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Specifications
|
Appearance |
White, off-white to yellow to brown solid |
|
Identification by NMR |
The test sample is consistent with the nuclear magnetic resonance (NMR) of the test sample |
|
Related Substances by HPLC |
Purity 99.0% min |
|
Any Single Impurity |
0.5% max |
|
Assay on Dried Basis (w/w) |
98.0% min |
|
Water Content by KF |
3.0% max |
|
Residue on Ignition |
0.20% max |
|
Heavy Metals |
10 ppm max |
Overview
Upadacitinib丨CAS 1310726-60-3 is a selective and potent JAK1 inhibitor, developed for the treatment of autoimmune and inflammatory disorders. It is a targeted small molecule therapy that modulates the JAK-STAT signaling pathway, which plays a critical role in the immune system's response to cytokines and growth factors.
Approved by regulatory agencies including the U.S. FDA and EMA, upadacitinib is commercially available under the brand name Rinvoq®, primarily for rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and atopic dermatitis.
Applications
1. Therapeutic Use
a. Rheumatoid Arthritis (RA)
● Approved as a monotherapy or in combination with methotrexate for adults with moderate to severe RA who have had an inadequate response to TNF blockers or other DMARDs.
b. Psoriatic Arthritis (PsA)
● Treats active PsA in patients unresponsive to conventional therapies or biologics.
c. Atopic Dermatitis
● Approved for moderate to severe atopic dermatitis, particularly in adults and adolescents (12 years and older) who are not adequately controlled with topical medications.
d. Ulcerative Colitis (UC)
● Used for moderate to severe UC as an oral alternative to corticosteroids and biologics.
e. Ankylosing Spondylitis & Axial Spondyloarthritis
● Indicated for adults with active ankylosing spondylitis or non-radiographic axial spondyloarthritis.
Mechanism of Action
● Upadacitinib丨CAS 1310726-60-3 selectively inhibits Janus kinase 1 (JAK1), one of four JAK family members involved in cytokine-mediated signal transduction.
● By inhibiting JAK1, it reduces the activity of pro-inflammatory cytokines like IL-6, IL-12, IL-23, and IFN-γ, without broadly affecting JAK2 or JAK3, which are involved in hematopoiesis and immune cell homeostasis.
● This selectivity contributes to its efficacy and potentially favorable safety profile compared to less selective JAK inhibitors.
Benefits
1. Targeted Immunomodulation
● Offers precise control of immune signaling pathways, reducing inflammation while preserving broader immune function.
2. Oral Administration
● Taken once daily as an oral tablet, providing a convenient alternative to injectable biologics like TNF inhibitors.
3. Rapid Onset of Action
● Clinical studies show symptom relief within weeks, making it suitable for patients requiring quick therapeutic impact.
4. Wide Indication Spectrum
● Approved across multiple chronic autoimmune diseases, reducing the need for multiple medications in comorbid conditions.
Summary
Upadacitinib (CAS 1310726-60-3) is a selective JAK1 inhibitor that has transformed the treatment landscape of autoimmune diseases by offering targeted, effective, and orally administered therapy. It is especially valuable for patients inadequately managed by traditional immunosuppressants or biologics. Its continued study in additional inflammatory conditions further underscores its therapeutic importance.
