Gilteritinib

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Gilteritinib is an onp drug catalogued in DrugCentral. It was first approved by the PMDA in 2018. DrugCentral lists 86 molecular targets, including LTK, AXL and NTRK1. Recorded indications include Acute myeloid leukemia, disease.

• Approval status: onp (first approved 2018 by the PMDA).
• Molecular targets: LTK, AXL, NTRK1 and ALK (86 listed in DrugCentral).
• Indications: Acute myeloid leukemia, disease.
• ATC code: L01EX13 (Other protein kinase inhibitors).
• Molecular formula: C29H44N8O3; molecular weight 552.72 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Acute myeloid leukemia, disease

Mechanism & targets

Molecular targets (86)

Target	Gene	Action	Activity
Leukocyte tyrosine kinase receptor	LTK	inhibitor	IC50 9.70
Tyrosine-protein kinase receptor UFO	AXL	inhibitor	IC50 9.10
High affinity nerve growth factor receptor	NTRK1	inhibitor	IC50 8.96
ALK tyrosine kinase receptor	ALK	unknown	IC50 8.82
Proto-oncogene tyrosine-protein kinase ROS	ROS1	unknown	IC50 8.72
Tyrosine-protein kinase Mer	MERTK	inhibitor	IC50 8.52
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	unknown	IC50 8.47
Receptor-type tyrosine-protein kinase FLT3	FLT3	inhibitor	IC50 8.30
Serine/threonine-protein kinase ULK3	ULK3	unknown	Kd 8.22
Interleukin-1 receptor-associated kinase 3	IRAK3	unknown	Kd 8.15
Cyclin-G-associated kinase	GAK	unknown	Kd 8.05
Uncharacterized protein FLJ45252	—	unknown	Kd 7.96
Serine/threonine-protein kinase PLK4	PLK4	unknown	Kd 7.75
AP2-associated protein kinase 1	AAK1	unknown	Kd 7.60
Non-receptor tyrosine-protein kinase TNK1	TNK1	unknown	Kd 7.41
Activin receptor type-1	ACVR1	unknown	Kd 7.41
BMP-2-inducible protein kinase	BMP2K	unknown	Kd 7.34
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	PHKG2	unknown	Kd 7.32
STE20-like serine/threonine-protein kinase	SLK	unknown	Kd 7.17
Mitogen-activated protein kinase kinase kinase kinase 1	MAP4K1	unknown	Kd 6.97

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2019-10-24	EMA	—	ASTELLAS PHARMA EUROPE BV	Yes
2018-11-28	FDA	—	ASTELLAS	Yes
2018-09-21	PMDA	—	Astellas Pharma Inc	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EX13	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: FLT3 · Testing Required
• FDA label: FLT3 · Testing Required
• HCSC label: FLT3 · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Myelosuppression	774.3
Febrile neutropenia	589.5
Acute myeloid leukaemia recurrent	441.8
Acute myeloid leukaemia	407.7
Platelet count decreased	383.6
Hepatic function abnormal	358.0
Cytopenia	347.6
Differentiation syndrome	318.6
Neutrophil count decreased	253.5
Blast cell count increased	236.5
Graft versus host disease	196.9
Electrocardiogram QT prolonged	179.7

Chemical structure

• Molecular formula: C₂₉H₄₄N₈O₃
• Molecular weight: 552.72 g/mol
• CAS number: 1254053-43-4
• InChIKey: GYQYAJJFPNQOOW-UHFFFAOYSA-N
• PubChem CID: 49803313

CCC1=NC(C(N)=O)=C(NC2=CC=C(N3CCC(CC3)N3CCN(C)CC3)C(OC)=C2)N=C1NC1CCOCC1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Gilteritinib used for?

DrugCentral lists the following indications for Gilteritinib: Acute myeloid leukemia, disease.

How does Gilteritinib work?

Its molecular targets in DrugCentral include LTK (inhibitor), AXL (inhibitor), NTRK1 (inhibitor) and ALK.

When was Gilteritinib first approved?

Gilteritinib was first approved by the PMDA in 2018.

What is the chemical formula of Gilteritinib?

Gilteritinib has the molecular formula C29H44N8O3 and a molecular weight of 552.72 g/mol.

Sources

• DrugCentral drug card 5306 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3301603 — compound record and bioactivity
• PubChem CID 49803313 — chemical identifiers
• DrugBank DB12141 — drug record
• FDA UNII 66D92MGC8M — substance identity
• DailyMed: FDA labels for Gilteritinib — current prescribing information (label search)
• UniProt P29376 (LTK) — target protein
• UniProt P30530 (AXL) — target protein
• UniProt P04629 (NTRK1) — target protein
• UniProt Q9UM73 (ALK) — target protein
• UniProt P08922 (ROS1) — target protein
• UniProt Q12866 (MERTK) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.