用户:Ych65/吉瑞替尼

**Ych65/吉瑞替尼**
临床资料
商品名（英语：Drug nomenclature）	Xospata
AHFS/Drugs.com	Monograph
MedlinePlus	a619003
核准状况	美 DailyMed: Gilteritinib;
怀孕分级	澳: D ; ;
给药途径	By mouth
ATC码	L01XE54 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 欧：Rx-only; 英：处方药（℞-only） (POM); 美：处方药（℞-only）; 处方药（℞-only）;
识别信息
	IUPAC命名法 6-Ethyl-3-[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide; ;
CAS号	1254053-43-4
PubChem CID	49803313;
DrugBank	DB12141;
ChemSpider	32055842;
UNII	66D92MGC8M;
KEGG	D10709; D10800;
ChEBI	CHEBI:145372;
化学信息
化学式	C29H44N8O3
摩尔质量	552.72 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CCc1nc(C(=O)N)c(Nc2ccc(N3CCC(CC3)N4CCN(C)CC4)c(OC)c2)nc1NC5CCOCC5;
	InChI InChI=1S/C29H44N8O3/c1-4-23-28(31-20-9-17-40-18-10-20)34-29(26(33-23)27(30)38)32-21-5-6-24(25(19-21)39-3)37-11-7-22(8-12-37)36-15-13-35(2)14-16-36/h5-6,19-20,22H,4,7-18H2,1-3H3,(H2,30,38)(H2,31,32,34); Key:GYQYAJJFPNQOOW-UHFFFAOYSA-N;

吉瑞替尼（Gilteritinib ）以Xospata为商品名出售，是一种抗癌药。^[6]它可作为AXL受体酪胺酸激酶抑制剂，因此是一种酪氨酸激酶抑制剂。 ^[7]

此药由安斯泰来制药（Astellas Pharma）开发。

2018年4月，安斯泰来向美国食品药品监督管理局（FDA）申请了吉瑞替尼的新药申请，用于治疗复发或难治性FLT3（英语：FLT3）突变急性骨髓性白血病成年患者。^[8]

2018年11月，美国FDA批准吉瑞替尼作为复发或难治性FLT3突变急性骨髓性白血病成年患者的治疗用药；FLT3突变须由美国FDA批准的测试测出。^[9]^[10]

美国FDA、欧洲联盟委员会、以及日本厚生劳动省授权吉瑞替尼作为某些急性骨髓白血病患者的罕用药。^[11]

2020年三月，吉瑞替尼被批准在澳洲用于医疗。^[12]

研究

吉瑞替尼的用途已被重新定位为有潜力的抗病毒药物，可能可以应用在治疗COVID-19上。^[13]

参考文献

^ ^1.0 ^1.1 Xospata Australian prescription medicine decision summary. Therapeutic Goods Administration (TGA). 11 April 2020 [16 August 2020].
^ Xospata 40 mg film-coated tablets - Summary of Product Characteristics (SmPC). (emc). 13 November 2019 [16 August 2020].
^ Xospata- gilteritinib tablet. DailyMed. 31 May 2019 [16 August 2020].
^ Xospata EPAR. European Medicines Agency (EMA). 16 September 2019 [16 August 2020].
^ Gilteritinib (Xospata) Use During Pregnancy. Drugs.com. 20 August 2019 [16 August 2020].
^ Selective inhibition of FLT3 by gilteritinib in relapsed or refractory acute myeloid leukaemia: a multicentre, first-in-human, open-label, phase 1-2 study. The Lancet. Oncology. August 2017, 18 (8): 1061–1075. PMC 5572576  . PMID 28645776. doi:10.1016/S1470-2045(17)30416-3.
^ Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor. Blood. January 2017, 129 (2): 257–260. PMC 5234222  . PMID 27908881. doi:10.1182/blood-2016-10-745133.
^ FDA Approval Sought for Gilteritinib in FLT3+ AML. onclive.com. April 24, 2018 [September 29, 2018].
^ FDA approves gilteritinib for relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation. U.S. Food and Drug Administration (FDA). 2018-11-28 [2018-11-29].
^ Xospata EPAR. European Medicines Agency (EMA). 16 September 2019 [16 August 2020.].
^ U.S. FDA Grants Priority Review to Astellas' New Drug Application for Gilteritinib for the Treatment of Adult Patients with Relapsed or Refractory Acute Myeloid Leukemia (AML). Drugs.com. [2018-12-03].
^ AusPAR: Gilteritinib (as fumarate). Therapeutic Goods Administration (TGA). 11 September 2020 [23 September 2020].
^ The Global Phosphorylation Landscape of SARS-CoV-2 Infection. Cell. 2020-08-06, 182 (3): 685–712.e19 [2020-07-24]. PMC 7321036  . PMID 32645325. doi:10.1016/j.cell.2020.06.034.

