巴瑞替尼

巴瑞替尼
临床资料
商品名（英语：Drug nomenclature）	Olumiant, others
其他名称	INCB28050, LY3009104
AHFS/Drugs.com	Monograph
MedlinePlus	a618033
核准状况	美 DailyMed: Baricitinib;
怀孕分级	澳: D ; Use is contraindicated;
给药途径	口服给药
ATC码	L04AF02 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 加：处方药（℞-only）; 欧：Rx-only; 美：处方药（℞-only）; 处方药（℞-only）;
药物动力学数据
生物利用度	79%
血浆蛋白结合率	50%
药物代谢	CYP3A4 (<10%)
生物半衰期	12.5 hours
排泄途径	75%尿液、20%粪便
识别信息
	IUPAC命名法 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	44205240;
DrugBank	DB11817;
ChemSpider	26373084;
UNII	ISP4442I3Y;
KEGG	D10308;
ChEBI	CHEBI:95341;
ChEMBL	ChEMBL2105759;
PDB配体ID	3JW (PDBe, RCSB PDB);
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID30152228 ;
ECHA InfoCard	100.219.080
化学信息
化学式	C16H17N7O2S
摩尔质量	371.42 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3ncnc4[nH]ccc34)cn2)C1;
	InChI 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;

巴瑞替尼（英语：Baricitinib），商品名爱灭炎（英语：Olumiant），是一种口服^[8]的免疫调节药物，用于类风湿性关节炎、圆秃和新冠肺炎^[6] ^[7] ^[9] ^[10]。它会抑制JAK激酶的两个亚型（Janus激酶1（英语：Janus kinase 1）和Janus激酶2（英语：Janus kinase 2）），同属Janus激酶抑制剂（英语：Janus kinase inhibitor）^[11]。

常见副作用包括恶心、上呼吸道感染、带状疱疹和单纯疱疹^[12]。其他副作用包括可能严重感染、淋巴瘤、血栓、肠胃穿孔和肝脏问题^[12]。尚无足够研究证实药物在在孕期使用，在动物研究发现对婴儿可能造成伤害^[12]。

巴瑞替尼分别于2017年和2018年，在欧洲及美国获得医疗使用许可^[8] ^[6]。

参考文献

^ ^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）.
^ Baricitinib (Olumiant) Use During Pregnancy. Drugs.com. 8 November 2019 [16 March 2020]. （原始内容存档于26 June 2020）.
^ 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）.
^ Summary Basis of Decision (SBD) for Olumiant. 加拿大卫生部. 23 October 2014 [29 May 2022]. （原始内容存档于31 May 2022）.
^ Regulatory Decision Summary for Olumiant. Drug and Health Products Portal. 26 January 2024 [2 April 2024].
^ ^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）.
^ ^7.0 ^7.1 Olumiant EPAR. European Medicines Agency (EMA). 3 December 2019 [17 March 2020]. （原始内容存档于25 August 2021）.
^ ^8.0 ^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.
^ 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）.
^ 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）.
^ 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）.
^ ^12.0 ^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）.

[Olumiant_AU_PI-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）.

[Drugs.com_pregnancy-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. 加拿大卫生部. 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].

[Olumiant_FDA_label-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）.

[Olumiant_EPAR-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）.

[EPAR2022-8] 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.

[FDA_snapshot-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）.

[FDA_PR_20220613-10] 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）.

[CHMP-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）.

[AHFS2022-12] 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）.

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