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Arena Pharmaceuticals, Inc. Message Board

jeremiahthirtythreeone 1496 posts  |  Last Activity: Apr 7, 2014 12:32 PM Member since: Feb 16, 2010
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  • The valvulopathy issue is a NON issue but Arena continues to provide evidence to refute the falsehoods produced by the paid charlatans.

    EFFECTS OF LORCASERIN ON PREEXISTING VALVULOPATHY IN TWO PHASE 3 LORCASERIN TRIALS: A POOLED ANALYSIS
    Neil J. Weissman, et al
    JACC (Journal of the American College of Cardiology), 2014-04-01, Volume 63, Issue 12, Supplement , Pages A1945-A1945
    2014 American College of Cardiology Foundation
    Background
    Lorcaserin (lor) is a selective 5-HT2C receptor agonist indicated for chronic weight management as an adjunct to lifestyle modification. Valvulopathy has been associated with nonselective serotonergic agonists; however, the phase 3 trials showed no significant increase in valvulopathy in patients (pts) on lor (relative risk ∼1.1, lor vs placebo; P=0.47). This analysis of the phase 3 studies sought to evaluate the effect of lor on pts with valvulopathy prior to taking lor.
    Methods
    Serial echocardiographs were performed at baseline (BL) and every 6 months in BLOSSOM (4,008 pts without type 2 diabetes [T2D] and BMI 30-45 kg/m2 or 27-29.9 kg/m2 with ≥1 weight-related comorbidity) and BLOOM-DM (604 pts with T2D and BMI 27-45 kg/m2). Echocardiographs were performed over 1 year (W52) in 168 pts with BL valvulopathy. American Society of Echocardiography criteria were used by an independent core lab with 2 blinded cardiologists. The primary endpoint is change in regurgitation from BL to W52 (last observation carried forward).
    Results
    The majority of shifts from BL to W52 were single-grade changes (Figure), with more pts demonstrating a decrease in regurgitation than an increase. At W52, 57.8% and 52.9% of lor and placebo pts with BL valvulopathy no longer met these criteria, using FDA criteria.
    Conclusions
    Lor pts with preexisting valvulopathy did not show progression of valve disease up to 1 year. Most showed regression of ttheir regurgitation, which was comparable to the placebo group.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Mar 4, 2014 1:37 PM Flag

    Few children are born obese-obesity develops over time, as children progress from infancy to childhood and adolescence. It is not only a parental problem but a societal problem as well. Thus, risk reduction among young children is clearly important, with the implication that wide-reaching, cost-effective policy and programmatic changes aimed at improving nutrition and physical activity among broad populations of children are key if we are to reduce early childhood weight gain and the risk of incident obesity throughout childhood. As we know these have proven to be difficult and expensive. Though clinical interventions such as those that aim to alter early life systems are likely to be most effective the problem still persists and though it has plateaued in recent years there is still need for a safe and effective anti-obesity pill.
    Belviq will definitely play a major role in the treatment and possibly the prevention of this problem.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Mar 4, 2014 1:23 PM Flag

    The FDA approved the trials in the pediatric population. If proven to be safe then they will be able to prescribe to this population. BTW, lorcaserin was approved for study in the pediatric population in Europe and when the EU decides to accept lorcaserin they will be able to begin studies there also.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • Incidence of Childhood Obesity in the United States
    Solveig A. Cunningham, Ph.D., Michael R. Kramer, Ph.D., and K.M. Venkat Narayan, M.D.
    N Engl J Med 2014; 370:403-411
    The following are some excerpts from this article
    Childhood obesity is a major health problem in the United States. The prevalence of a body-mass index (BMI; the weight in kilograms divided by the square of the height in meters) at the 95th percentile or higher among children between the ages of 6 and 11 years increased from 4.2% in 1963–1965 to 15.3% in 1999–20002,3 and may have plateaued during the first decade of the 21st century. National data on the incidence of pediatric obesity to date have pertained only to adolescents transitioning to adulthood. A study that was based on data from the National Longitudinal Study of Adolescent Health showed that the 5-year cumulative incidence of obesity among persons who were 13 to 20 years of age in 1996 and 19 to 26 years of age in 2001 was 12.7%, ranging from 6.5% among Asian girls to 18.4% among non-Hispanic black girls.

