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Chemical structure of the small molecule gilteritinib.svg
Clinical data
Trade namesXospata
License data
Routes of
By mouth
ATC code
Legal status
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
Chemical and physical data
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)

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]

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]


  1. ^ a b "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. ^ a b "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". 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)". Retrieved 2018-12-03.
  11. ^ "AusPAR: Gilteritinib (as fumarate)". Therapeutic Goods Administration (TGA). 11 September 2020. Retrieved 23 September 2020.

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