Anakinra (AMG-719, Raleukin) is a recombinant, non glycosylated human interleukin-1 receptor antagonist (IL-1Ra). It is produced using DNA recombination technology in the Escherichia coli expression system andamino acid sequence is MRPSGRKSSKMQAFRIWDVNQKTFYLRNNQLVAGYLQGPNVNLEEKIDVVPIEPHALFLGIHGGKMCLSCVKSGDETRLQLEAVNITDLSENRKQDKRFAFIRSDSGPTTSFESAACPGWFLCTAMEADQPVSLTNMPDEGVMVTKFYFQEDE. Anakinra represents the inaugural biological therapy designed to neutralize the inflammatory actions of IL-1[1][2]. Anakinra has been proven effective for the treatment of various inflammatory and autoimmune diseases, including Still's disease[3].
Anakinra was administered at a dose of 100 mg/kg via intraperitoneal injection, and the same route was used to administer Etanercept at a dose of 5 mg/kg daily for seven consecutive days, which significantly facilitated the successful implantation of marginal quality human islet cells in mice with impaired immune systems [2]. Anakinra enhances tumor growth inhibition in mice receiving peptide vaccination and treated with beta-(1-3),(1-6)-D-glucan by blocking the IL-1 receptor and reducing IL-1-induced IL-6 production[4].
References:
[1] Cvetkovic RS, et al. Anakinra. BioDrugs. 2002;16(4):303-11; discussion 313-4.
[2] McCall M, et al. Anakinra potentiates the protective effects of etanercept in transplantation of marginal mass human islets in immunodeficient mice. Am J Transplant. 2012 Feb;12(2):322-9.
[3] Vastert Sebastiaan J, et al. Anakinra in children and adults with Still's disease. Rheumatology (Oxford) 2019 Nov 1;58(Suppl 6):vi9-vi22. PMID:31769856. DOI:10.1093/rheumatology/kez350.
[4] Harnack U, et al. IL-1 receptor antagonist anakinra enhances tumour growth inhibition in mice receiving peptide vaccination and beta-(1-3),(1-6)-D-glucan. Anticancer Res. 2010 Oct;30(10):3959-65.
阿那白滞素(Anakinra)是一种重组的、非糖基化的人类白细胞介素-1受体拮抗剂（IL-1Ra）。它是利用大肠杆菌表达系统的DNA重组技术生产的，并且氨基酸序列为MRPSGRKSSKMQAFRIWDVNQKTFYLRNNQLVAGYLQGPNVNLEEKIDVVPIEPHALFLGIHGGKMCLSCVKSGDETRLQLEAVNITDLSENRKQDKRFAFIRSDSGPTTSFESAACPGWFLCTAMEADQPVSLTNMPDEGVMVTKFYFQEDE。阿那白滞素代表了首个旨在中和IL-1炎症作用的生物疗法[1][2]。阿那白滞素已被证明可用于治疗斯蒂尔病等多种炎症和自身免疫性疾病[3]。
阿那白滞素通过腹腔注射100 mg/kg，以及相同途径每日给予依那西普（Etanercept）5 mg/kg的剂量，连续7天，显著促进了在免疫系统受损的小鼠中，边缘质量的人类胰岛细胞的成功植入[2]。阿那白滞素通过阻断 IL-1 受体来减少 IL-1 诱导的 IL-6 生成，增强了接受肽疫苗接种并经β-(1-3),(1-6)-D-葡聚糖处理的小鼠中肿瘤生长的抑制[4]。