From Wikipedia, the free encyclopedia
Chemical compound
Gilteritinib
Trade names Xospata
AHFS /
Drugs.com
Monograph
MedlinePlus
a619003
License data
Pregnancy category
Routes of administration
By mouth
ATC code
Legal status
6-Ethyl-3-[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide
CAS Number
PubChem
CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
CompTox Dashboard (
EPA )
Formula C 29 H 44 N 8 O 3
Molar mass 552.724 g·mol−1 3D model (
JSmol )
CCc1nc(C(=O)N)c(Nc2ccc(N3CCC(CC3)N4CCN(C)CC4)c(OC)c2)nc1NC5CCOCC5
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
Gilteritinib , sold under the brand name Xospata , is an anti-cancer drug.
[7]
It acts as an
inhibitor of
FLT3 , hence it is a
tyrosine kinase inhibitor .
[8]
It was
developed by
Astellas Pharma .
In April 2018, Astellas filed a
new drug application with the
Food and Drug Administration for gilteritinib for the treatment of adult patients with
FLT3 mutation –positive relapsed or refractory
acute myeloid leukemia (AML).
[9]
In November 2018, the FDA approved gilteritinib for treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation as detected by an FDA-approved test.
[10]
[5]
Gilteritinib was granted
orphan drug status by the U.S. FDA, the European Commission (EC) and the Japan Ministry of Health, Labor and Welfare, for some AML patients.
[11]
Gilteritinib was approved for medical use in Australia in March 2020.
[12]
References
^
a
b
"Xospata Australian prescription medicine decision summary" . Therapeutic Goods Administration (TGA) . 11 April 2020. Retrieved 16 August 2020 .
^
"FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)" . nctr-crs.fda.gov .
FDA . Retrieved 22 Oct 2023 .
^
"Summary Basis of Decision (SBD) for Xospata" .
Health Canada . 23 October 2014. Retrieved 29 May 2022 .
^
"Xospata 40 mg film-coated tablets - Summary of Product Characteristics (SmPC)" . (emc) . 13 November 2019. Retrieved 16 August 2020 .
^
a
b
"Xospata- gilteritinib tablet" . DailyMed . 31 May 2019. Retrieved 16 August 2020 .
^
"Xospata EPAR" .
European Medicines Agency (EMA) . 16 September 2019. Retrieved 16 August 2020 .
^ Perl AE, Altman JK, Cortes J, Smith C, Litzow M, Baer MR, et al. (August 2017).
"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 . 18 (8): 1061–1075.
doi :
10.1016/S1470-2045(17)30416-3 .
PMC
5572576 .
PMID
28645776 .
^ Lee LY, Hernandez D, Rajkhowa T, Smith SC, Raman JR, Nguyen B, et al. (January 2017).
"Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor" . Blood . 129 (2): 257–260.
doi :
10.1182/blood-2016-10-745133 .
PMC
5234222 .
PMID
27908881 .
^
"FDA Approval Sought for Gilteritinib in FLT3+ AML" . onclive.com. April 24, 2018. Retrieved 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. Retrieved 2018-11-29 .
^
"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 . Retrieved 2018-12-03 .
^
"AusPAR: Gilteritinib (as fumarate)" .
Therapeutic Goods Administration (TGA) . 11 September 2020. Retrieved 23 September 2020 .
Further reading
External links
CI
monoclonal antibodies ("-mab")
Tyrosine kinase inhibitors ("-nib")
Receptor tyrosine kinase
RET inhibitors:
Entrectinib (ALK, ROS1, NTRK),
Futibatinib (FGFR2),
Infigratinib ,
Larotrectinib (NTRK),
Pemigatinib (FGFR),
Pralsetinib ,
Repotrectinib (ROS1, TRK, ALK),
Selpercatinib (VEGFR, FGFR),
Vandetanib (VEGFR, EGFR).
Non-receptor
Other