巴瑞替尼

化合物

巴瑞替尼(英語:Baricitinib),商品名愛滅炎(英語:Olumiant),是一种口服[8]免疫调节藥物,用於類風濕性關節炎圓禿新冠肺炎[6] [7] [9] [10]。它會抑制JAK激酶的兩個亞型(Janus激酶1英语Janus kinase 1Janus激酶2英语Janus kinase 2),同屬Janus激酶抑制剂英语Janus kinase inhibitor[11]

巴瑞替尼
臨床資料
商品名英语Drug nomenclatureOlumiant, others
其他名稱INCB28050, LY3009104
AHFS/Drugs.comMonograph
MedlinePlusa618033
核准狀況
懷孕分級
  • : D [1][2]
  • Use is contraindicated
给药途径口服给药
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度79%
血漿蛋白結合率50%
药物代谢CYP3A4 (<10%)
生物半衰期12.5 hours
排泄途徑75%尿液、20%糞便
识别信息
  • 2-[1-Ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile
CAS号1187594-09-7
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB配體ID
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.219.080 編輯維基數據鏈接
化学信息
化学式C16H17N7O2S
摩尔质量371.42 g·mol−1
3D模型(JSmol英语JSmol
  • CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1
  • InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)
  • Key:XUZMWHLSFXCVMG-UHFFFAOYSA-N

常见副作用包括恶心、上呼吸道感染带状疱疹单纯疱疹[12]。其他副作用包括可能严重感染、淋巴瘤血栓腸胃穿孔和肝脏问题[12]。尚无足夠研究證實药物在在孕期使用,在动物研究發現对婴儿可能造成伤害[12]

巴瑞替尼分別于2017年和2018年,在欧洲及美國獲得醫療使用許可[8] [6]

參考文獻

  1. ^ 1.0 1.1 Olumiant Product Information (PDF). Therapeutic Goods Administration英语Therapeutic Goods Administration (TGA). [12 June 2021]. (原始内容存档于20 September 2021). 
  2. ^ Baricitinib (Olumiant) Use During Pregnancy. Drugs.com. 8 November 2019 [16 March 2020]. (原始内容存档于26 June 2020). 
  3. ^ AusPAR: Baricitinib. Therapeutic Goods Administration英语Therapeutic Goods Administration (TGA). 20 May 2021 [11 June 2021]. (原始内容存档于20 May 2021). 
  4. ^ Summary Basis of Decision (SBD) for Olumiant. 加拿大衛生部. 23 October 2014 [29 May 2022]. (原始内容存档于31 May 2022). 
  5. ^ Regulatory Decision Summary for Olumiant. Drug and Health Products Portal. 26 January 2024 [2 April 2024]. 
  6. ^ 6.0 6.1 6.2 Olumiant- baricitinib tablet, film coated. DailyMed. 13 November 2019 [16 March 2020]. (原始内容存档于27 September 2020). 
  7. ^ 7.0 7.1 Olumiant EPAR. European Medicines Agency (EMA). 3 December 2019 [17 March 2020]. (原始内容存档于25 August 2021). 
  8. ^ 8.0 8.1 Olumiant EPAR. European Medicines Agency (EMA). 3 December 2019 [1 September 2021]. (原始内容存档于25 August 2021).  Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  9. ^ Drug Trials Snapshots: Olumiant. U.S. Food and Drug Administration (FDA). 31 May 2018 [16 March 2020]. (原始内容存档于13 December 2019). 
  10. ^ FDA Approves First Systemic Treatment for Alopecia Areata. U.S. Food and Drug Administration (FDA) (新闻稿). 13 June 2022 [13 June 2022]. (原始内容存档于14 June 2022). 
  11. ^ Summary of opinion for Olumiant (PDF). European Medicines Agency (EMA). 15 December 2016 [18 December 2016]. (原始内容存档 (PDF)于15 March 2018). 
  12. ^ 12.0 12.1 12.2 Baricitinib Monograph for Professionals. Drugs.com. [8 January 2022]. (原始内容存档于21 September 2021) (英语).