乌帕替尼

乌帕替尼
临床资料
读音	/juˌpædəˈsaɪtɪnɪb/; ew-PAD-ə-SY-ti-nib
商品名（英语：Drug nomenclature）	Rinvoq
其他名称	ABT-494
AHFS/Drugs.com	Monograph
MedlinePlus	a619051
核准状况	欧 EMA: yes; 美 DailyMed: Upadacitinib;
怀孕分级	澳: D ; Not recommended;
给药途径	口服给药
药物类别（英语：Drug class）	Janus激酶抑制剂（英语：Janus kinase inhibitor）
ATC码	L04AF03 (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; 英：处方药（℞-only） (POM); 美：处方药（℞-only）; 处方药（℞-only）;
药物动力学数据
血浆蛋白结合率	52%
药物代谢	肝脏 (CYP3A（英语：CYP3A）主, CYP2D6 辅)
代谢产物	M4, 酰基葡萄糖苷酸（英语：glucuronide）
生物半衰期	9–14 (6–15) 小时
排泄途径	基本不变，粪便（38%）和尿液（24%）
识别信息
	IUPAC命名法 (3S,4R)-3-Ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide; ;
CAS号	1310726-60-3
PubChem CID	58557659;
IUPHAR/BPS	9246;
DrugBank	DB15091 ;
ChemSpider	44210449 ;
UNII	4RA0KN46E0;
KEGG	D10994 ; D11048 ;
ChEMBL	ChEMBL3622821 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID901027919 ;
化学信息
化学式	C17H19F3N6O
摩尔质量	380.38 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1c1cnc2cnc3[nH]ccc3n12;
	InChI InChI=1S/C17H19F3N6O/c1-2-10-7-25(16(27)24-9-17(18,19)20)8-11(10)13-5-22-14-6-23-15-12(26(13)14)3-4-21-15/h3-6,10-11,21H,2,7-9H2,1H3,(H,24,27)/t10-,11+/m1/s1 ; Key:WYQFJHHDOKWSHR-MNOVXSKESA-N ;

乌帕替尼（商品名：英语：Rinvoq，台湾：锐虎），类风湿性关节炎、干癣性关节炎、异位性皮肤炎、溃疡性结肠炎、克隆氏症、僵直性脊椎炎和中轴型脊柱关节炎^[9] ^[10]。因疗效与注射类型的蛋白质大分子生物制剂相近，在台湾又通称为口服小分子标靶药物^[13]。标靶目标是JAK激酶，它与引发炎的过程有关，药物能阻断它的作用，进而控制身体的发炎反应^[10]。因此称为Janus激酶抑制剂（英语：Janus kinase inhibitor）^[9] ^[14] ^[10]。

常见副作用包括上呼吸道感染（如感冒、鼻窦炎）、恶心、咳嗽和发烧^[15] ^[16]。

乌帕替尼在2019年获得欧洲和美国的医疗使用许可^[15] ^[16]。

参考文献

^ Upadacitinib (Rinvoq) Use During Pregnancy. Drugs.com. 23 September 2019 [17 March 2020]. （原始内容存档于18 March 2020）.
^ AusPAR: Upadacitinib. Therapeutic Goods Administration (TGA). 25 August 2021 [4 September 2021]. （原始内容存档于4 September 2021）.
^ Rinvoq (Abbvie Pty Ltd). [9 November 2022]. （原始内容存档于9 November 2022）.
^ Rinvoq (Abbvie Pty Ltd). Therapeutic Goods Administration (TGA). 16 February 2023 [9 April 2023]. （原始内容存档于18 March 2023）.
^ Rinvoq Product information. Health Canada. 25 April 2012 [29 May 2022]. （原始内容存档于30 May 2022）.
^ Summary Basis of Decision (SBD) for Rinvoq. Health Canada. 23 October 2014 [29 May 2022]. （原始内容存档于31 May 2022）.
^ Regulatory Decision Summary for Rinvoq. Drug and Health Products Portal. 21 July 2023 [1 April 2024].
^ Rinvoq 15 mg prolonged-release tablets - Summary of Product Characteristics (SmPC). (emc). 1 March 2020 [22 August 2020]. （原始内容存档于27 August 2021）.
^ ^9.0 ^9.1 ^9.2 Rinvoq- upadacitinib tablet, extended release. DailyMed. 1 March 2020 [29 April 2020]. （原始内容存档于27 August 2021）.
^ ^10.0 ^10.1 ^10.2 ^10.3 Rinvoq EPAR. European Medicines Agency (EMA). 16 October 2019 [29 April 2020]. （原始内容存档于20 October 2020）.
^ ^11.0 ^11.1 Rinvoq: EPAR – Public assessment report (PDF). European Medicines Agency. 5 March 2020 [21 July 2020]. （原始内容存档 (PDF)于21 July 2020）.
^ ^12.0 ^12.1 Mohamed MF, Camp HS, Jiang P, Padley RJ, Asatryan A, Othman AA. Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Participants with Rheumatoid Arthritis. Clinical Pharmacokinetics. December 2016, 55 (12): 1547–1558. PMID 27272171. S2CID 39036534. doi:10.1007/s40262-016-0419-y.
^ 類風濕性關節炎 - 類風濕性關節炎的藥物與治療. 台湾免疫风湿疾病关怀协会. 2017-01-20 （中文（台湾））.
^ Drug Trials Snapshots: Rinvoq. U.S. Food and Drug Administration (FDA). 16 August 2019 [18 March 2020]. （原始内容存档于5 August 2020）.
^ ^15.0 ^15.1 Rinvoq. [13 September 2021]. （原始内容存档于20 October 2020）.
^ ^16.0 ^16.1 Upadacitinib Monograph for Professionals. Drugs.com. [13 September 2021]. （原始内容存档于22 August 2021）（英语）.

