Taspoglutide是什么
WebTaspoglutide是为治疗2型糖尿病而开发的长效GLP-1受体激动剂,EC50值为0.06nM。 … WebTaspoglutide is a long-acting glucagon-like peptide 1 ( GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC50 value of 0.06 nM. Taspoglutide (R1583/BIM51077) is a long acting 10% formulation of (Aib8-35) human GLP-1 (7-36 amides) with 93% homology with the native polypeptide. It activates the GLP-1 receptor.
Taspoglutide是什么
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WebDec 28, 2024 · The linkers allowed tuning the taspoglutide release over more than one order of magnitude providing stable serum levels from ~0.08 to 3 μmol/L for ~20 h. Amylin and pramlintide levels were ~20 nmol/L and stable for at least 24 h. Importantly, all peptide therapeutics were protected against proteolytic degradation within the prodrug, especially ... WebJun 1, 2010 · To determine whether the modified peptide had activity at the hGLP-1R, the effect of hGLP-1 and taspoglutide on cAMP accumulation in CHO cells expressing hGLP-1R was determined ().The EC 50 obtained for hGLP-1 was consistent with that reported previously (), suggesting that the recombinant human receptor expressed in CHO-K1 …
WebJul 1, 2012 · More than half of the patients treated with taspoglutide 10 mg (58.5%) and taspoglutide 20 mg (54.9%) experienced both a loss in body weight and a reduction in HbA1c compared with only 26.6% of patients in the placebo group (Fig. 3B). Anthropometric measures (waist and hip circumference and waist to hip ratio) were similar across …
WebTaspoglutide is closely similar to natural GLP-1 analog with presence of Aib at positions 2 and 29 (Fig. 5).These modifications provided stability to DPP-4 and other plasma enzymes such as kallikerin and plasmin. In phase 3 studies the sustained release formulation of taspoglutide showed very good profile with consistent HbA1c reductions, however … WebJul 17, 2008 · Patients will be randomized to receive taspoglutide (10mg once weekly or 10mg once weekly for 4 weeks followed by 20mg once weekly) or exenatide (5 micrograms twice daily for 4 weeks followed by 10 micrograms twice daily) in a ratio of 1:1:1 in addition to continued prestudy metformin and thiazolidinedione either alone or in combination. The ...
WebJul 13, 2024 · His7, Aib8, Glu9, and Thr11 of semaglutide and taspoglutide form …
WebDec 9, 2014 · Key points. Taspoglutide was being developed as a once-weekly GLP-1 receptor agonist. In a head-to-head study with exenatide twice-daily, taspoglutide was more effective in reducing HbA 1c, with similar effects on weight. An unexpectedly high number of adverse events in Phase 3 trials, including gastrointestinal symptoms and … lyle wayne whitworthTaspoglutide is a former experimental drug, a glucagon-like peptide-1 agonist (GLP-1 agonist), that was under investigation for treatment of type 2 diabetes and being codeveloped by Ipsen and Roche. Initially, phase II trials reported it was effective and well tolerated. Of the eight planned phase III clinical … See more Taspoglutide is the peptide with the sequence H2N-His-2-methyl-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-2-methyl-Ala-Arg-CONH2. See more • Incretin See more king transport trackingWebNational Center for Biotechnology Information lyle washington stateWebJun 1, 2010 · To determine whether the modified peptide had activity at the hGLP-1R, the … lyle wa weather 1 dayWebFeb 10, 2012 · Taspoglutide is a human glucagon-like peptide 1 analog with a pharmacokinetic profile suitable for once-weekly subcutaneous administration ().In a phase 2 clinical trial, once-weekly taspoglutide added to metformin lowered HbA 1c by up to 1%, reduced body weight, and was generally well tolerated ().The efficacy and safety of … lyle washington d.cWebTaspoglutide is a long-acting glucagon-like peptide 1 ( GLP-1) receptor agonist … lyle washington wineriesWebFeb 20, 2024 · 例如，降糖药他司鲁泰（Taspoglutide）是基于人类序列的GLP-1类似物，因严重的超敏反应（发生概率不足1%）而终止研发[31]。 另外，药物的给药途径可能影响其免疫原性，虽然给药途径不能直接改变多肽或蛋白的免疫原性特性，但它可以增加具有免疫原性 … king transport inc