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Arena Pharmaceuticals, Inc. Message Board

jeremiahthirtythreeone 7 posts  |  Last Activity: Apr 8, 2016 1:25 PM Member since: Feb 16, 2010
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  • FDA - new warnings to the affected drug labels about safety risk to:
    • Onglyza (saxagliptin; AstraZeneca)
    • Kombiglyze XR (saxagliptin/metformin ext-rel; AstraZeneca)
    • Nesina (alogliptin; Takeda)
    • Kazano (alogliptin/metformin; Takeda)
    • Oseni (alogliptin/pioglitazone; Takeda)

    Two large trials (SAVOR and EXAMINE) demonstrated that more patients who who recieved saxagliptin- or alogliptin containing drugs were hospitalized for heart failure vs patients receiving placebo.

    A big pharma (?AstraZeneca) or partner could come in and perform a large 6 month study to verify the BLOOM-DM results because:
    Belviq+metformin is much safer and has about same efficacy in decreasing HgbA1C with the added benefit of weight loss. Again, Belviq improves glucose homeostasis by a mechanism apart from weight loss.

    Somehow Arena management have missed the boat on this one!!!

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • This very important study's conclusion is "the potential for metabolic drug-drug interaction or toxicological effects of lorcaserin N-sulfamate is remote in a normal patient population."
    Identification of Human Sulfotransferases Involved in Lorcaserin N-Sulfamate Formation.
    Abstract
    Lorcaserin [(R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine] hydrochloride hemihydrate, a selective serotonin 5-hydroxytryptamine (5-HT) 5-HT2C receptor agonist, is approved by the U.S. Food and Drug Administration for chronic weight management. Lorcaserin is primarily cleared by metabolism, which involves multiple enzyme systems with various metabolic pathways in humans. The major circulating metabolite is lorcaserin N-sulfamate. Both human liver and renal cytosols catalyze the formation of lorcaserin N-sulfamate, where the liver cytosol showed a higher catalytic efficiency than renal cytosol. Human sulfotransferases (SULTs) SULT1A1, SULT1A2, SULT1E1, and SULT2A1 are involved in the formation of lorcaserin N-sulfamate.. Inhibitory effects of lorcaserin N-sulfamate on major human cytochrome P450 (P450) enzymes were not observed or minimal. Lorcaserin N-sulfamate binds to human plasma protein with high affinity (i.e., 99%). Thus, despite being the major circulating metabolite, the level of free lorcaserin N-sulfamate would be minimal at a lorcaserin therapeutic dose and unlikely be sufficient to cause drug-drug interactions. Considering its formation kinetic parameters, high plasma protein binding affinity, minimal P450 inhibition or induction potential, and stability, the potential for metabolic drug-drug interaction or toxicological effects of lorcaserin N-sulfamate is remote in a normal patient population.
    Citation
    Identification of Human Sulfotransferases Involved in Lorcaserin N-Sulfamate Formation. Sadeque AJ, Palamar S, Usmani KA, Chen C, Cerny MA, Chen WG, - Drug Metab. Dispos. - April 1, 2016; 44 (4); 570-5
    MEDLINE

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • 1. Massachusetts General Hospital, Boston
    2. Mayo Clinic, Rochester, Minnesota
    3. Johns Hopkins Hospital, Baltimore, Maryland
    3. UCLA Medical Center, Los Angeles
    5. Cleveland Clinic, Ohio
    6. Brigham and Women's Hospital, Boston, Massachusetts
    7. New York-Presbyterian University Hospital of Columbia and Cornell, New York City
    8. UCSF Medical Center, San Francisco
    9. Hospitals of the University of Pennsylvania-Penn Presbyterian, Philadelphia
    10. Barnes-Jewish Hospital/Washington University, St. Louis, Missouri
    11. Northwestern Memorial Hospital, Chicago, Illinois
    12. NYU Langone Medical Center, New York City
    13. UPMC-University of Pittsburgh Medical Center, Pennsylvania
    14. Duke University Hospital, Durham, North Carolina
    15. Stanford Health-Stanford Hospital, Stanford, California

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • Reply to

    Ralinepag's STEALING THE SHOW, by-Stockvadar

    by stockvadar Jul 24, 2015 9:59 AM
    jeremiahthirtythreeone jeremiahthirtythreeone Jul 24, 2015 12:10 PM Flag

    Yes, and UCLA was recently ranked the third best hospital in the nation, tide with John Hopkins.
    Thanks Sharon

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • Reply to

    Ralinepag's STEALING THE SHOW, by-Stockvadar

    by stockvadar Jul 24, 2015 9:59 AM
    jeremiahthirtythreeone jeremiahthirtythreeone Jul 24, 2015 11:03 AM Flag

    PAH prognosis:
    Goldman-Cecil Medicine, Twenty-Fifth Edition
    Goldman, Lee, MD
    Copyright © 2016

    Prognosis
    Several clinical factors are correlated with prognosis The natural history of symptomatic idiopathic pulmonary arterial hypertension is a median survival of 2.8 years with 1-, 3-, and 5-year survival rates of 68%, 48%, and 34%, respectively. In the era of targeted therapies, survival has improved but still remains suboptimal, with 1-, 2-, and 3-year survival of 86%, 70%, and 55% for incident cases.
    Pulmonary hypertension itself is the direct cause of death in about 50% of patients and contributes to but does not directly cause death in the other 50%.

    This is why there may be some basis to stockvadar's post.
    It's only a matter of time

    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • Reply to

    Eisai Japan Belviq XR

    by sharonconk Jul 23, 2015 8:31 AM
    jeremiahthirtythreeone jeremiahthirtythreeone Jul 24, 2015 10:31 AM Flag

    Thank you Sharon for your diligence!!
    Daniel
    UCLA MD

    Sentiment: Strong Buy

  • jeremiahthirtythreeone by jeremiahthirtythreeone Jun 28, 2015 9:08 AM Flag

    US Obese Now Overtake the Merely Overweight

    120 million Americans affected by obesity and overweight and Arena/Eisai cannot and does not appear to know how to address the problem with a proper and aggressive marketing approach. The need is clearly there and it is a huge -pardon the pun-need which has not be solved despite millions of dollars spent on diet and exercise awareness. Hopefully there is a big pharma who understands this potential

    MEDSCAPE June 25, 2015

    More Americans are now obese than are overweight, say researchers, who base this new conclusion on a reanalysis of data from the National Health and Nutrition Examination Survey (NHANES).

    They estimate that 67.6 million Americans over the age of 25 are obese and an additional 65.2 million are overweight.

    The finding shows the urgent need for government action that could improve Americans' diets and physical activity, coauthor Lin Yang, PhD, from the division of public-health sciences, Washington University, in Saint Louis, Missouri, told Medscape Medical News.

    "We really need the environment and support for people to keep their healthy behaviors sustainable," said Dr Yang.

    Dr Yang and her colleague, Graham A Colditz, MD, PhD, published the new data as a research letter June 22 in JAMA Internal Medicine

    They estimate that the proportion of women who are overweight or obese increased from 55% in the 1988–1994 NHANES to 63% in an aggregate of NHANES from 2007 to 2012. The figures for overweight or obese men went from 63% to 75%, they said.

    Daniel
    UCLA MD

    Sentiment: Strong Buy

ARNA
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