Fedratinib

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Fedratinib is an onp drug catalogued in DrugCentral. It was first approved by the FDA in 2019. DrugCentral lists 282 molecular targets, including GAK, DAPK3 and JAK2. Recorded indications include Myelofibrosis, Post-essential thrombocythaemia myelofibrosis, Post-polycythaemia vera myelofibrosis and Primary myelofibrosis.

• Approval status: onp (first approved 2019 by the FDA).
• Molecular targets: GAK, DAPK3, JAK2 and STK16 (282 listed in DrugCentral).
• Indications: Myelofibrosis, Post-essential thrombocythaemia myelofibrosis, Post-polycythaemia vera myelofibrosis and Primary myelofibrosis.
• ATC code: L01EJ02 (Janus-associated kinase (JAK) inhibitors).
• Molecular formula: C27H36N6O3S; molecular weight 524.68 g/mol.

Indications & contraindications

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

Indications (4)

• Myelofibrosis
• Post-essential thrombocythaemia myelofibrosis
• Post-polycythaemia vera myelofibrosis
• Primary myelofibrosis

Mechanism & targets

Molecular targets (282)

Target	Gene	Action	Activity
Cyclin-G-associated kinase	GAK	unknown	Kd 8.96
Death-associated protein kinase 3	DAPK3	unknown	Kd 8.92
Tyrosine-protein kinase JAK2	JAK2	inhibitor	IC50 8.52
Serine/threonine-protein kinase 16	STK16	unknown	Kd 8.18
Serine/threonine-protein kinase DCLK3	DCLK3	unknown	Kd 7.89
Receptor-type tyrosine-protein kinase FLT3	FLT3	inhibitor	IC50 7.82
Death-associated protein kinase 1	DAPK1	unknown	Kd 7.80
Mitogen-activated protein kinase kinase kinase 19	MAP3K19	unknown	Kd 7.72
Death-associated protein kinase 2	DAPK2	unknown	Kd 7.54
BMP-2-inducible protein kinase	BMP2K	unknown	Kd 7.50
NUAK family SNF1-like kinase 1	NUAK1	unknown	Kd 7.47
AP2-associated protein kinase 1	AAK1	unknown	Kd 7.46
Tyrosine-protein kinase Fyn	FYN	unknown	Kd 7.42
Serine/threonine-protein kinase SIK1	SIK1	unknown	Kd 7.41
Tyrosine-protein kinase ABL1	ABL1	unknown	Kd 7.40
Focal adhesion kinase 1	PTK2	unknown	Kd 7.38
Serine/threonine-protein kinase 17B	STK17B	unknown	Kd 7.35
Platelet-derived growth factor receptor beta	PDGFRB	unknown	Kd 7.35
Mast/stem cell growth factor receptor Kit	KIT	unknown	Kd 7.34
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	unknown	IC50 7.32

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2021-02-08	EMA	—	CELGENE EUROPE BV
2019-08-16	FDA	—	IMPACT	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EJ02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Janus-associated kinase (JAK) inhibitors

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
Vitamin B1 decreased	231.7
Vitamin B1 deficiency	187.0
Splenomegaly	109.7
Death	102.7
Diarrhoea	91.5
Full blood count decreased	66.4
Nausea	49.2
Platelet count decreased	46.3
Haemoglobin decreased	35.9

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Fedratinib is on its molecule page.

• Molecular formula: C₂₇H₃₆N₆O₃S
• Molecular weight: 524.68 g/mol
• CAS number: 936091-26-8
• InChIKey: JOOXLOJCABQBSG-UHFFFAOYSA-N
• PubChem CID: 16722836

CC1=CN=C(NC2=CC=C(OCCN3CCCC3)C=C2)N=C1NC1=CC=CC(=C1)S(=O)(=O)NC(C)(C)C

Frequently asked questions

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

What is Fedratinib used for?

DrugCentral lists the following indications for Fedratinib: Myelofibrosis, Post-essential thrombocythaemia myelofibrosis, Post-polycythaemia vera myelofibrosis and Primary myelofibrosis.

How does Fedratinib work?

Its molecular targets in DrugCentral include GAK, DAPK3, JAK2 (inhibitor) and STK16.

When was Fedratinib first approved?

Fedratinib was first approved by the FDA in 2019.

What is the chemical formula of Fedratinib?

Fedratinib has the molecular formula C27H36N6O3S and a molecular weight of 524.68 g/mol.

Sources

• DrugCentral drug card 5347 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1287853 — compound record and bioactivity
• PubChem CID 16722836 — chemical identifiers
• DrugBank DB12500 — drug record
• FDA UNII 6L1XP550I6 — substance identity
• DailyMed: FDA labels for Fedratinib — current prescribing information (label search)
• UniProt O14976 (GAK) — target protein
• UniProt O43293 (DAPK3) — target protein
• UniProt O60674 (JAK2) — target protein
• UniProt O75716 (STK16) — target protein
• UniProt Q9C098 (DCLK3) — target protein
• UniProt P36888 (FLT3) — 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.