部份中文非戈替尼处方资料（仅供参考）
英文名：Filgotinib Maleate
商品名：Jyseleca tablets
中文名：非戈替尼片
生产商：吉利德 药业
药品简介
2020年11月24日，新药Jyseleca（filgotinib）在日本推出，该药是一种新的、每日口服一次的、选择性JAK1抑制剂，用于治疗对常规疗法应答不足的类风湿性关节炎（RA）成人患者，包括预防结构性关节损伤。
据估计，日本有60-100万RA患者。虽然RA治疗在进步，但许多患者仍然没有获得充分的疾病缓解，仍然存在着显着的未满足医疗需求。Jyseleca的上市，将为该地区RA患者群体提供一种新的治疗选择。
ジセレカ錠200mg／ジセレカ錠100mg
药效分类名称
口服JAK1优先抑制剂
批准日期：2020年10月9日
商品名：
Jyseleca tablets
一般的名称
フィルゴチニブマレイン酸塩（Filgotinib Maleate）［JAN］
化学名
N-(5-{4-[(1,1-Dioxo-λ6-thiomorpholin-4-yl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide monomaleate
分子式
C21H23N5O3S・C4H4O4
分子量
541.58
性状
白色至微黄白色固体
化学構造式
融点
約237℃（フィルゴチニブ遊離塩基として）
分配係数
Log P=1.4（1-オクタノール/pH7.4のリン酸塩緩衝液）
溶解性
它微溶于二甲亚砜或 N-甲基吡咯烷酮，微溶于二甲基甲酰胺，微溶于四氢呋喃或甲醇，极微溶于乙醇 (95)、丙酮、2-丙醇或乙腈。
审批条件
<常见效果>
制定药品风险管理计划并妥善实施。
<类风湿性关节炎>
在生产和销售后，直到收集到一定数量的病例数据，我们将对所有病例进行用药结果调查，以尽早收集有关该药物的安全性和有效性的数据。采取必要措施正确使用这种药。
<溃疡性结肠炎>
由于日本的临床试验病例数极为有限，因此可以通过对制造和销售后的所有病例进行药物使用结果调查，直到积累一定数量的病例数据来使用该药物。使用本药的患者，及早收集本药的安全性和有效性数据，并采取必要措施正确使用本药。
药效药理
作用机制
Filgotinib是一种选择性和可逆的三磷酸腺苷(ATP)竞争性Janus激酶(JAK)抑制剂。JAK是一种细胞内酶，可将细胞因子或生长因子-受体相互作用产生的信号传递至细胞膜，并影响造血、细胞因子信号传导和免疫细胞功能的细胞过程。在信号通路中，JAK磷酸化并激活调节细胞内活动（包括基因表达）的信号和转录激活因子(STAT)。Filgotinib通过抑制STAT的磷酸化和活化来调节信号通路。
JAK抑制活性
在生化试验中，丝氨酸替尼抑制JAK1、JAK2、JAK3和TYK2，IC50分别为10-53nmol/L、28-70nmol/L、311-810 nmol/L和116-177nmol/L。在细胞试验中，filgotinib抑制JAK1介导的各种 STAT 磷酸化，IC5​​0为 179-3364 nmol/L。在细胞因子和生长因子刺激的全血测定中，丝氨酸可抑制STAT1的JAK1依赖性磷酸化和 STAT3或STAT5的JAK2依赖性磷酸化，IC5​​0分别为506至1180nmol/L和7118至17453 nmol/L。filgotinib的主要代谢物GS-829845在体外的活性约为filgotinib的1/10，但显示出相似的JAK选择性。
对胶原诱导的关节炎模型的抑制作用
Filgotinib在大鼠胶原诱导的关节炎模型中剂量依赖性地抑制炎症评分、足垫水肿、Larsen评分和跟骨侵蚀。
对肠道炎症模型的抑制作用
Filgotinib在小鼠硫酸葡聚糖诱导的肠道炎症模型和T细胞过继模型中改善了体重、粪便僵硬、肠道出血和结肠炎症的组织病理学炎症特征，并抑制了肠道炎症。
适应症
○现有治疗方法不足的类风湿性关节炎（包括预防关节结构性损伤）
○中度至重度溃疡性结肠炎的治疗和维持治疗（仅在现有治疗不充分的情况下）
用法与用
<类风湿性关节炎>
通常的成人剂量是每天一次口服 200mg filgotinib。此外，根据患者的情况，可以每天服用一次100毫克。
<溃疡性结肠炎>
通常的成人剂量是每天一次口服 200mg filgotinib。在维持治疗中，根据患者的情况，可以每天服用一次100毫克。
包装
片剂
200mg：14片（14片x 1）PTP
100mg：14片（14片x 1）PTP
制造商和分销商
吉利德科学有限公司
销售
卫材有限公司
プロモーション提携
EAファーマ株式会社
注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明资料附件：
https://www.info.pmda.go.jp/go/pack/3999053F1023_1_03/
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JYSELECA Tablets 200mg（Filgotinib maleate）
Active ingredient:Filgotinib maleate
Dosage form:pale brown tablet, major axis: approx. 17mm, minor axis: approx. 8mm,thickness: approx.6.6 mmImprint or print on wrapping:
(Face) ジセレカ錠 200mg, ジセレカ GSI 200
(Back)Jyseleca 200mg, ジセレカ 200mg
Effects of this medicine
This medicine affects the action of several substances associated with expression of inflammation or pain by inhibiting the activity of an enzyme called Janus Kinase (JAK), thereby showing improvement on symptoms of rheumatoid arthritis or ulcerative colitis.
It is usually used to treat rheumatoid arthritis with inadequate response to conventional therapies (including prevention of structural joint damage). It is also used to treat moderate to severe ulcerative colitis (only in the case with inadequate response to conventional therapies) and as its maintenance therapy.
The following patients may need to be careful when using this medicine.
Be sure to tell your doctor and pharmacist.
