奎扎替尼

化合物

奎扎替尼(Quizartinib)是一种用于治疗急性骨髓性白血病的药物,商品名为Vanflyta[2]

奎扎替尼
IUPAC名
N-(5-tert-Butyl-1,2-oxazol-3-yl)-N′-(4-{7-[2-(morpholin-4-yl)ethoxy]imidazo[2,1-b][1,3]benzothiazol-2-yl}phenyl)urea
别名
  • AC220
  • AC010220
  • Vanflyta
识别
CAS号 950769-58-1  checkY[PubChem]
PubChem 24889392
ChemSpider 24640357
SMILES
 
  • CC(C)(C)c1cc(no1)NC(=O)Nc2ccc(cc2)c3cn4c5ccc(cc5sc4n3)OCCN6CCOCC6
InChI
 
  • 1/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4-9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36)
InChIKey CVWXJKQAOSCOAB-UHFFFAOYAF
ChEBI 90217
DrugBank DB12874
KEGG D09955
IUPHAR配体 5658
性质
化学式 C29H32N6O4S
摩尔质量 560.67 g·mol−1
药理学
ATC代码 L01EX11L01
药品分级
若非注明,所有数据均出自标准状态(25 ℃,100 kPa)下。

它是一种小分子受体酪氨酸激酶抑制剂。其分子靶点是FLT3,也称CD135(一种原癌基因)。[3]

它在2019年10月在日本获许使用,[4]2023年7月在美国得到批准。[2]

参考文献

  1. ^ Vanflyta- quizartinib tablet, film coated. DailyMed. 26 July 2023 [6 August 2023]. (原始内容存档于7 August 2023). 
  2. ^ 2.0 2.1 2.2 FDA approves quizartinib for newly diagnosed acute myeloid leukemia. U.S. Food and Drug Administration (FDA). 20 July 2023 [21 July 2023]. (原始内容存档于21 July 2023).    本文含有此來源中屬於公有领域的内容。
  3. ^ Chao Q, Sprankle KG, Grotzfeld RM, Lai AG, Carter TA, Velasco AM, et al. Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. Journal of Medicinal Chemistry. December 2009, 52 (23): 7808–7816. PMID 19754199. doi:10.1021/jm9007533. 
  4. ^ Daiichi Sankyo Launches FLT3 Inhibitor Vanflyta in Japan for the Treatment of Patients with Relapsed/Refractory FLT3-ITD AML (新闻稿). [16 February 2021]. (原始内容存档于2023-08-10). 

外部链接

  • Clinical trial number NCT02668653 for "Quizartinib With Standard of Care Chemotherapy and as Continuation Therapy in Patients With Newly Diagnosed FLT3-ITD (+) Acute Myeloid Leukemia (AML) (QuANTUM-First)" at ClinicalTrials.gov