Baricitinib; 1187594-09-7; INCB028050; LY3009104; 2-(3-(4-(7H-Pyrrolo[2,3-D]Pyrimidin-4-Yl)-1H-Pyrazol-1-Yl)-1-(Ethylsulfonyl)Azetidin-3-Yl)Acetonitrile; INCB 028050;

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Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. Upon administration, baricitinib binds to JAK1/2, which inhibits JAK1/2 activation and leads to the inhibition of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This decreases the production of inflammatory cytokines and may prevent an inflammatory response. In addition, baricitinib may induce apoptosis and reduce proliferation of JAK1/2-expressing tumor cells. JAK kinases are intracellular enzymes involved in cytokine signaling, inflammation, immune function and hematopoiesis; they are also upregulated and/or mutated in various tumor cell types.

Baricitinib is an orally available small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis and more recently was given emergency use authorization as therapy in combination with remdesivir for severe COVID-19. Baricitinib is associated with transient and usually mild elevations in serum aminotransferase levels during therapy but has yet to be linked to cases of clinically apparent acute liver injury.

Baricitinib is a selective and reversible Janus kinase 1 (JAK1) and 2 (JAK2) inhibitor. Janus kinases belong to the tyrosine protein kinase family and play an important role in the proinflammatory pathway signalling that is frequently over-activated in autoimmune disorders such as rheumatoid arthritis. By blocking the actions of JAK1/2, baricitinib disrupts the activation of downstream signalling molecules and proinflammatory mediators. Rheumatoid arthritis is a progressive autoimmune disease commonly associated with discomfort, diasability, and joint damage. Throughout disease progression, the disease may further lead to joint erosions and deformities, causing premature mortality, functional impairment, and reduced quality of life. While there are several disease modifying antirheumatic drugs (DMARDs) available for treatment, patients often experience inadequate threapeutic resposes to these drugs. In animal models of inflammatory arthritis, baricitinib was shown to have significant anti-inflammatory effects, but also led to preservation of cartilage and bone, with no detectable suppression of humoral immunity or adverse hematologic effects. In the EU, baricitinib was approved in February of 2017 as a second-line orally administered treatment for moderate to severe active rheumatoid arthritis in adults, either as a monotherapy or when combined with methotrexate. It is marketed under the trade name Olumiant. Baricitinib in combination with [remdesivir] for the treatment of COVID-19, was granted an FDA Emergency Use Authorization on 19 November 2020.

Baricitinib Cas 1187594-09-7; INCB028050; LY3009104; 2-(3-(4-(7H-Pyrrolo[2,3-D]Pyrimidin-4-Yl)-1H-Pyrazol-1-Yl)-1-(Ethylsulfonyl)Azetidin-3-Yl)Acetonitrile; INCB 028050;

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