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Updated: May 8, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
[JAK inhibitor]
Kunihiro Yamaoka1, Yoshiya Tanaka
1The First Department of Internal Medicine, University of Occupational and Enviromental Health, Japan.
Biologics targeting inflammatory cytokine has become a standardized tool for remission induction in rheumatoid arthritis (RA). However, it is handled under restricted conditions and their cost of acquisition is high. Small molecule drugs targeting Janus kinase (JAK), a molecule involved in intracellular signaling pathway has shown similar treatment effect as biologics. Moreover, inhibitory effect on bone destruction has been demonstrated and has been approved in 2012 as a new disease modifying anti-rheumatic drug in USA. However, since the inhibition of JAK results in inhibition of multiple cytokine signaling pathways, the clinical studies have also shown adverse events differing from biologics.
Biologics targeting inflammatory cytokine has become a standardized tool for remission induction in rheumatoid arthritis (RA). However, it is handled under restricted conditions and their cost of acquisition is high. Small molecule drugs targeting Janus kinase (JAK), a molecule involved in intracellular signaling pathway has shown similar treatment effect as biologics. Moreover, inhibitory effect on bone destruction has been demonstrated and has been approved in 2012 as a new disease modifying anti-rheumatic drug in USA. However, since the inhibition of JAK results in inhibition of multiple cytokine signaling pathways, the clinical studies have also shown adverse events differing from biologics.
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