Gilteritinib

Gilteritinib
Clinical data
Trade names	Xospata
AHFS/Drugs.com	xospata
ATC code	L01XE54 (WHO) ;
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;
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.[1] It acts as an inhibitor of AXL receptor tyrosine kinase, hence it is a tyrosine kinase inhibitor.[2]

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).[3]

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

References

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.

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[1] 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.

[2] 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.

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

[fda-gilteritinib-2018-11-28-4] 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.

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

[6] "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.