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              2012年12月FDA批準新藥帕斯瑞肽pasireotide治療庫興氏病
              2013-01-10 10:08:08 來源:有機化學網 瀏覽:6111

               

              美國FDA 2012年12月14日批準治療庫興氏病新藥(帕斯瑞肽)pasireotide diasparate

                莫菲特癌癥中心(Moffitt Cancer Center)的研究員及其國際研究小組的同事,報道了一項有關諾華(Novartis)實驗性新型多受體靶向性生長抑素類似物(somatostatin analogue)pasireotide(SOM230)研究的結果。
                這項II期、開放標簽、多中心研究,在奧曲肽LAR療法(octreotide LAR)不再響應的晚期神經內分泌腫瘤(neuroendocrine tumors,NET)患者中開展,研究結果表明,pasireotide能夠有效地控制患者的癥狀,同時具有良好的耐受性。
                該項研究的結果發表于最新一期的《內分泌相關癌癥》(Endocrine-Related Cancer)上。
                “NET通常無癥狀(asymptomatic),在確診時,往往已經發生轉移,通常是轉移至肝臟,”研究的通訊作者、莫菲特研究員、神經內分泌腫瘤科主任Larry K.Kvols醫師說道。“手術在轉移性NET管理中至關重要,對于早期疾病有望治愈,但多數患者需要進一步的治療。”
                根據Kvols,奧曲肽(octreotide)和蘭瑞肽(lanreotide)是2種類似于天然生長抑素的藥物,已成為NET癥狀管理中的“中流砥柱(the mainstay)”。然而,許多患者最終對這些藥物不再響應,預后很差。
                “pasireotide是一種新型多受體靶向性生長抑素類似物,能夠結合5種已知生長抑素受體亞型中的4種,”Kvols說道。“由于其結合能力,pasireotide可能改善對傳統療法不再響應的NET患者的癥狀。

              Name:  Pasireotide
               
              CAS#:  396091-73-9. 

              Synonym:   Pasireotide;  SOM230; SOM-203

              IUPAC/Chemical name: 

              (3S,6R,9S,12S,15S,19R,20aS)-6-((1H-indol-3-yl)methyl)-9-(4-aminobutyl)-15-benzyl-12-(4-(benzyloxy)benzyl)-1,4,7,10,13,16-hexaoxo-3-phenylicosahydropyrrolo[1,2-a][1,4,7,10,13,16]hexaazacyclooctadecin-19-yl (2-aminoethyl)carbamate

              Chemical Formula: C58H66N10O9

              Exact Mass: 1046.50142

              Molecular Weight: 1047.21

              Elemental Analysis: C, 66.52; H, 6.35; N, 13.38; O, 13.75
               
              Chemical structure

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