163451-81-8
163451-81-8 结构式
基本信息
特立氟胺杂质
特瑞氟米特杂质
来氟米特杂质1
来氟米特EP杂质B
来氟米特欧洲药典杂质B
A 1726:特立氟胺
来氟米特杂质B(EP/BP)
来氟米特杂质B(EP) 标准品
来氟米特相关化合物B(USP)
HMR 1726
Flucyamide
Teriflunomide(b)
Leflunomide Impurity B
A77 1726 (Teriflunomide)
LeflunoMide EP IMpurity B
A-771726
A 771726
A771726
(2Z)-2-Cyano-3-hydroxy-N-[4-(triflu
A-771726
A 77-1726
A771726
HMR-1726
物理化学性质
应用领域
Teriflunomide is the active metabolite of leflunomide. Teriflunomide is an immunomodulatory drug inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase. It is uncertain whether this explains its effect on MS lesions. Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. It has been found that teriflunomide blocks the transcription factor NF-κB.
常见问题列表
2018年7月23日之前，中国的复发缓解型多发性硬化患者只能皮下或者肌肉注射β-干扰素预防复发。2018年7月24日以后，中国患者可以免受皮肉之苦，通过口服特立氟胺来预防疾病复发。特立氟胺的商品名为奥巴捷。
据赛诺菲2020年财报显示，Aubagio上市后销售额持续增长达20.45亿欧元，儿科适应症的获批有望成为Aubagio销售额新的增长动力。
值得关注的是，2020年8月，该药又在中国获批用于治疗临床孤立综合征（CIS）。目前特立氟胺已纳入国家医保乙类目录。
在国内，南京海纳制药和盛世泰科医药于2020年3月联合提交了特立氟胺片（新4类）的上市申请，并以“罕见病治疗药”为由纳入优先评审程序，历时近两年，首仿获批、首家视同过评。
Teriflunomide primarily acts as an inhibitor of dihydroorotate dehydrogenase (DHODH), a key mitochondrial enzyme involved in the de novo synthesis of pyrimidines in rapidly proliferating cells. By reducing the activity of high-avidity proliferating T lymphocytes and B lymphocytes, teriflunomide likely attenuates the inflammatory response to autoantigens in MS. Thus, teriflunomide can be considered a cytostatic rather than a cytotoxic drug to leukocytes.
Teriflunomide has demonstrated beneficial effects in two independent animal models of demyelinating disease. In the dark agouti rat model of experimental autoimmune encephalitis (EAE), teriflunomide administration results in clinical, histopathological, and electrophysiological evidence of efficacy both as a prophylactic and therapeutic agent. Similarly, in the female Lewis rat model of EAE, teriflunomide administration results in beneficial prophylactic and therapeutic clinical effects, with a delay in disease onset and symptom severity.