Gilteritinib

Gilteritinib, sold under the brand name Xospata, is an anti-cancer drug.[6] It acts as an inhibitor of FLT3, hence it is a tyrosine kinase inhibitor.[7]

Gilteritinib
Clinical data
Trade namesXospata
AHFS/Drugs.comMonograph
MedlinePlusa619003
License data
Pregnancy
category
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Identifiers
  • 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
Chemical and physical data
FormulaC29H44N8O3
Molar mass552.724 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

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).[8]

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.[9][4]

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.[10]

Gilteritinib was approved for medical use in Australia in March 2020.[11]

References
  1. "Xospata Australian prescription medicine decision summary". Therapeutic Goods Administration (TGA). 11 April 2020. Retrieved 16 August 2020.
  2. "Summary Basis of Decision (SBD) for Xospata". Health Canada. 23 October 2014. Retrieved 29 May 2022.
  3. "Xospata 40 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 13 November 2019. Retrieved 16 August 2020.
  4. "Xospata- gilteritinib tablet". DailyMed. 31 May 2019. Retrieved 16 August 2020.
  5. "Xospata EPAR". European Medicines Agency (EMA). 16 September 2019. Retrieved 16 August 2020.
  6. 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.
  7. 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.
  8. "FDA Approval Sought for Gilteritinib in FLT3+ AML". onclive.com. April 24, 2018. Retrieved September 29, 2018.
  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. Retrieved 2018-11-29.
  10. "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.
  11. "AusPAR: Gilteritinib (as fumarate)". Therapeutic Goods Administration (TGA). 11 September 2020. Retrieved 23 September 2020.

Further reading


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