烏帕替尼

烏帕替尼
臨床資料
讀音	/juˌpædəˈsaɪtɪnɪb/; ew-PAD-ə-SY-ti-nib
商品名（英語：Drug nomenclature）	Rinvoq
其他名稱	ABT-494
AHFS/Drugs.com	Monograph
MedlinePlus	a619051
核准狀況	歐 EMA: yes; 美 DailyMed: Upadacitinib;
懷孕分級	澳: D ; Not recommended;
給藥途徑	口服給藥
藥物類別（英語：Drug class）	Janus激酶抑制劑（英語：Janus kinase inhibitor）
ATC碼	L04AF03 (WHO) ;
法律規範狀態
法律規範	澳：限醫生處方（S4）; 加：處方藥（℞-only）; 歐：Rx-only; 英：處方藥（℞-only） (POM); 美：處方藥（℞-only）; 處方藥（℞-only）;
藥物動力學數據
血漿蛋白結合率	52%
藥物代謝	肝臟 (CYP3A（英語：CYP3A）主, CYP2D6 輔)
代謝產物	M4, 酰基葡萄糖苷酸（英語：glucuronide）
生物半衰期	9–14 (6–15) 小時
排泄途徑	基本不變，糞便（38%）和尿液（24%）
識別資訊
	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號	1310726-60-3
PubChem CID	58557659;
IUPHAR/BPS	9246;
DrugBank	DB15091 ;
ChemSpider	44210449 ;
UNII	4RA0KN46E0;
KEGG	D10994 ; D11048 ;
ChEMBL	ChEMBL3622821 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID901027919 ;
化學資訊
化學式	C17H19F3N6O
摩爾質量	380.38 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	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 ;

烏帕替尼（商品名：英語：Rinvoq，台灣：銳虎），類風濕性關節炎、乾癬性關節炎、異位性皮膚炎、潰瘍性結腸炎、克隆氏症、僵直性脊椎炎和中軸型脊柱關節炎^[9] ^[10]。因療效與注射類型的蛋白質大分子生物製劑相近，在台灣又通稱為口服小分子標靶藥物^[13]。標靶目標是JAK激酶，它與引發炎的過程有關，藥物能阻斷它的作用，進而控制身體的發炎反應^[10]。因此稱為Janus激酶抑制劑（英語：Janus kinase inhibitor）^[9] ^[14] ^[10]。

常見副作用包括上呼吸道感染（如感冒、鼻竇炎）、噁心、咳嗽和發燒^[15] ^[16]。

烏帕替尼在2019年獲得歐洲和美國的醫療使用許可^[15] ^[16]。

參考文獻

^ Upadacitinib (Rinvoq) Use During Pregnancy. Drugs.com. 23 September 2019 [17 March 2020]. （原始內容存檔於18 March 2020）.
^ AusPAR: Upadacitinib. Therapeutic Goods Administration (TGA). 25 August 2021 [4 September 2021]. （原始內容存檔於4 September 2021）.
^ Rinvoq (Abbvie Pty Ltd). [9 November 2022]. （原始內容存檔於9 November 2022）.
^ Rinvoq (Abbvie Pty Ltd). Therapeutic Goods Administration (TGA). 16 February 2023 [9 April 2023]. （原始內容存檔於18 March 2023）.
^ Rinvoq Product information. Health Canada. 25 April 2012 [29 May 2022]. （原始內容存檔於30 May 2022）.
^ Summary Basis of Decision (SBD) for Rinvoq. Health Canada. 23 October 2014 [29 May 2022]. （原始內容存檔於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]. （原始內容存檔於27 August 2021）.
^ ^9.0 ^9.1 ^9.2 Rinvoq- upadacitinib tablet, extended release. DailyMed. 1 March 2020 [29 April 2020]. （原始內容存檔於27 August 2021）.
^ ^10.0 ^10.1 ^10.2 ^10.3 Rinvoq EPAR. European Medicines Agency (EMA). 16 October 2019 [29 April 2020]. （原始內容存檔於20 October 2020）.
^ ^11.0 ^11.1 Rinvoq: EPAR – Public assessment report (PDF). European Medicines Agency. 5 March 2020 [21 July 2020]. （原始內容存檔 (PDF)於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. 台灣免疫風濕疾病關懷協會. 2017-01-20 （中文（臺灣））.
^ Drug Trials Snapshots: Rinvoq. U.S. Food and Drug Administration (FDA). 16 August 2019 [18 March 2020]. （原始內容存檔於5 August 2020）.
^ ^15.0 ^15.1 Rinvoq. [13 September 2021]. （原始內容存檔於20 October 2020）.
^ ^16.0 ^16.1 Upadacitinib Monograph for Professionals. Drugs.com. [13 September 2021]. （原始內容存檔於22 August 2021）（英語）.

[Drugs.com_pregnancy-1] Upadacitinib (Rinvoq) Use During Pregnancy. Drugs.com. 23 September 2019 [17 March 2020]. （原始內容存檔於18 March 2020）.

[2] AusPAR: Upadacitinib. Therapeutic Goods Administration (TGA). 25 August 2021 [4 September 2021]. （原始內容存檔於4 September 2021）.

[3] Rinvoq (Abbvie Pty Ltd). [9 November 2022]. （原始內容存檔於9 November 2022）.

[4] Rinvoq (Abbvie Pty Ltd). Therapeutic Goods Administration (TGA). 16 February 2023 [9 April 2023]. （原始內容存檔於18 March 2023）.

[5] Rinvoq Product information. Health Canada. 25 April 2012 [29 May 2022]. （原始內容存檔於30 May 2022）.

[6] Summary Basis of Decision (SBD) for Rinvoq. Health Canada. 23 October 2014 [29 May 2022]. （原始內容存檔於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]. （原始內容存檔於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]. （原始內容存檔於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]. （原始內容存檔於20 October 2020）.

[AssessmentReport-11] 11.0 ^11.1 Rinvoq: EPAR – Public assessment report (PDF). European Medicines Agency. 5 March 2020 [21 July 2020]. （原始內容存檔 (PDF)於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. 台灣免疫風濕疾病關懷協會. 2017-01-20 （中文（臺灣））.

[FDA_snapshot-14] Drug Trials Snapshots: Rinvoq. U.S. Food and Drug Administration (FDA). 16 August 2019 [18 March 2020]. （原始內容存檔於5 August 2020）.

[EPAR2021-15] 15.0 ^15.1 Rinvoq. [13 September 2021]. （原始內容存檔於20 October 2020）.

[AHFS2021-16] 16.0 ^16.1 Upadacitinib Monograph for Professionals. Drugs.com. [13 September 2021]. （原始內容存檔於22 August 2021）（英語）.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[10]

[8]

[9]

[12]

[11]

[13]

[14]

[15]

[16]