Synthesis of tritium labeled 30-KDa PEG and conjugation to form [3H]Pegbelfermin,Journal of Labelled Compounds and Radiopharmaceuticals

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Synthesis of tritium labeled 30-KDa PEG and conjugation to form [3H]Pegbelfermin
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2021-08-12 , DOI: 10.1002/jlcr.3940
John A Easter ₁ , Yuan Tian ₁ , Richard C Burrell ₁ , Yang Hong ₁ , Samuel J Bonacorsi ₁

Affiliation

Non-alcoholic steatohepatitis (NASH) is the most chronic liver condition in the western population and is fueled by the obesity and type 2 diabetes epidemic. Pegbelfermin (1), a PEGylated human fibroblast growth factor 21 (FGF21) analogue, has previously been shown to improve markers of metabolism and liver fibrosis in obese patients with type 2 diabetes. Radiolabeled Pegbelfermin was needed to access the accumulation of intact drug and metabolized PEG. In an effort to accomplish both goals with one labeled synthesis, the isotopic label was positioned in the PEG. A total of 21 mCi of tritium labeled Pegbelfermin was synthesized having a specific activity of 21.6 Ci/mmol for use in animal studies.

中文翻译：

合成氚标记的 30-KDa PEG 并缀合形成 [3H]Pegbelfermin

非酒精性脂肪性肝炎 (NASH) 是西方人群中最慢性的肝脏疾病，肥胖和 2 型糖尿病的流行加剧了这种疾病。 Pegbelfermin ( 1 ) 是一种聚乙二醇化人成纤维细胞生长因子 21 (FGF21) 类似物，此前已被证明可以改善患有 2 型糖尿病的肥胖患者的代谢和肝纤维化标志物。需要放射性标记的 Pegbelfermin 来获取完整药物和代谢 PEG 的积累。为了通过一次标记合成来实现这两个目标，同位素标记被定位在 PEG 中。总共合成了 21 mCi 的氚标记 Pegbelfermin，其比活性为 21.6 Ci/mmol，用于动物研究。

更新日期：2021-10-06

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