• Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias? (wikipedia.org)
  • 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)
  • with the torcetrapib data, investigators at competing drug manufacturer, Merck, reported encouraging data with their version of CETP inhibitor, anacetrapib. (undoctored.com)
  • Spokesman Daniel Bloomfield, M.D., of Merck Research Laboratories reported that "The favorable lipid effects seen in this study with multiple doses of anacetrapib were significant, and confirm the continued evaluation of the clinical benefits of CETP inhibitors in the treatment of dyslipidemia. (undoctored.com)
  • Notably, the last of the phase III CETP inhibitor trials, the pivotal REVEAL trial for anacetrapib, is slated to be released in the final Hot Line session of the conference. (medpagetoday.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)
  • Merck (NYSE: MRK), known as MSD outside the U.S. and Canada, today announced that the company will not submit applications for regulatory approval for anacetrapib, Merck's investigational cholesteryl ester transfer protein (CETP) inhibitor. (merck.com)
  • 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)
  • 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)
  • Torcetrapib is the first among the "cholesteryl-ester transfer protein inhibitors," or CETP-inhibitors, drugs that block the exchange of cholesterol and triglycerides between HDL and VLDL particles and prevent formation of the unwanted small LDL particles. (undoctored.com)
  • CETP Inhibitors (cholesteryl ester transfer protein inhibitors) are still under development. (wikidoc.org)
  • These include the next generation peroxisome proliferator-activated receptorα agonists, cholesteryl ester transfer protein inhibitors and monoclonal antibody therapy targeting proprotein convertase subtilisin/kexin type 9. (biomedcentral.com)
  • He emphasized that cost limits the use of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors and small-interfering (si)RNA drugs, "so there is a huge unmet need globally in order to get patients to goal. (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)
  • Praluent is the only EC-approved PCSK9 inhibitor that is available in two starting doses, offering two levels of efficacy. (europeanpharmaceuticalreview.com)
  • Launch of PCSK9 inhibitors (Praluent) for treating hyperlipidemia in 2016 is likely to fuel expansion of anti-hyperlipidemia drugs market segment by 2025 augmenting global cardiovascular drugs market. (ipsnews.net)
  • Introduction of new anti-hyperlipidemia drug such as PCSK9 Inhibitor (Praluent) and increasing incidences of hyperlipidemia is likely to propel expansion of the segment. (ipsnews.net)
  • 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)
  • 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)
  • 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)
  • In an updated statement, a Task Force from the European Society of Cardiology and European Atherosclerosis Society provided practical guidance to aid clinicians considering treatment with a PCSK9 inhibitor in ASCVD patients or FH patients without clinical events, focusing on threshold LDL-C levels and other indices of cardiovascular risk. (eas-society.org)
  • Two different algorithms were created for patients with familial hypercholesterolemia (FH) and recommend a lower threshold for the use of PCSK9 inhibitors. (cardiometabolichealth.org)
  • Although ezetimibe is considered appropriate for high-risk primary prevention, Dr. Lloyd-Jones said not enough data yet exists on PCSK9 inhibitors to support their use in primary prevention. (cardiometabolichealth.org)
  • PCSK9 inhibitor use, according to the document, should be reserved for those patients at highest risk (eg, those with FH, ACS, or those who are statin intolerant). (cardiometabolichealth.org)
  • Later that day, Dr. Christie M. Ballantyne will chair a lunch symposium titled, "Patient-focused LDL-C Management and Risk Reduction in Clinical Practice: The Utility of PCSK9 Inhibitors. (cardiometabolichealth.org)
  • The trial included multiple exclusion criteria, such as current clinically manifest atherosclerotic cardiovascular disease including, but not limited to, a major adverse cardiovascular event within 3 months prior to randomization or New York Heart Association Functional Classification Class III or IV heart failure, concomitant use of PCSK9 inhibitors or bempedoic acid, BMI of 40 kg/m2 or greater, an HbA1c of 10% or greater, uncontrolled hypertension, renal dysfunction, and others. (consultantlive.com)
  • A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein (CETP). (wikipedia.org)
  • citation needed] CETP inhibitors inhibit cholesterylester transfer protein (CETP), which normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL). (wikipedia.org)
  • When cholesterylester transfer protein (CETP) inhibitors were first being investigated, the theory that raising HDL-C could decrease the risk of CVD events in at-risk patients was being accepted as a medical reality. (biopharmadive.com)
  • With the presentation of the dal-OUTCOMES trial at the American Heart Association in Los Angeles andsimultaneous publication in the New England Journal of Medicine, dalcetrapib joins torceptrapib on the list of once-promising CETP inhibitors. (cardiobrief.org)
  • Roche announced today that it had ended development of dalcetrapib, its entry in the once-promising class of HDL-raising CETP inhibitors. (cardiobrief.org)
  • PARIS, France-The experimental agent dalcetrapib appears to raise high-density lipoprotein (HDL) cholesterol levels by inhibiting cholesterol ester transfer protein (CETP) activity without adversely affecting blood pressure or endothelial function, according to phase II trial data presented Sunday, August 28 at the European Society of Cardiology Congress 2011. (tctmd.com)
  • Dalcetrapib is one of four CETP inhibitors to have reached full-scale development. (dalcorpharma.com)
