AUBAGIO(特立氟胺 teriflunomide)片获美国及欧盟批准批准上市，作为一种新的日服一次的药物，用于复发型多发性硬化症患者的治疗。
批准日期：September 12，2012；公司：Sanofi
初次批准：2012
作用机制
Teriflunomide，一种免疫调制药有抗炎性质，抑制双氢乳清酸酯脱氢酶一种涉及嘧啶的从头合成的线粒体酶。在多发性硬化症中teriflunomide发挥其治疗效应的确切机制不知道但可能涉及减少在CNS中激活的淋巴细胞数.
适应证和用途
AUBAGIO是一种嘧啶合成抑制剂适用于有多发性硬化症的复发型患者治疗。
剂量和给药方法
7mg或14mg口服每天1次，有或无食物。
剂型和规格
7mg和14mg薄膜衣片
禁忌证
严重肝受损
妊娠
当前来氟米特[leflunomide]治疗。
警告和注意事项
（1）给予考来烯胺[cholestyramine]或活性碳共11天可能加速AUBAGIO的消除
（2）AUBAGIO可能减低WBC。开始AUBAGIO前应得到最近CBC。监测感染的体征和症状。考虑暂停用AUBAGIO治疗和严重感染的情况中使用加速消除方法步骤。有活动性感染患者中不要开始AUBAGIO
（3）周围神经病变：如患者发生症状与周围神经病变一致，评价患者和考虑终止AUBAGIO和使用加速消除方法步骤。
（4）急性肾衰/高钾血症：在肾衰或高钾血症症状患者中监测肾功能和钾。
（5）严重皮肤反应：停止AUBAGIO和使用加速消除方法步骤。
（6）血压：治疗开始时测量。治疗期间适当监测和处理。
不良反应
最常见不良反应(10%和大于安慰剂2%)：ALT增加，脱发，腹泻，流感，恶心，和感觉异常。
药物相互作用
被CYP2C8代谢药物：监测患者因teriflunomide可能增加其暴露
Teriflunomide可能增加炔雌醇[ethinylestradiol]和左炔诺孕酮[levonorgestrel]的暴露。选择一种适当口服避孕药
被CYP1A2代谢药物：监测患者因teriflunomide可能减低其暴露
华法林[Warfarin]：监测INR因teriflunomide可能减低INR
特殊人群中使用
在妊娠中禁忌；得到妊娠注册
INDICATION
AUBAGIO® (teriflunomide) is indicated for the treatment of patients with relapsing forms of multiple sclerosis.
IMPORTANT SAFETY INFORMATION
WARNING: HEPATOTOXICITY AND RISK OF TERATOGENICITY
Severe liver injury including fatal liver failure has been reported in patients treated with leflunomide, which is indicated for rheumatoid arthritis. A similar risk would be expected for teriflunomide because recommended doses of teriflunomide and leflunomide result in a similar range of plasma concentrations of teriflunomide. AUBAGIO is contraindicated in patients with severe hepatic impairment and in patients taking leflunomide. Concomitant use of AUBAGIO with other potentially hepatotoxic drugs may increase the risk of severe liver injury. Obtain transaminase and bilirubin levels within 6 months before initiation of AUBAGIO therapy. Monitor ALT levels at least monthly for 6 months after starting AUBAGIO. If drug-induced liver injury is suspected, discontinue AUBAGIO and start an accelerated elimination procedure with cholestyramine or charcoal. Patients with pre-existing liver disease may be at increased risk of developing elevated serum transaminases when taking AUBAGIO.
Based on animal data, AUBAGIO may cause major birth defects if used during pregnancy. Pregnancy must be excluded before starting AUBAGIO. AUBAGIO is contraindicated in pregnant women or women of childbearing potential who are not using reliable contraception. Pregnancy must be avoided during AUBAGIO treatment or prior to the completion of an accelerated elimination procedure after AUBAGIO treatment.
Warnings and Precautions
Patients with pre-existing acute or chronic liver disease, or those with serum ALT >2 times the upper limit of normal (ULN) before initiating treatment, should not normally be treated with AUBAGIO. In clinical trials, if ALT elevation was >3 times the ULN on 2 consecutive tests, patients discontinued AUBAGIO and underwent accelerated elimination. Consider additional monitoring if co-administering AUBAGIO with other potentially hepatotoxic drugs; monitor patients who develop symptoms suggestive of hepatic dysfunction (eg, unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, or jaundice and/or dark urine).
Before starting therapy, use of reliable contraception must be confirmed, and the patient counseled on risks to the fetus. Patients with delayed onset of menses or other reason to suspect pregnancy should immediately see their physician for pregnancy testing. Patients who become pregnant or wish to become pregnant should discontinue treatment, followed by accelerated elimination until plasma concentrations of <0.02 mcg/mL are verified, a level expected to pose minimal risk to the fetus. Women who become pregnant while taking AUBAGIO may enroll in the AUBAGIO pregnancy registry by calling 1-800-745-4447, option 2.
Teriflunomide is eliminated slowly from the plasma—it takes an average of 8 months, or up to 2 years, to reach plasma concentrations <0.02 mcg/mL. Elimination may be accelerated by administration of cholestyramine or charcoal, but this may cause disease activity to return in patients who were responding to AUBAGIO.
Decreases in white blood cell counts, mainly of neutrophils and lymphocytes, and platelets have been reported with AUBAGIO. Obtain a complete blood cell count within 6 months before starting treatment, with further monitoring based on signs and symptoms of bone marrow suppression. AUBAGIO is not recommended for patients with severe immunodeficiency, bone marrow disease, or severe uncontrolled infections. Tuberculosis (TB) has been observed in clinical studies of AUBAGIO. Before starting treatment, screen patients for latent TB infection with a tuberculin test. Treatment in patients with acute or chronic infections should not be started until the infection(s) is resolved. Administration of live vaccines is not recommended. The risk of malignancy, particularly lymphoproliferative disorders, or infection may be increased with the use of some medications with immunosuppressive potential, including teriflunomide.
Peripheral neuropathy, including polyneuropathy and mononeuropathy, has been reported with AUBAGIO. Age >60 years, concomitant neurotoxic medications, and diabetes may increase the risk. If peripheral neuropathy is suspected, consider discontinuing treatment and performing accelerated elimination.
Interstitial lung disease and rare cases of Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported with leflunomide; a similar risk would be expected for teriflunomide. If a severe skin reaction develops with AUBAGIO, stop treatment and use accelerated elimination.
Blood pressure increases and hypertension have occurred with AUBAGIO. Measure blood pressure at treatment initiation and manage any elevations during treatment.
Adverse Reactions: The most frequent adverse reactions (≥10% and ≥2% greater than placebo) with AUBAGIO 7 mg and 14 mg and placebo, respectively, were headache (18% and 16% vs 15%), ALT increased (13% and 15% vs 9%), diarrhea (13% and 14% vs 8%), alopecia (10% and 13% vs 5%), and nausea (8% and 11% vs 7%).
Drug Interactions: Monitor patients when teriflunomide is coadministered with warfarin, or with drugs metabolized by CYP1A2, CYP2C8, substrates of OAT3 transporters, substrates of BCRP, or OATP1B1/1B3 transporters.
Use in Specific Populations: AUBAGIO is detected in human semen. To minimize any possible fetal risk, men not wishing to father a child and their female partners should use reliable contraception. Men wishing to father a child should discontinue therapy and undergo accelerated elimination, with verification of plasma concentrations <0.02 mcg/mL. Nursing mothers should not use AUBAGIO.
----------------------------------------
产地国家：德国
原产地英文商品名:
Aubagio 14mg/Tablet 28Tablets/box
原产地英文药品名:
Teriflunomide
中文参考商品译名:
Aubagio 14毫克／片 28片/盒
中文参考药品译名:
特立氟胺
生产厂家中文参考译名:
健赞制药
生产厂家英文名:
Genzyme

