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  1. pharmadog
  2. ›drugs
  3. ›INREBIC
drug · small molecule
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INREBIC

updated 3mo ago
by $BMY BRISTOL MYERS SQUIBB CO🔗 ChEMBL
community read0 votes

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  • tagApproval28 co-mentions · 7 sources
  • drugfedratinib28 co-mentions · 7 sources
  • tagSmall Molecule14 co-mentions · 7 sources

Small molecule drug with a maximum clinical stage of Approval (across all indications), with an approval for 3 indications.

targets

Tyrosine-protein kinase JAK2Receptor-type tyrosine-protein kinase FLT3

all catalysts(0)

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brand
INREBIC
trade names
Inrebic
generic
FEDRATINIB HYDROCHLORIDE
MOA
12.1 Mechanism of Action Fedratinib is an oral kinase inhibitor with activity against wild type and mutationally activated Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Fedratinib is a JAK2-selective inhibitor with higher inhibitory activity for JAK2 over family members JAK1, JAK3 and TYK2. Abnormal activation of JAK2 is associated with myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera. In cell models expressing mutationally active JAK2 V617F or FLT3 ITD , fedratinib reduced phosphorylation of signal transducer and activator of transcription (STAT3/5) proteins, inhibited cell proliferation, and induced apoptotic cell death. In mouse models of JAK2 V617F -driven myeloproliferative disease, fedratinib blocked phosphorylation of STAT3/5, and improved survival, white blood cell counts, hematocrit, splenomegaly, and fibrosis.
indication
1 INDICATIONS AND USAGE INREBIC ® is indicated for the treatment of adult patients with intermediate-2 or high-risk primary or secondary (post-polycythemia vera or post-essential thrombocythemia) myelofibrosis (MF). INREBIC is a kinase inhibitor indicated for the treatment of adult patients with intermediate-2 or high-risk primary or secondary (post-polycythemia vera or post-essential thrombocythemia) myelofibrosis (MF) ( 1 ).
Data sources
ClinicalTrials.gov · OpenTargets
last refreshed 20m ago
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