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fedratinib

Structure via PubChem · Public domain (PubChem)

EntityQ7670147· pop 8· linked from 223 articles

fedratinib

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Also known as SAR302503, TG-101348, TG101348

Fedratinib, sold under the brand name Inrebic, is an anti-cancer medication used to treat myeloproliferative diseases including myelofibrosis. It is used in the form of fedratinib hydrochloride capsules that are taken by mouth. It is a semi-selective inhibitor of Janus kinase 2 (JAK-2). It was approved by the FDA on 16 August 2019.

Chemical data

Formula
C27H36N6O3S
Molecular weight
524.7 g/mol
IUPAC name
N-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
SMILES
CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)OCCN4CCCC4
InChIKey
JOOXLOJCABQBSG-UHFFFAOYSA-N
XLogP
4.8
Polar surface area
117 Ų
H-bond donors
3
H-bond acceptors
9
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Approved
Molecule type
Small molecule
First approval
2019
Admin. routes
oral
Indications
neoplasm, primary myelofibrosis, liver disease, kidney disease

via ChEMBL · EBI

Wikidata facts

Mass
524.257
Has use
medication
Show 5 more facts
Commons category
Fedratinib
medical condition treated
myelofibrosis
canonical SMILES
CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)OCCN4CCCC4
chemical formula
C₂₇H₃₆N₆O₃S
Sources (2)

via Wikidata · CC0

~3 min read

Encyclopedic overview

6 sections
Contents
  • Medical uses
  • Pharmacology
  • Mechanism of action
  • History
  • References
  • External links

Fedratinib, sold under the brand name Inrebic, is an anti-cancer medication used to treat myeloproliferative diseases including myelofibrosis. It is used in the form of fedratinib hydrochloride capsules that are taken by mouth. It is a semi-selective inhibitor of Janus kinase 2 (JAK-2). It was approved by the FDA on 16 August 2019.

Myelofibrosis is a myeloid cancer associated with anemia, splenomegaly, and constitutional symptoms. Patients with myelofibrosis frequently harbor mutations which activate the JAK-STAT signaling pathway and which are sensitive to fedratinib. Phase I trial results focused on safety and efficacy of fedratinib in patients with high- or intermediate-risk primary or post–polycythemia vera/essential thrombocythemia myelofibrosis have been published in 2011.

Excerpted from Wikipedia’s “fedratinib” article, available under the CC BY-SA 4.0 licence.

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