Gilteritinib

Gilteritinib
Clinical data
Trade names	Xospata
AHFS/Drugs.com	Monograph
MedlinePlus	a619003
License data	US DailyMed: Gilteritinib;
Pregnancy; category	AU: D; ;
Routes of; administration	By mouth
ATC code	L01EX13 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: WARNINGRx-only; EU: Rx-only; In general: ℞ (Prescription only);
Identifiers
	IUPAC name 6-Ethyl-3-[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide;
CAS Number	1254053-43-4;
PubChem CID	49803313;
DrugBank	DB12141;
ChemSpider	32055842;
UNII	66D92MGC8M;
KEGG	D10709; as salt: D10800;
ChEBI	CHEBI:145372;
CompTox Dashboard (EPA)	DTXSID701027949 ;
Chemical and physical data
Formula	C29H44N8O3
Molar mass	552.724 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCc1nc(C(=O)N)c(Nc2ccc(N3CCC(CC3)N4CCN(C)CC4)c(OC)c2)nc1NC5CCOCC5;
	InChI 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 (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

^ ^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.
^ 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.
^ "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.

External links

"Gilteritinib". Drug Information Portal. U.S. National Library of Medicine.
"Gilteritinib fumarate". NCI Drug Dictionary. National Cancer Institute.
"Gilteritinib fumarate". National Cancer Institute. 17 January 2019.

This antineoplastic or immunomodulatory drug article is a stub. You can help Wikipedia by expanding it.

[Xospata_APMDS-1] "Xospata Australian prescription medicine decision summary". Therapeutic Goods Administration (TGA). 11 April 2020. Retrieved 16 August 2020.

[FDA-AllBoxedWarnings-2] "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.

[3] "Summary Basis of Decision (SBD) for Xospata". Health Canada. 23 October 2014. Retrieved 29 May 2022.

[4] "Xospata 40 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 13 November 2019. Retrieved 16 August 2020.

[Xospata_FDA_label-5] "Xospata- gilteritinib tablet". DailyMed. 31 May 2019. Retrieved 16 August 2020.

[Xospata_EPAR-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.

[fda-gilteritinib-2018-11-28-11] "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.

[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.

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