User:Ych65/吉瑞替尼

**Ych65/吉瑞替尼**
臨床資料
商品名（英语：Drug nomenclature）	Xospata
AHFS/Drugs.com	Monograph
MedlinePlus	a619003
核准狀況	美 DailyMed: Gilteritinib;
懷孕分級	澳: D ; ;
给药途径	By mouth
ATC碼	L01XE54 (WHO) ;
法律規範狀態
法律規範	澳：限医生处方（S4）; 歐：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為商品名出售，是一種抗癌藥。^[6]它可作為AXL受體酪胺酸激酶抑制劑，因此是一種酪氨酸激酶抑制劑。 ^[7]

此藥由安斯泰來製藥（Astellas Pharma）開發。

2018年4月，安斯泰來向美國食品藥品監督管理局（FDA）申请了吉瑞替尼的新藥申請，用於治療復發或難治性FLT3（英语：FLT3）突變急性骨髓性白血病成年患者。^[8]

2018年11月，美國FDA批准吉瑞替尼作為復發或難治性FLT3突變急性骨髓性白血病成年患者的治療用藥；FLT3突變須由美國FDA批准的測試測出。^[9]^[10]

美國FDA、歐洲聯盟委員會、以及日本厚生勞動省授權吉瑞替尼作為某些急性骨髓白血病患者的罕用藥。^[11]

2020年三月，吉瑞替尼被批准在澳洲用於醫療。^[12]

研究[编辑]

吉瑞替尼的用途已被重新定位為有潛力的抗病毒藥物，可能可以應用在治療COVID-19上。^[13]

參考文獻[编辑]

^ ^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.

延伸閱讀[编辑]

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

外部連結[编辑]

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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