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Upadacitinib

Upadacitinib structure

CAS No:
1310726-60-3
Formula:
C17H19F3N6O
Chemical Name:
Upadacitinib
Synonyms:
Upadacitinib;Upadacitinib (ABT-494);ABT-494 (Upadacitinib);Upadacitinib (Rinvoq);ABT-494; ABT494; ABT 494;CS-2730;(3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, Upadacitinib;1-Pyrrolidinecarboxamide, 3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-, (3S,4R)-
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Upadacitinib is a JAK1 inhibitor (IC50= 47 nM). It is selective for JAK1 over JAK3 and tyrosine kinase 2 (Tyk2; IC50s = 2,304 and 4,690 nM, respectively), as well as a panel of 83 additional kinases at 1 μM, but does inhibit JAK2, Rho-associated kinase I (ROCK1), and ROCK2 (IC50s = 120, 920, and 430 nM, respectively). Upadacitinib decreases cytokine-induced STAT phosphorylation in a variety of human cells with IC50values ranging from 1.6 to 649 nM. It reducesM. tuberculosis-induced paw swelling and bone erosion in a rat model of arthritis when administered at doses of 1, 3, and 10 mg/kg twice per day for 17 days. Formulations containing upadacitinib have been used in the treatment of rheumatoid arthritis.

Upadacitinib was discovered by AbbVie scientists, RINVOQ is a JAK inhibitor that is being studied in several immune-mediated inflammatory diseases. In human leukocyte cellular assays, RINVOQ inhibited cytokine-induced STAT phosphorylation mediated by JAK1 and JAK1/JAK3 more potently than JAK2/JAK2 mediated STAT phosphorylation. Upadacitinib (RINVOQ) received FDA approval in 2019 for the treatment of moderate to severe RA.

Upadacitinib Basic Attributes

Molecular Weight：

380.37

Exact Mass：

380.37

EC Number：

213-161-9

Color/Form：

White to off-white

Characteristics

PSA：

78.32

XLogP3：

3.2367

Density：

1.56±0.1 g/cm3(Predicted)

PKA：

11.89±0.60(Predicted)

Critical Temperature & Pressure：

Store at -20°C

Safety Information

Storage features：

Store at -20°C

Upadacitinib Use and Manufacturing

Upadacitinib also known as ABT-494, is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders, Janus kinase inhibitors for rheumatoid arthritis. It is used to treat moderate to severely active rheumatoid arthritis, active psoriatic arthritis, ankylosing spondylitis, non-radiographic axial spondyloarthritis (a type of arthritis in the spine) with objective signs of swelling, moderate to severe ulcerative colitis, and moderate to severe Crohn's disease in patients who have taken other medicines (eg, methotrexate) that did not work well. It is also used to treat moderate to severe atopic dermatitis (eczema) in patients who have taken other medicines that did not work well and whose condition is not well controlled with other treatments or in patients who cannot tolerate these treatments. It is also used to treatpsoriatic arthritis, axial SpA and Giant Cell Arteritis and Takayasu Arteritis.

Synthesis Route

1428243-26-8

Suppliers(32)

1310726-60-3

Suppliers(69)

Drug Function and Efficacy

It is a Janus kinase (JAK) inhibitor that blocks the phosphorylation and activation of STAT by regulating the JAK signaling pathway. Its inhibitory effects on JAK1 and JAK2 are higher than those on JAK3 and TYK2. In cell assays, it has a stronger inhibitory effect on the signaling pathways mediated by JAK1 and JAK1/JAK3.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Upadacitinib extended-release tablets
Ingredients	The main ingredient of this product is upadacitinib.
Specifications	15mg*28 tablets

Registered Holders

LEE PHARMA LTD

United States
Active
CURIA SPAIN SAU

United States
Active
MSN LABORATORIES PRIVATE LTD

United States
Active

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