Sotatercept (ACE-011) 是一种可溶性激活素受体 2A (ACVR2A) 型 IgG Fc 融合蛋白。Sotatercept 结合了激活素和生长分化因子，试图恢复生长促进和生长抑制信号通路之间的平衡。Sotatercept 在肺动脉高压、贫血、骨质流失、红细胞生成、多发性骨髓瘤 (MM) 溶骨性病变中有潜在的应用。
Sotatercept (ACE-011) is a soluble activin receptor 2A (growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial pertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions[1][2][3][4][5].
Sotatercept (100 μg/mL) 下调了基质细胞分泌的 VEGF、抑瘤素 M (OSM)、IL-6、BMP-2、MMP-1 和 MMP13 表达水平[5]。
[1]. Humbert M, et al. Sotatercept for the Treatment of Pulmonary Arterial pertension. N Engl J Med. 2021 Apr 1;384(13):1204-1215.
[2]. Raje N, et al. Sotatercept, a soluble activin receptor type 2A IgG-Fc fusion protein for the treatment of anemia and bone loss. Curr Opin Mol Ther. 2010 Oct;12(5):586-97.
[3]. Abdulkadyrov KM, et al. Sotatercept in patients with osteolytic lesions of multiple myeloma. Br J Haematol. 2014 Jun;165(6):814-23.
[4]. Sherman ML, et al. Multiple-dose, safety, pharmacokinetic, and pharmacodynamic study of sotatercept (ActRIIA-IgG1), a novel erythropoietic agent, in healt postmenopausal women. J Clin Pharmacol. 2013 Nov;53(11):1121-30.
[5]. Iancu-Rubin C, et al. Stromal cell-mediated inhibition of erythropoiesis can be attenuated by Sotatercept (ACE-011), an activin receptor type II ligand trap. Exp Hematol. 2013 Feb;41(2):155-166.e17.
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