    Our estimates are consistent with nationally representative data, which showed the prevalence of obesity at 16.9% among all children and 18.0% among elementary-school children between the ages of 6 and 11 years in 2009 and 2010.4 The incidence of obesity between adolescence and adulthood in the United States was estimated at 2.5% annually from 1995 through 2000.

    Arena has already begun to evaluate the use of Belviq in this population.
    Single Dose Study to Determine the Safety, Tolerability, and Pharmacokinetic Properties of Lorcaserin Hydrochloride (BELVIQ) in Obese Adolescents From 12 to 17 Years of Age

    ClinicalTrials.gov Identifier:
    NCT02022956
    First received: December 23, 2013
    Last updated: January 21, 2014
    Last verified: January 2014

    FYI
    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Feb 21, 2014 12:15 PM Flag

    oops, thanks
    Patents beneficial for patients :)
    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Feb 21, 2014 11:42 AM Flag

    Inventors: Robert M. Jones (San Diego, CA, US)
    Assignees: ARENA PHARMACEUTICALS, INC.
    IPC8 Class: AC07D40114FI
    USPC Class: 514269
    Class name: Hetero ring is six-membered consisting of two nitrogens and four carbon atoms (e.g., pyridazines, etc.) 1,3-diazines (e.g., pyrimidines, etc.) pyrimidines with chalcogen bonded directly to a ring carbon of said pyrimidine moiety
    Publication date: 2014-02-20
    Patent application number: 20140051714

    ======
    Patent application title: MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO

    Inventors: Robert M. Jones (San Diego, CA, US) Juerg Lehmann (San Diego, CA, US) Weichao Chen (San Diego, CA, US) Jeffrey Edwards (San Diego, CA, US) Glen Marquez (San Jose, CA, US) Michael E. Morgan (San Diego, CA, US) Abu J.m. Sadeque (San Diego, CA, US) Sun Hee Kim (San Diego, CA, US)
    Assignees: ARENA PHARMACEUTICALS, INC.
    IPC8 Class: AC07D41314FI
    USPC Class: 514 65
    Class name:
    Publication date: 2014-02-20
    Patent application number: 20140051629

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • The present invention relates to the GPR119 agonist, 4-(1-(5-ethylpyrimidin-2-yl...(Compound 1): and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing the secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto
    ========

    The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-(3-...)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neuroldisorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

    Read more wwwdotfaqsdotorg/patents/app/20140051629#ixzz2tyXHuf38

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • Reply to

    Why Brazil filing is important

    by sharonconk Feb 12, 2014 9:03 AM
    jeremiahthirtythreeone jeremiahthirtythreeone Feb 12, 2014 10:49 AM Flag

    Sharon,
    Thank you for all the important information you provide. I look forward to reading all your posts because you not only provide factual information you back it up always. There are only a few posters on this board worth reading and yourself and sauve9 are the two most important.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • Reply to

    Only 47% respond, and this is bad why?

    by lukb4ujump Jan 31, 2014 3:20 PM
    jeremiahthirtythreeone jeremiahthirtythreeone Jan 31, 2014 3:57 PM Flag

    Great post lukb4ujump. I might add that the loss of 5-10% of body weight decreases the risk of diabetes by 58%. The saddest thing that wall street is guilty of is trying to depress a medication that can help millions of their fellow human beings from the devastating effects of obesity on morbidity and mortality. Greed trumps helping our fellow sojourners on this terrestrial ball we inhabitat.

    Nevertheless, this is temporary - Belviq is too selective, its has potential for multiple indications, it is well tolerated, it is an oral medication - you cannot get better than that in a novel new drug - and it will succeed on a very solid scientific foundation. Obsessing on the weekly scripts is futile and those of us who have been here a long time have seen this medication progress in its intended purpose, baby steps for sure, but it will begin running in the not too distant future.

