called the Thermobius aquaticus IB (TaqIB) affecting the 277th nucleotide in the first intron of the CETP gene [ 18 ]. (biomedcentral.com)
Scientists now have several promising candidates thanks to the discovery of a gene variation in humans that appears to increase lifespan and lower the risk of cardiovascular diseases. (3quarksdaily.com)
In 2003, Nir Barzilai and Gil Atzmon, who study aging at Albert Einstein College of Medicine in New York, discovered that people with a certain polymorphism of the cholesterol-influencing gene CETP lived longer than those without it. (3quarksdaily.com)

We always knew dalcetrapib was an extremely weak inhibitor of CETP,' says Stanley Hazen, section head of preventive cardiology and cardiac rehabilitation at the Cleveland Clinic. (chemistryworld.com)
The HDL elevation is substantially lower with dalcetrapib and, more importantly, there was no LDL ['bad' cholesterol] reduction. (chemistryworld.com)
Dalcetrapib has clearly been hit a mortal blow, but I don't think the CETP inhibitor as a class of drug has yet. (chemistryworld.com)

statins are particularly well-suited for lowering LDL, the cholesterol with the strongest links to cardiovascular diseases. (wikidoc.org)
In studies using standard doses, statins have been found to lower LDL-C by 18% to 55%, depending on the specific statin being used. (wikidoc.org)

Even though cardiovascular outcomes trials of most CETP inhibitors failed to meet their primary outcomes, this finding was compound-specific rather than class-specific . (medscape.com)
The CETP-expressing mice also had worse sepsis outcomes. (asbmb.org)

In 2016 it was announced that a new drug that Eli Lilly was developing to lower cholesterol was abandoned because it offered no improvement in heart health. (healthimpactnews.com)

Elevated LDL-cholesterol (LDL-C) levels are well-established to cause cardiovascular disease and several LDL-C-lowering therapies are clinically available to manage this vascular risk factor. (biomedcentral.com)

In normolipidemic subjects, the absence of the TaqIB restriction site (B2 allele) is associated with decreased CETP activity and, in turn, increased HDL-C levels [ 19 ] resembling a mild form of CETP deficiency. (biomedcentral.com)

The American College of Cardiology (ACC) has released guidance on the role of nonstatin therapies in the lowering of LDL cholesterol, as additional data on their use have become available since the ACC and American Heart Association (AHA) last updated the cholesterol guidelines in 2013. (cardiometabolichealth.org)
The efficacy of LDL-C-lowering therapies to reduce risk of all-cause dementia and AD is now important to address as recent studies demonstrate a role for LDL in Alzheimer's Disease (AD) as well as in all-cause dementia. (biomedcentral.com)
The therapeutic potential of existing and emerging LDL-lowering therapies for VCID will be discussed. (biomedcentral.com)

New guidance on use of nonstatin cholesterol-lowering drugs. (cardiometabolichealth.org)
Cholesterol-lowering drugs are the best-selling drugs of all time. (healthimpactnews.com)
There is one major flaw with cholesterol-lowering drugs: they neither improve heart health nor prolong life according to scientific studies. (healthimpactnews.com)
Since blockbuster cholesterol-lowering drugs like Lipitor now have expired patents, millions of dollars have been spent in research to develop new cholesterol-lowering drugs. (healthimpactnews.com)

It behaves substantially differently from the two more potent, cleaner CETP inhibitors still under development. (chemistryworld.com)
ACE inhibitors prevent the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, and lower aldosterone secretion. (medscape.com)

Furthermore, not only did further lowering of LDL-C levels reduce cardiovascular events, but there was also significant reduction in major adverse limb events, defined as acute limb ischaemia, major amputation, or urgent peripheral revascularization for ischaemia. (eas-society.org)

The plasma LDL- and VLDL-cholesterol concentrations were significantly higher where as HDL-cholesterol concentration was significantly lower in fish oil fed hamsters especially at high fat levels. (mun.ca)
Unlike apoav-/- mice, injection of apoA-V rHDL into gpihbp1-/- mice had no effect on plasma TG levels, and apoA-V remained associated with plasma VLDL.Intravenously injected apoA-V rHDL significantly lowers plasma TG in an apoA-V deficient mouse model. (omicsdi.org)

Workshop 5 : Will we be able to answer the question of HDL as a therapeutic target after the CETP inhibitor trials? (canal-u.tv)
Just because an intervention raises HDL cholesterol, you can't assume risk of [heart attack] will be lower and it raises serious questions about whether HDL cholesterol can be used as a surrogate for heart attack risk in drug trials,' he says. (chemistryworld.com)

Genetic predisposition to higher HDL-C, specifically to cholesterol in medium-sized high-density lipoprotein particles, is associated with both a lower risk of small vessel stroke and lower WMH volume. (ox.ac.uk)

Consistent with our in vitro findings, these results suggest that the lower level of FoxO3a that is present in BCR ABL mice is predominantly phosphorylated and is therefore inactive. (mi-rna.com)
Unlike humans, wild-type mice do not express catalytically active CETP and have HDL as their major lipoprotein fraction. (biomedcentral.com)
Genetic restoration of CETP expression in mice to generate a more human-like lipid profile may increase the relevance of murine models for VCID studies. (biomedcentral.com)
However, when the researchers injected purified LPS into mice to simulate infection, the mice that were genetically altered to express CETP cleared endotoxins at a slower rate than mice who expressed no CETP. (asbmb.org)