[Drugs.com_pregnancy-1] Upadacitinib (Rinvoq) Use During Pregnancy. Drugs.com. 23 September 2019 [17 March 2020]. （原始内容存档于18 March 2020）.

[2] AusPAR: Upadacitinib. Therapeutic Goods Administration (TGA). 25 August 2021 [4 September 2021]. （原始内容存档于4 September 2021）.

[3] Rinvoq (Abbvie Pty Ltd). [9 November 2022]. （原始内容存档于9 November 2022）.

[4] Rinvoq (Abbvie Pty Ltd). Therapeutic Goods Administration (TGA). 16 February 2023 [9 April 2023]. （原始内容存档于18 March 2023）.

[5] Rinvoq Product information. Health Canada. 25 April 2012 [29 May 2022]. （原始内容存档于30 May 2022）.

[6] Summary Basis of Decision (SBD) for Rinvoq. Health Canada. 23 October 2014 [29 May 2022]. （原始内容存档于31 May 2022）.

[7] Regulatory Decision Summary for Rinvoq. Drug and Health Products Portal. 21 July 2023 [1 April 2024].

[8] Rinvoq 15 mg prolonged-release tablets - Summary of Product Characteristics (SmPC). (emc). 1 March 2020 [22 August 2020]. （原始内容存档于27 August 2021）.

[Rinvoq_FDA_label-9] 9.0 ^9.1 ^9.2 Rinvoq- upadacitinib tablet, extended release. DailyMed. 1 March 2020 [29 April 2020]. （原始内容存档于27 August 2021）.

[Rinvoq_EPAR-10] 10.0 ^10.1 ^10.2 ^10.3 Rinvoq EPAR. European Medicines Agency (EMA). 16 October 2019 [29 April 2020]. （原始内容存档于20 October 2020）.

[AssessmentReport-11] 11.0 ^11.1 Rinvoq: EPAR – Public assessment report (PDF). European Medicines Agency. 5 March 2020 [21 July 2020]. （原始内容存档 (PDF)于21 July 2020）.

[Eslam-12] 12.0 ^12.1 Mohamed MF, Camp HS, Jiang P, Padley RJ, Asatryan A, Othman AA. Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Participants with Rheumatoid Arthritis. Clinical Pharmacokinetics. December 2016, 55 (12): 1547–1558. PMID 27272171. S2CID 39036534. doi:10.1007/s40262-016-0419-y.

[13] 類風濕性關節炎 - 類風濕性關節炎的藥物與治療. 台湾免疫风湿疾病关怀协会. 2017-01-20 （中文（台湾））.

[FDA_snapshot-14] Drug Trials Snapshots: Rinvoq. U.S. Food and Drug Administration (FDA). 16 August 2019 [18 March 2020]. （原始内容存档于5 August 2020）.

[EPAR2021-15] 15.0 ^15.1 Rinvoq. [13 September 2021]. （原始内容存档于20 October 2020）.

[AHFS2021-16] 16.0 ^16.1 Upadacitinib Monograph for Professionals. Drugs.com. [13 September 2021]. （原始内容存档于22 August 2021）（英语）.

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