    The science is prevailing.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 31, 2014 11:39 AM Flag

    Thanks xoma and thanks for remembering. She is now a sophomore at UCLA in the premedical program in physiological sciences and is working extremely hard - very competitive. My other son just graduated from UCLA and has been accepted to law school and is doing well also.
    Thanks for asking

    Daniel
    UCLA MD

    Sentiment: Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 31, 2014 11:37 AM Flag

    stockvadar
    The standard of care for patients who undergo coronary artery stenting or who have an acute coronary syndrome (ACS) to reduce the risk of subsequent cardiovascular events such as stent thrombosis or recurrent ACS is the use of aspirin and clopidogrel. Therefore using temanogrel with aspirin and/or clopidogrel is tto assess the safety of this combination. If temanogrel demonstrates superior results with ASA (aspirin) as compared to with clopidogrel then the choice would be temanogrel with aspirin which would open the potential for studies for monotherapy in the future.

    But the key is that it is necessary to first study the safety aspects of this dual therapy. Remember the problem with clopidogrel is the high incidence of resistance and/or nonresponsiveness therefore by studying the dual therapy they can demonstrate whether temanogrel with ASA is superior to ASA with clopidogrel.

    Hope you understand why now

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 31, 2014 8:41 AM Flag

    The main advantage of a selective 5HT2a antagonist is that it does not directly affect antithrombotic agents. It works by preventing platelet aggregation and vasoconstriction that lead to thrombosis by direct 5HT2a antagonism and thus the presumed reason that it does not cause increased bleeding.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 31, 2014 8:30 AM Flag

    vjstocks,
    Several problems with plavix (clopidogrel):
    1. The best available observational data come from a retrospective analysis assessing the risk of bleeding in 118,606 patients with atrial fibrillation treated with different combinations of aspirin, clopidogrel, and vitamin K antagonist . During a mean follow-up of 3.3 years, 11.4 percent of patients experienced nonfatal (10.3 percent) or fatal (1.2 percent) bleeding.

    2. Adverse cardiovascular events occur despite recommended dual antiplatelet therapy (aspirin and clopidogrel) and this has been attributed in part to variable pharmacodynamic efficacy of one or both agents. Patients with "high on-treatment platelet reactivity” (HPR) have been labeled as being nonresponsive, hyporesponsive, or resistant. Numerous observational studies have demonstrated a strong link between HPR and recurrent ischemic events in stented patients. Prospective evaluating personalized antiplatelet therapy based on platelet function testing has not demonstrated clinical benefit

    3. Clopidogrel treatment failure is the occurrence of a thrombotic/ischemic event during clopidogrel therapy in patients with heightened platelet reactivity. These events are usually stent thrombosis or recurrent acute coronary syndrome

    The WOEST trial did not improve significantly these results.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • This post is to answer some of the important questions brought up from my previous post regarding the advantage of Temanogrel over other antithrombotic meds on the market.

    From the study I posted we read the following - a very important point:

    "5HT2A receptor antagonists, including ketanserin, sarpogrelate,
    and AR246686, can effectively block arterial thrombosis
    without increasing bleeding. However, lack of selectivity
    and suboptimal pharmacokinetics limit the usefulness of
    these compounds in the clinic. Thus, our goal was to improve
    the selectivity and pharmacokinetic profiles, which resulted
    in the discovery of APD791. Recently, APD791 was tested in
    the Folts dog model of coronary stenosis and was shown to
    effectively block coronary thrombosis without increasing
    bleeding time . The separation of
    antithrombosis effects and bleeding is of potential clinical
    relevance."

    Someone asked what drugs would Temangrel replace. Here is the list - we are all familiar with warfarin (coumadin) and plavix - both of which have problems with bleeding.

    The others include dabigatran, rivaroxaban, and apixaban. Anticoagulation with each of these newer agents leads to similar or lower rates both of ischemic stroke and major bleeding compared to warfarin. However, the risk of gastrointestinal bleeding was increased in these agents. There is a potentially higher rate of myocardial infarction with dabigatran and twice daily regimen (dabigatran and apixaban) Though they may have lower rates of major bleeding compared to warfarin it is still a risk with these drugs.