延伸阅读

AusPAR: Gilteritinib (as fumarate). Therapeutic Goods Administration (TGA) (报告). September 2020.

外部链接

Gilteritinib. Drug Information Portal. U.S. National Library of Medicine.
Gilteritinib fumarate. NCI Drug Dictionary. National Cancer Institute.
Gilteritinib fumarate. National Cancer Institute.

[[Category:罕用药]] [[Category:酪氨酸激酶抑制剂]] [[Category:哌啶]] [[Category:哌嗪]] [[Category:吡嗪]] [[Category:Drugs with non-standard legal status]] [[Category:安斯泰來製藥]]

[Xospata_APMDS-1] 1.0 ^1.1 Xospata Australian prescription medicine decision summary. Therapeutic Goods Administration (TGA). 11 April 2020 [16 August 2020].

[2] Xospata 40 mg film-coated tablets - Summary of Product Characteristics (SmPC). (emc). 13 November 2019 [16 August 2020].

[Xospata_FDA_label-3] Xospata- gilteritinib tablet. DailyMed. 31 May 2019 [16 August 2020].

[Xospata_EPAR-4] Xospata EPAR. European Medicines Agency (EMA). 16 September 2019 [16 August 2020].

[Drugs.com_pregnancy-5] Gilteritinib (Xospata) Use During Pregnancy. Drugs.com. 20 August 2019 [16 August 2020].

[6] Selective inhibition of FLT3 by gilteritinib in relapsed or refractory acute myeloid leukaemia: a multicentre, first-in-human, open-label, phase 1-2 study. The Lancet. Oncology. August 2017, 18 (8): 1061–1075. PMC 5572576  . PMID 28645776. doi:10.1016/S1470-2045(17)30416-3.

[7] Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor. Blood. January 2017, 129 (2): 257–260. PMC 5234222  . PMID 27908881. doi:10.1182/blood-2016-10-745133.

[8] FDA Approval Sought for Gilteritinib in FLT3+ AML. onclive.com. April 24, 2018 [September 29, 2018].

[fda-gilteritinib-2018-11-28-9] FDA approves gilteritinib for relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation. U.S. Food and Drug Administration (FDA). 2018-11-28 [2018-11-29].

[10] Xospata EPAR. European Medicines Agency (EMA). 16 September 2019 [16 August 2020.].

[11] U.S. FDA Grants Priority Review to Astellas' New Drug Application for Gilteritinib for the Treatment of Adult Patients with Relapsed or Refractory Acute Myeloid Leukemia (AML). Drugs.com. [2018-12-03].

[12] AusPAR: Gilteritinib (as fumarate). Therapeutic Goods Administration (TGA). 11 September 2020 [23 September 2020].

[13] The Global Phosphorylation Landscape of SARS-CoV-2 Infection. Cell. 2020-08-06, 182 (3): 685–712.e19 [2020-07-24]. PMC 7321036  . PMID 32645325. doi:10.1016/j.cell.2020.06.034.

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