Gilteritinib

Gilteritinib
Clinical data
Trade names	Xospata
AHFS/Drugs.com	xospata
ATC code	L01XE54 (WHO) ;
Legal status
Legal status	US: WARNING;
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;
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 (trade name Xospata) is an anti-cancer drug.^[2] It acts as an inhibitor of AXL receptor tyrosine kinase, hence it is a tyrosine kinase inhibitor.^[3]

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).^[4]

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.^[5] The recommended dose of gilteritinib is 120 mg orally once daily.^[6]

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.^[7]

Gilteritinib has been repurposed as a potential antiviral drug as a possible application in the treatment of COVID-19.^[8]

References

^ "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.
^ 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.
^ U.S. Food and Drug Administration (2018-11-28). "FDA approves gilteritinib for relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation". www.fda.gov. Retrieved 2018-11-29.
^ "Prescribing information for XOSPATA (gilteritinib)" (PDF). U.S. Food and Drug Administration.
^ "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.
^ Bouhaddou M, Memon D, Meyer B, White KM, Rezelj VV, et al. (2020-08-06). "The Global Phosphorylation Landscape of SARS-CoV-2 Infection". Cell. 182: 1–28. doi:10.1016/j.cell.2020.06.034. Retrieved 2020-07-24.

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[FDA-AllBoxedWarnings-1] "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.

[2] 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.

[3] 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.

[4] "FDA Approval Sought for Gilteritinib in FLT3+ AML". onclive.com. April 24, 2018. Retrieved September 29, 2018.

[fda-gilteritinib-2018-11-28-5] U.S. Food and Drug Administration (2018-11-28). "FDA approves gilteritinib for relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation". www.fda.gov. Retrieved 2018-11-29.

[6] "Prescribing information for XOSPATA (gilteritinib)" (PDF). U.S. Food and Drug Administration.

[7] "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.

[8] Bouhaddou M, Memon D, Meyer B, White KM, Rezelj VV, et al. (2020-08-06). "The Global Phosphorylation Landscape of SARS-CoV-2 Infection". Cell. 182: 1–28. doi:10.1016/j.cell.2020.06.034. Retrieved 2020-07-24.

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