They simply lower cholesterol levels, which is assumed to contribute to better health. (healthimpactnews.com)
The other raised HDL levels but did not lower LDL levels at all. (healthimpactnews.com)
However, a recent analysis found that people with very high HDL levels (80 mg/dL or higher) were about as likely to die from heart disease as people with low HDL (30 mg/dL or lower). (harvard.edu)
People who consumed the most sugar had HDL levels that were, on average, about 11 points lower than the low-sugar-intake group. (harvard.edu)
However, there is another question overshadowing the CETP inhibitors - how much does raising your HDL levels help to protect your heart? (chemistryworld.com)
It lowers plasma insulin levels and is used to treat type 2 diabetes associated with insulin resistance. (medscape.com)
For example, high HDL-C levels caused by some genetic disorders may not be associated with a lower risk of cardiovascular disorders, and low HDL-C levels caused by some genetic disorders may not be associated with an increased risk of cardiovascular disorders. (msdmanuals.com)
Recent studies show an association between elevated plasma LDL, a well-known cardiovascular risk factor, and a higher risk of AD, and considerable evidence suggests that high HDL levels are associated with reduced CAA and lower neuroinflammation. (biomedcentral.com)
The hamsters were fed diets rich in either fish oil or a MIX oil to investigate whether fish oil has beneficial effects in lowering plasma lipid and lipoprotein levels. (mun.ca)
HDL cholesterol and the larger HDL in particular is thought to help remove cholesterol from thickened artery walls and high levels of HDL are linked to lower incidence of atherosclerosis and may even help to reverse the condition. (cognitivelabs.com)
Thus, individuals in these regions have increased susceptibility to cardiometabolic abnormalities at lower absolute levels of adiposity. (biomedcentral.com)

Years after failures by Merck, Lilly, Pfizer and Roche, NewAmsterdam hopes to bring a CETP inhibitor to market to lower cholesterol, and signs on with Menarini to lead commercial efforts in Europe. (citeline.com)

Lowering LDL reduces that risk. (harvard.edu)

Studies with animal models have been limited, because many species do not express a functional CETP protein and are not reliable to provide strong evidence for CETP's role in disease. (biomedcentral.com)

They are called lipid-lowering drugs (LLD) or agents. (wikidoc.org)
It is expected that these drugs will mainly increase HDL while lowering LDL. (wikidoc.org)
Treatment involves dietary changes, exercise, and lipid-lowering drugs. (msdmanuals.com)

that the current findings should allay fears over CETP inhibitors as a class. (medscape.com)
It will be interesting to observe the fate of the cholesterol-lowering vaccines in the light of recent findings showing no significant effect of the reduction of "bad" cholesterol, induced in that case by a small molecule targeting CETP, on cardiovascular diseases rate. (martinalutter.com)

Low CETP activity is associated with better cardiovascular health, due to decreased LDL and increased HDL, which may also improve brain health. (biomedcentral.com)
Considering the potential detrimental role of LDL in AD and the importance of HDL's beneficial effects on endothelial cells, high CETP activity may lead to compromised BBB integrity, increased CAA deposits and greater neuroinflammation. (biomedcentral.com)
Site-specific mutations in the heparin-binding region of apoA-V (amino acids 186 to 227) attenuated apoA-V rHDL TG-lowering activity by 50%, suggesting that this sequence element is required for optimal TG-lowering activity in vivo. (omicsdi.org)

Sales to date from this one particular cholesterol-lowering statin drug have exceeded $140 billion. (healthimpactnews.com)
How can a drug that lowers something that is associated with benefit not show any benefit? (healthimpactnews.com)

Dezima Pharma has announced the publication of the phase 2b TULIP study results with its CETP inhibitor, TA-8995, in patients with mild dyslipidaemia. (europeanpharmaceuticalreview.com)

The researchers suggest looking into the inflammatory response over time to better understand the role CETP plays in the inflammatory process and, possibly, in sepsis. (asbmb.org)

The results clearly showedthe taxonomic shifts in each stage of CETP, which aligned with physico-chemical changes. (scitechnol.com)

In the present guidelines, low HDL cholesterol both modifies the goal for LDL-lowering therapy and is used as a risk factor to estimate 10-year risk for CHD. (medscape.com)
For lowering your risk of heart attack and stroke, reducing elevated LDL cholesterol is still the main priority," says Dr. Plutzky. (harvard.edu)

The belief that lowering cholesterol offers health benefit is a belief that has never been proven scientifically. (healthimpactnews.com)

The literature search strategy used focused on the search terms AD, VCID, LDL, HDL, and CETP to identify primary papers and review articles in PubMed and Medline within the last 25 years. (biomedcentral.com)

With higher overdispersion, θ = 4, or lower calf:cow ratios, r = 0.05 or 0.1, >400 groups must be sampled to attain 20% relative precision (Fig. 5A). (cetp-signal.com)

Yet we see continued physician optimism for CETP inhibitors, which also primarily target HDL-C. While this enthusiasm is driven by their additional LDL-C-lowering ability, the pendulum appears to be swinging back to LDL-C as the most robust modifiable dyslipidemia target, according to experts we interviewed," says Dr Narang. (pharmatimes.com)

Anatomy8

Organisms9

Diseases15

Chemicals and Drugs81

Analytical, Diagnostic and Therapeutic Techniques and Equipment10

Psychiatry and Psychology1

Phenomena and Processes34

Technology, Industry, Agriculture1

Information Science2

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Health Care4

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Anacetrapib6

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Inhibition4

Cholesterylester transfe2

Increased CETP activity1

Obicetrapib6

PCSK95

Triglycerides4

Lipoprotein cholesterol4

Cholesteryl ester10

Gene11

Dalcetrapib3

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Cholesterol-lower4

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High-density lip1

Mice4

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