163451-81-8
基本信息
特立氟胺雜質(zhì)
特瑞氟米特雜質(zhì)
來氟米特雜質(zhì)1
來氟米特EP雜質(zhì)B
來氟米特歐洲藥典雜質(zhì)B
A 1726:特立氟胺
來氟米特雜質(zhì)B(EP/BP)
來氟米特雜質(zhì)B(EP) 標(biāo)準(zhǔn)品
來氟米特相關(guān)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
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
應(yīng)用領(lǐng)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.
常見問題列表
2018年7月23日之前,中國的復(fù)發(fā)緩解型多發(fā)性硬化患者只能皮下或者肌肉注射β-干擾素預(yù)防復(fù)發(fā)。2018年7月24日以后,中國患者可以免受皮肉之苦,通過口服特立氟胺來預(yù)防疾病復(fù)發(fā)。特立氟胺的商品名為奧巴捷。
據(jù)賽諾菲2020年財(cái)報(bào)顯示,Aubagio上市后銷售額持續(xù)增長達(dá)20.45億歐元,兒科適應(yīng)癥的獲批有望成為Aubagio銷售額新的增長動力。
值得關(guān)注的是,2020年8月,該藥又在中國獲批用于治療臨床孤立綜合征(CIS)。目前特立氟胺已納入國家醫(yī)保乙類目錄。
在國內(nèi),南京海納制藥和盛世泰科醫(yī)藥于2020年3月聯(lián)合提交了特立氟胺片(新4類)的上市申請,并以“罕見病治療藥”為由納入優(yōu)先評審程序,歷時(shí)近兩年,首仿獲批、首家視同過評。
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.