Upadacitinib CAS 1310726-60-3
Upadacitinib (CAS 1310726 60 3), marketed as Rinvoq, is a selective JAK1 inhibitor indicated for multiple immune mediated diseases including rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, IBD, and atopic dermatitis. Its mechanism centers on modulating inflammatory signaling pathways. While effective for many patients, it carries risks of serious side effects requiring medical oversight. Costs can be high without insurance, but patient assistance and savings programs may mitigate this. Real world patient insights emphasize both tangible benefits and challenges in managing side effects and access.
What is Upadacitinib CAS 1310726-60-3 ?
Upadacitinib (CAS 1310726-60-3), sold under the brand name Rinvoq, is a prescription medication belonging to the class of Janus kinase (JAK) inhibitors. It works by selectively blocking the JAK1 enzyme to reduce the immune system's inflammatory signaling, making it an effective treatment for moderate to severe conditions like Rheumatoid Arthritis and Atopic Dermatitis.
|
Name |
Upadacitinib |
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IUPAC Name |
(3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide |
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CAS Number |
1310726-60-3 |
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Molecular Formula (MF) |
C₁₇H₁₉F₃N₆O |
|
Molecular Weight (MW) |
~380.37 g/mol |
|
Purity |
≥99% |
|
Physical Form |
Solid (White to off-white solid powder) |
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Solubility |
Soluble in DMSO (Dimethyl sulfoxide) and Ethanol |
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Storage (Short-Term) |
Dry, dark, and at at 0–4°C. |
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Storage (Long-Term) |
−20°C |
Upadacitinib Mechanism of Action
Upadacitinib exerts its therapeutic effect by selectively inhibiting Janus kinase 1 (JAK1), a key enzyme in the JAK STAT signaling pathway involved in immune cell activation and inflammatory cytokine signaling. By blocking JAK1 mediated phosphorylation of STAT proteins, upadacitinib reduces transcription of pro inflammatory genes. This targeted immunomodulation dampens excessive immune responses driving chronic inflammation in autoimmune diseases.
Mechanistically, this selectivity helps control symptoms such as joint pain, stiffness, intestinal inflammation, skin rash, and systemic immune activation that are characteristic of underlying autoimmune pathology.
What Is Upadacitinib Used For?
Upadacitinib (Rinvoq) is indicated for the treatment of multiple moderate to severe inflammatory conditions, especially in patients who have had inadequate response or intolerance to other therapies such as TNF blockers:
Autoimmune and Rheumatic Diseases:
Rheumatoid arthritis (RA) in adults
Psoriatic arthritis (PsA) in adults and pediatric patients ≥2 years
Active ankylosing spondylitis (AS)
Non radiographic axial spondyloarthritis (nr axSpA)
Giant cell arteritis (GCA)
Gastrointestinal Autoimmune Diseases:
Moderately to severely active ulcerative colitis (UC)
Moderately to severely active Crohn's disease (CD)
Dermatologic Autoimmune Disease:
Moderate to severe atopic dermatitis (eczema) in adults and children ≥12 years when other systemic therapies have failed.
Upadacitinib Side Effects
Common Side Effects:
- Patients taking upadacitinib may experience:
- Upper respiratory symptoms (cold, sinusitis), nausea, headache
- Acne or rash
- Abdominal discomfort, weight changes
- Folliculitis (hair follicle inflammation)
- Changes in blood counts (e.g., anemia, neutropenia)
Serious Side Effects :
- Upadacitinib carries boxed warnings, including increased risk of:
- Serious infections (e.g., TB, opportunistic infections)
- Malignancies and certain cancers
- Major cardiovascular events (heart attack, stroke)
- Blood clots (DVT, pulmonary embolism)
- Patients should be monitored regularly with lab tests to check blood counts, liver function, lipids, and signs of infection.
Precautions:
- Avoid live vaccines during therapy
- Not recommended for combination with other JAK inhibitors or potent immunosuppressants
- Special consideration before pregnancy and in liver impairment.
Upadacitinib Cost
Without insurance coverage, the approximate retail cost for upadacitinib can range from $5,500 to $6,500 per month in the United States, depending on dose and pharmacy pricing.
Community & Patient Insights
Beyond formal prescribing information, patients share real world experiences and concerns in online forums:
Positive Feedback:
Rapid symptom improvement in inflammatory bowel disease, often within days to weeks
Significant reduction in flare severity and improved daily functioning reported by some users
Common Patient Discussed Concerns:
Acne and skin changes - frequently discussed as an inconvenient but manageable side effect
Immune suppression effects - including increased infection risk or necessity of pausing therapy during viral illness
Hair thinning or loss - reported by some patients, not widely documented officially
Insurance and approval hurdles, especially with high list prices
These patient perspectives reflect variability in individual responses and priorities - with efficacy and quality of life gains being weighed against side effect profiles and cost/coverage issues in community discussions.
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