  • 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 conference also features a a Mendelian randomization comparison of CETP inhibitors and statins. (medpagetoday.com)
  • This approach has already benefitted the health of patients with acne, heart attack risks, or certain cancers due to the development of retinoids, statins, and checkpoint inhibitors. (drugdiscoveryonline.com)
  • Statins or HMG-CoA reductase inhibitors modestly increase HDL-C levels. (medscape.com)
  • Increases in HDL-C levels may also be attributable to decreasing plasma cholesteryl ester transfer protein (CETP) activity by statins. (medscape.com)
  • ezetimibe (Zetia) is a selective inhibitor of dietary cholesterol absorption. (wikidoc.org)
  • With the trial meeting its primary and secondary endpoints, results provide evidence use of the once-daily, oral, low-dose cholesteryl ester transfer protein (CETP) inhibitor from NewAmsterdam Pharma Company, in combination with ezetimibe, was associated with statistically significant and clinically meaningful reductions in LDL-C and apolipoprotein B (ApoB). (consultantlive.com)
  • Learn more about CETP inhibition for lipid management. (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)
  • 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)
  • Still, another new CETP inhibitor called obicetrapib looks promising. (harvard.edu)
  • 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)
  • JTT-705: is there still future for a CETP inhibitor after torcetrapib? (wikipedia.org)
  • The adverse effects of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib on cardiovascular outcome, which were observed despite a substantial increase in HDL levels, have suggested that a better understanding of the vascular effects of HDL from patients with CAD is urgently required. (health.am)
  • According to discussant Keith A. A. Fox, MD, of the University of Edinburgh (Edinburgh, Scotland), researchers were eager to find a CETP inhibitor that showed efficacy without dangerous side effects, because a previous agent, torcetrapib, reached phase III trials before being dropped because of an increase in deaths. (tctmd.com)
  • For one thing, it's not clear whether torcetrapib failed because of its CETP activity, or just because it there was something odd about torcetrapib itself. (chemistryworld.com)
  • This is another step forward for personalized medicine-and potentially a second chance for CETP inhibitors and Roche. (biopharmadive.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)
  • Roche (with their partners at Japan Tobacco) and Merck are known to be in the clinic with CETP inhibitors of their own. (chemistryworld.com)
  • CETP inhibitors do not reduce rates of mortality, heart attack, or stroke in patients already taking a statin. (wikipedia.org)
  • Another HDL-raising CETP inhibitor has failed to demonstrate cardiovascular benefit in a large clinical trial. (cardiobrief.org)
  • 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)
  • Posthoc analyses of large clinical trials with CETP inhibitors have demonstrated their potential anti-diabetic properties. (bvsalud.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)
  • Despite success in REVEAL outcomes trial, Merck will not submit the for the cholesteryl ester transfer protein (CETP) inhibitor for regulatory approval. (citeline.com)
  • The present invention relates to kinase inhibitors for the treatment of cancer. (justia.com)
  • Bortezomib restores expression of FoxO3a in imatinib resistant T315I cells The T315I BCR ABL mutation frequently occurs in CML patients that are resistant to imatinib, and even remains refractory to the more potent second generation kinase inhibitors. (mi-rna.com)
  • The drug inhibits CETP, thus increasing HDL. (tctmd.com)
  • This is the same pathway blocked by blood pressure drugs like ACE inhibitors lisinopril and enalapril, ARBs like losartan. (undoctored.com)
  • It will clearly be many years before we have a confident answer on whether the CETP-inhibitor class of drugs will be a safe choice for correction of cholesterol abnormalities, especially low HDL. (undoctored.com)
  • More than three decades of chasing high-density lipoprotein (HDL) cholesterol as a driver of cardiovascular events, including the costly development and failure of CETP inhibitor drugs, demonstrated that low HDL, though a risk factor, is not a driver of heart disease. (drugdiscoveryonline.com)
  • Cholesteryl ester transfer protein (CETP) inhibitors are specific drugs designed to increase HDLC and HDL functions. (bvsalud.org)
  • This is one of several inhibitors of heme biosynthesis in firmicutes that was identified, using the screen described in the accompanying manuscript. (mdpi.com)
  • Of every group had adequate CETP Inhibitor Compound vitamin B12 and vitamin D levels, and these parameters have been larger in supplement users. (trpv1inhibitor.com)
  • What really obscures things is that Roche's compound seems to act on CETP through a different mechanism, and thus probably through a different binding site. (chemistryworld.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)
  • Less CETP activity essentially means more HDL, which helps to reduce the build up of fatty atherosclerotic plaques that block blood vessels. (chemistryworld.com)
  • Though CETP inhibitors offer the potential for a one-stop opportunity to raise HDL substantially, there are still many strategies available to raise HDL. (undoctored.com)
  • People are spending hundreds of millions of dollars to find out more about CETP. (chemistryworld.com)
  • Workshop 5 : Will we be able to answer the question of HDL as a therapeutic target after the CETP inhibitor trials? (canal-u.tv)
  • 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)
  • But skeptics think CETP inhibitors are a dead end A new company is betting hundreds of millions of dollars that it can snatch victory from the jaws of defeat. (cardiobrief.org)