----------------------------------------
产地国家：德国
原产地英文商品名:
Aubagio 14mg/Tablet 84Tablets/box
原产地英文药品名:
Teriflunomide
中文参考商品译名:
Aubagio 14毫克／片 84片/盒
中文参考药品译名:
特立氟胺
生产厂家中文参考译名:
健赞制药
生产厂家英文名:
Genzyme

----------------------------------------
产地国家：美国
原产地英文商品名:
Aubagio 7mg/Tablet 5Tablets/box
原产地英文药品名:
Teriflunomide
中文参考商品译名:
Aubagio 7毫克／片 5片/盒
中文参考药品译名:
特立氟胺
生产厂家中文参考译名:
健赞制药
生产厂家英文名:
Genzyme
----------------------------------------
产地国家：美国
原产地英文商品名:
Aubagio 7mg/Tablet 28Tablets/box
原产地英文药品名:
Teriflunomide
中文参考商品译名:
Aubagio 7毫克／片 28片/盒
中文参考药品译名:
特立氟胺
生产厂家中文参考译名:
健赞制药
生产厂家英文名:
Genzyme

----------------------------------------
产地国家：美国
原产地英文商品名:
Aubagio 14mg/Tablet 5Tablets/box
原产地英文药品名:
Teriflunomide
中文参考商品译名:
Aubagio 14毫克／片 5片/盒
中文参考药品译名:
特立氟胺
生产厂家中文参考译名:
健赞制药
生产厂家英文名:
Genzyme
----------------------------------------
产地国家：美国
原产地英文商品名:
Aubagio 14mg/Tablet 28Tablets/box
原产地英文药品名:
Teriflunomide
中文参考商品译名:
Aubagio 14毫克／片 28片/盒
中文参考药品译名:
特立氟胺
生产厂家中文参考译名:
健赞制药
生产厂家英文名:
Genzyme