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Arena Pharmaceuticals, Inc. Message Board

jeremiahthirtythreeone 2 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

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