If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines or foods.
If you have infections (pneumonia, sepsis, viral infection, etc.), active tuberculosis, renal dysfunction, liver dysfunction, decreased neutrophils, decreased lymphocyte, decreased hemoglobin, hepatitis B or a history of herpes zoster.
If you are pregnant, possibly pregnant or breastfeeding.
If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
Your dosing schedule prescribed by your doctor is ((to be written by a healthcare professional))
Rheumatoid arthritis: In general, for adults, take 1 tablet (200 mg of filgotinib) at a time, once a day. The dosage may be decreased to 100 mg at a time, once a day, according to your condition.
Ulcerative colitis: In general, for adults, take 1 tablet (200 mg of filgotinib) at a time, once a day. For maintenance therapy, the dosage may be decreased to 100 mg at a time, once a day, according to your conditions.
In any case, strictly follow the instructions.
If you miss a dose, take the missed dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time.
If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
If you have a childbearing potential, use birth control to avoid pregnancy while using this medicine and for a certain period after the completion of the therapy with this medicine.
This medicine may cause impaired spermatogenesis and reduced fertility in men.
You should routinely undergo laboratory tests such as chest X-ray while using this medicine in order to monitor for tuberculosis infection.
This medicine may cause decreased neutrophils, decreased lymphocyte, decreased hemoglobin level or abnormal lipid level. You should routinely undergo blood test, including before treatment initiation.
For healthcare professional use only
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include nausea, upper respiratory infection, bronchitis, epipharyngitis, urinary tract infection, headache, constipation, upper abdominal pain and diarrhea. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, see your doctor immediately.
rash with painful small blisters appearing in a belt-like shape, fever, chills, malaise[infection]
severe abdominal pain, nausea, vomiting[perforation of digestive tract]
sudden high fever, sore throat, malaise, dizziness, headache[decreased neutrophils, decreased lymphocyte, decreased hemoglobin]
malaise, loss of appetite, nausea[liver dysfunction]
fever, cough, breathing difficulty[interstitial lung disease]
fever, skin turning blueish purple or dark purple, pain in lower limbs[venous thromboembolism]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.
Storage conditions and other information
Do not receive live vaccines (such as BCG, measles, rubella, measles-rubella (MR), chicken pox and mumps vaccines) while using this medicine. If you wish to receive vaccination, consult with your doctor.
Keep out of the reach of children. Store away from direct sunlight, heat and moisture.
Discard the remainder. Do not store them. Ask the pharmacy and the medical institution how to discard them.
Gilead Sciences K. K.
Revised: 06/2022
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.