伊布替尼

伊布替尼
临床资料
商品名（英语：Drug nomenclature）	Imbruvica, others
其他名称	PCI-32765, CRA-032765
AHFS/Drugs.com	Monograph
MedlinePlus	a614007
核准状况	美 DailyMed: Ibrutinib;
怀孕分级	澳: D ; ;
给药途径	口服给药
ATC码	L01EL01 (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	97.3%
药物代谢	肝 (CYP3A（英语：CYP3A） & CYP2D6)
生物半衰期	4–6 小时
排泄途径	粪便 (80%), 尿液 (10%)
识别信息
	IUPAC命名法 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one; ;
CAS号	936563-96-1
PubChem CID	24821094;
IUPHAR/BPS	6912;
DrugBank	DB09053;
ChemSpider	26637187;
UNII	1X70OSD4VX;
KEGG	D10223;
ChEBI	CHEBI:76612;
ChEMBL	ChEMBL1873475;
PDB配体ID	1E8 (PDBe, RCSB PDB);
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID60893450 ;
ECHA InfoCard	100.232.543
化学信息
化学式	C25H24N6O2
摩尔质量	440.51 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES C=CC(=O)N1CCC[C@H](C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N;
	InChI InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m1/s1; Key:XYFPWWZEPKGCCK-GOSISDBHBU;

伊布替尼（Ibrutinib）用于治疗被套细胞淋巴瘤（mantle cell lymphoma，MCL）、慢性淋巴细胞白血病（chronic lymphocytic leukemia，CLL）和华氏巨球蛋白血症（英语：Waldenström macroglobulinemia）（Waldenström's macroglobulinemia）的口服药物^[8] ^[9]。当以上淋巴瘤和白血病以用于其他治疗无效时，可考虑使用^[9]。也可能用于移植物抗宿主病^[8]。

常见副作用包括血小板减少症、贫血、白细胞减少症、腹泻、皮疹、出血和口腔发炎^[8]。其他副作用包括可能感染、心脏衰竭、高血压、其他癌症和肿瘤溶解症候群（英语：Tumor lysis syndrome）^[8]。孕期使用可能对胎儿有害^[8]。作用机转是阻断布鲁顿酪氨酸激酶（英语：Bruton's tyrosine kinase）（Bruton's tyrosine kinase，BTK），进而减缓B细胞的分裂与数量^[9]。

伊布替尼分别于 2013 年与2014年在美国与欧洲取得医疗使用许可^[10] ^[9]。名世界卫生组织基本药物标准清单^[11]。已有学名药流通于市^[12]。

参考文献

^ Ibrutinib (Imbruvica) Use During Pregnancy. Drugs.com. 3 December 2019 [28 March 2020].
^ Prescription medicines: registration of new chemical entities in Australia, 2015. Therapeutic Goods Administration (TGA). 21 June 2022 [10 April 2023].
^ Regulatory Decision Summary for Imbruvica. Drug and Health Products Portal. 4 August 2023 [2 April 2024].
^ Imbruvica 140 mg Film-Coated Tablets - Summary of Product Characteristics (SmPC). (emc). 16 January 2020 [28 March 2020].
^ UK Ibrutinib label. UK Electronic Medicines Compendium. 25 August 2016 [20 November 2016]. （原始内容存档于30 July 2019）.
^ Imbruvica- ibrutinib capsule Imbruvica- ibrutinib tablet, film coated. DailyMed. 8 April 2020 [21 April 2020].
^ Imbruvica EPAR. European Medicines Agency (EMA). 8 July 2021 [14 July 2021].
^ ^8.0 ^8.1 ^8.2 ^8.3 ^8.4 Imbruvica- ibrutinib capsule Imbruvica- ibrutinib tablet, film coated. DailyMed. 8 April 2020 [21 April 2020]. （原始内容存档于12 August 2020）.
^ ^9.0 ^9.1 ^9.2 ^9.3 Imbruvica EPAR. European Medicines Agency (EMA). 8 July 2021 [14 July 2021]. （原始内容存档于10 April 2021）.
^ Ibrutinib Monograph for Professionals. Drugs.com. [24 November 2021]. （原始内容存档于10 July 2020）（英语）.
^ World Health Organization. World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. 2021. WHO/MHP/HPS/EML/2021.02.
^ Ibrutinib: FDA-Approved Drugs. U.S. Food and Drug Administration (FDA). [19 June 2021]. （原始内容存档于24 June 2021）.

[Drugs.com_pregnancy-1] Ibrutinib (Imbruvica) Use During Pregnancy. Drugs.com. 3 December 2019 [28 March 2020].

[2] Prescription medicines: registration of new chemical entities in Australia, 2015. Therapeutic Goods Administration (TGA). 21 June 2022 [10 April 2023].

[3] Regulatory Decision Summary for Imbruvica. Drug and Health Products Portal. 4 August 2023 [2 April 2024].

[4] Imbruvica 140 mg Film-Coated Tablets - Summary of Product Characteristics (SmPC). (emc). 16 January 2020 [28 March 2020].

[UKlabel2016-5] UK Ibrutinib label. UK Electronic Medicines Compendium. 25 August 2016 [20 November 2016]. （原始内容存档于30 July 2019）.

[Imbruvica_FDA_label-6] Imbruvica- ibrutinib capsule Imbruvica- ibrutinib tablet, film coated. DailyMed. 8 April 2020 [21 April 2020].

[Imbruvica_EPAR-7] Imbruvica EPAR. European Medicines Agency (EMA). 8 July 2021 [14 July 2021].

[PI2021-8] 8.0 ^8.1 ^8.2 ^8.3 ^8.4 Imbruvica- ibrutinib capsule Imbruvica- ibrutinib tablet, film coated. DailyMed. 8 April 2020 [21 April 2020]. （原始内容存档于12 August 2020）.

[EPAR2021-9] 9.0 ^9.1 ^9.2 ^9.3 Imbruvica EPAR. European Medicines Agency (EMA). 8 July 2021 [14 July 2021]. （原始内容存档于10 April 2021）.

[10] Ibrutinib Monograph for Professionals. Drugs.com. [24 November 2021]. （原始内容存档于10 July 2020）（英语）.

[WHO22nd-11] World Health Organization. World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. 2021. WHO/MHP/HPS/EML/2021.02.

[12] Ibrutinib: FDA-Approved Drugs. U.S. Food and Drug Administration (FDA). [19 June 2021]. （原始内容存档于24 June 2021）.

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