    Therefore, if the second phase 1 trial and subsequent phase 2a and 3 trials confirm the preclinical study results of blocking thrombosis through its unique and very specific 5HT2a receptor antagonist with no increased bleeding then Temanogrel will become a major player in antithrombotic therapy

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 30, 2014 12:59 PM Flag

    Again, the emphasize the brilliance of Arena's scientist with regard to developing drugs with very high affinity for the receptors they are intended to act upon here is the statement from S9's post on the nicotine rat study:

    Summary and conclusions
    1. Lorcaserin is one of the most selective 5-HT2C receptor agonists identified to date, having ~20-fold functional selectivity for 2C vs. 2A, and ~120-fold functional selectivity for 2C vs. 2B (Thomsen et al, 2008). In vivo this apparent selectivity is demonstrated by the fact that acute effects of this drug in wild type C57BL/B6 mice, evident over a 10- fold dose range is completely eliminated in 5-HT2C receptor KO mice across same dose range (Fletcher et al, 2009).

    For those who don't know KO mice do not have have the receptor

    I keep bringing this up because we have another GPCR developed agonist in CB2. Arena's ability to develop drugs with high affinity for the receptor has history and therefore CB2 agonist will likely be very selective.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 30, 2014 11:34 AM Flag

    That is correct. Thanks for clarifying that.

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 30, 2014 11:32 AM Flag

    Yes that is correct. And if it demonstrates sufficient efficacy in academic clinical trials then Arena can then seek FDA approval for this indication but what is important here is that while waiting for this physicians can still prescribe it. What about insurance coverage? Well, nifedipine is covered by insurance for the treatment of preterm labor although it is not FDA approved for this. And it can't be marketed for preterm labor yet it is the most widely prescribed drug for preterm labor and therefore very successful. Restrictions on marketing for off label indications do not prevent successful use of the drug. In fact, it does not need marketing because it is a necessary treatment.

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 30, 2014 11:18 AM Flag

    You do not have to go through these types of trials to study the effects of belviq on tobacco cessation and other substance abuse indications. This can be done without having an FDA approved indication because if the studies demonstrate sufficient efficacy they can be prescribed off-label legally, they just cant be marketed as the indication for tobacco cessation. Once a drug is on the market it can be studied for other indications. I have listed multiple drugs that have been approved for a specific indication and academic clinical trials have been performed for completely unrelated indications and used in clinical practice for these off-label indications. One example is nifedipine, an anti-hypertensive medication, has been shown to be effective in preterm labor - an unrelated indication - and is sold in the millions for the off-label indication. It didn't have to go through phase1-3 trials and yet it is completely legal to prescribe it to pregnant women for preterm labor - this is just one example of many.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 30, 2014 11:09 AM Flag

    S9
    Thank you for the followup on this. This information is exceedingly valuable. It is so important to keep bringing it up because we tend to have short term memories when thinking about the multiple benefits of this one drug. As always excellent work.

    There will be snowball effect in future clinical trials with belviq for treatment in addiction, T2DM, and hopefully soon fibromyalgia.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone jeremiahthirtythreeone Jan 30, 2014 10:53 AM Flag

    Continued

    The second most advanced 5-HT2C agonist is vabicaserin which completed a 6 week Phase II trial in 313 patients diagnosed and hospitalized with schizophrenia [79]. At a 200 mg dose (but not 400 mg), vabicaserin reduced positive signs [PANSS (positive and negative syndrome scale) positive, PANSS total, CGI (clinical global impression) scales] without any significant safety alerts. Unlike the positive olanzapine control, vabicaserin was not associated with weight gain. The current clinical status of this drug is unclear. Various other 5-HT2C receptor agonists have entered and likely been withdrawn from clinical development with little publicly disclosed information, including ATHX-105 (Athersys), whereas newer 5-HT2C agonists are beginning to emerge

    Now that lorcaserin is on the market, it seems inevitable that investigator-initiated studies will test this approach. An immediate appeal for lorcaserin is that it would likely prevent any weight-gain associated with smoking cessation.However, even though the medical need is great and the market size large.

    Nonetheless, as the first clinically approved 5-HT2C recep-tor agonist, lorcaserin represents a viable tool for proof-of-concept studies. If positive, this could open the door for a new class of therapy to treat addiction.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

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