Fostamatinib

BLOOD AND BLOOD FORMING ORGANS

Key facts

Fostamatinib is an ofp drug catalogued in DrugCentral. It was first approved by the FDA in 2018. DrugCentral lists 265 molecular targets, including FLT3, STK16 and KIT. Recorded indications include Chronic idiopathic thrombocytopenic purpura and Immune thrombocytopenia.

• Approval status: ofp (first approved 2018 by the FDA).
• Molecular targets: FLT3, STK16, KIT and EIF2AK4 (265 listed in DrugCentral).
• Indications: Chronic idiopathic thrombocytopenic purpura and Immune thrombocytopenia.
• ATC code: B02BX09 (Other systemic hemostatics).
• Molecular formula: C23H26FN6O9P; molecular weight 580.47 g/mol.

Indications & contraindications

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

Indications (2)

• Chronic idiopathic thrombocytopenic purpura
• Immune thrombocytopenia

Mechanism & targets

Molecular targets (265)

Target	Gene	Action	Activity
Receptor-type tyrosine-protein kinase FLT3	FLT3	unknown	Kd 9.43
Serine/threonine-protein kinase 16	STK16	unknown	Kd 8.77
Mast/stem cell growth factor receptor Kit	KIT	unknown	Kd 8.60
Eukaryotic translation initiation factor 2-alpha kinase 4	EIF2AK4	unknown	Kd 8.48
Platelet-derived growth factor receptor beta	PDGFRB	unknown	Kd 8.48
Tyrosine-protein kinase JAK2	JAK2	unknown	Kd 8.46
Mitogen-activated protein kinase kinase kinase 10	MAP3K10	unknown	Kd 8.42
Serine/threonine-protein kinase PLK4	PLK4	unknown	Kd 8.38
Mitogen-activated protein kinase kinase kinase 9	MAP3K9	unknown	Kd 8.37
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	inhibitor	IC50 8.30
Serine/threonine-protein kinase PLK3	PLK3	unknown	Kd 8.29
Serine/threonine-protein kinase Nek6	NEK6	unknown	Kd 8.20
Serine/threonine-protein kinase ULK3	ULK3	unknown	Kd 8.15
Proto-oncogene tyrosine-protein kinase Src	SRC	unknown	Kd 8.08
Serine/threonine-protein kinase 17B	STK17B	unknown	Kd 8.04
Vascular endothelial growth factor receptor 3	FLT4	unknown	Kd 8.04
Epithelial discoidin domain-containing receptor 1	DDR1	unknown	Kd 8.03
Interleukin-1 receptor-associated kinase 1	IRAK1	unknown	Kd 8.01
Mitogen-activated protein kinase 9	MAPK9	unknown	EC50 8.00
Mitogen-activated protein kinase 8	MAPK8	unknown	EC50 8.00

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2022-12-23	PMDA	—	Kissei Pharmaceutical Co., Ltd.	Yes
2020-01-09	EMA	—	Instituto Grifols S.A.
2018-04-17	FDA	—	RIGEL PHARMS INC

ATC classification

ATC code	Therapeutic hierarchy
B02BX09	BLOOD AND BLOOD FORMING ORGANS › ANTIHEMORRHAGICS › VITAMIN K AND OTHER HEMOSTATICS › Other systemic hemostatics

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
Platelet count decreased	318.8
Platelet count	266.5
Diarrhoea	146.7
Death	118.7
Hospitalisation	108.9
Product prescribing issue	96.6
Hepatic function abnormal	83.8
Platelet count increased	76.0
Splenectomy	74.2
Off label use	61.7
Drug ineffective	61.5
Hypertension	60.1

Chemical structure

• Molecular formula: C₂₃H₂₆FN₆O₉P
• Molecular weight: 580.47 g/mol
• CAS number: 901119-35-5
• InChIKey: GKDRMWXFWHEQQT-UHFFFAOYSA-N
• PubChem CID: 11213558

COC1=CC(NC2=NC(NC3=CC=C4OC(C)(C)C(=O)N(COP(O)(O)=O)C4=N3)=C(F)C=N2)=CC(OC)=C1OC

Frequently asked questions

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

What is Fostamatinib used for?

DrugCentral lists the following indications for Fostamatinib: Chronic idiopathic thrombocytopenic purpura and Immune thrombocytopenia.

How does Fostamatinib work?

Its molecular targets in DrugCentral include FLT3, STK16, KIT and EIF2AK4.

When was Fostamatinib first approved?

Fostamatinib was first approved by the FDA in 2018.

What is the chemical formula of Fostamatinib?

Fostamatinib has the molecular formula C23H26FN6O9P and a molecular weight of 580.47 g/mol.

Sources

• DrugCentral drug card 5280 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2103830 — compound record and bioactivity
• PubChem CID 11213558 — chemical identifiers
• DrugBank DB07159 — drug record
• FDA UNII RC3A285J2G — substance identity
• DailyMed: FDA labels for Fostamatinib — current prescribing information (label search)
• UniProt P36888 (FLT3) — target protein
• UniProt O75716 (STK16) — target protein
• UniProt P10721 (KIT) — target protein
• UniProt Q9P2K8 (EIF2AK4) — target protein
• UniProt P09619 (PDGFRB) — target protein
• UniProt O60674 (JAK2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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