Gilteritinib

Last updated

Gilteritinib
Gilteritinib.svg
Clinical data
Trade names Xospata
AHFS/Drugs.com Monograph
MedlinePlus a619003
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
CompTox Dashboard (EPA)
Chemical and physical data
Formula C29H44N8O3
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]

Contents

Mechanism of action

Gilteritinib acts as an inhibitor of FLT3, hence it is a tyrosine kinase inhibitor. [8]

History

Gilteritinib 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 (both ITD and TKD [9] ) relapsed or refractory acute myeloid leukemia (AML). [10]

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. [11] [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. [12]

Gilteritinib was approved for medical use in Australia in March 2020. [13]

References

  1. 1 2 "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. ↑ "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.
  5. 1 2 "Xospata- gilteritinib tablet". DailyMed. 31 May 2019. Retrieved 16 August 2020.
  6. ↑ "Xospata EPAR". European Medicines Agency (EMA). 16 September 2019. Retrieved 16 August 2020.
  7. ↑ 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.
  8. ↑ 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.
  9. ↑ Molica M, Perrone S, Rossi M (May 2023). "Gilteritinib: The Story of a Proceeding Success into Hard-to-Treat FLT3-Mutated AML Patients". Journal of Clinical Medicine. 12 (11): 3647. doi: 10.3390/jcm12113647 . PMC   10253262 . PMID   37297842.
  10. ↑ "FDA Approval Sought for Gilteritinib in FLT3+ AML". onclive.com. April 24, 2018. Retrieved September 29, 2018.
  11. ↑ "FDA approves gilteritinib for relapsed or refractory AML with a FLT3 mutation". U.S. Food and Drug Administration (FDA). 2018-11-28. Retrieved 2018-11-29.
  12. ↑ "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.
  13. ↑ "AusPAR: Gilteritinib (as fumarate)". Therapeutic Goods Administration (TGA). 11 September 2020. Retrieved 23 September 2020.

Further reading

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