Active Pharmaceutical Ingredients

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Baricitinib

1187594-09-7

\(C_{16}H_{17}N_{7}O_{2}\)

357.35

Baricitinib features a bicyclic core structure, with a purine – like moiety. It has several nitrogen – containing rings and side chains that are crucial for its interaction with the Janus kinases (JAKs). The structure allows it to selectively target specific JAK enzymes.

Usually appears as a solid, often in a white to off – white crystalline powder form.

Sparingly soluble in water. It has better solubility in certain organic solvents, which is important for formulating it into various pharmaceutical products, such as tablets or oral solutions.

Janus kinase (JAK) inhibitor

Baricitinib works by inhibiting the JAK family of enzymes, specifically JAK1 and JAK2. These kinases are involved in the signaling pathways of various cytokines. By blocking JAK1 and JAK2, baricitinib inhibits the downstream signaling of cytokines like interleukin – 6 (IL – 6), interferon – γ, and others. This leads to a reduction in the activation of immune cells and the subsequent inflammatory response.

Rheumatoid Arthritis: Approved for the treatment of rheumatoid arthritis in adults who have had an inadequate response to one or more disease – modifying antirheumatic drugs (DMARDs). It helps to reduce joint pain, swelling, and improve physical function. COVID – 19: In some cases, it has been used in hospitalized patients with COVID – 19, as the cytokine storm associated with severe COVID – 19 is thought to be partially mediated by JAK – related pathways. However, its use in COVID – 19 is still under evaluation.

Stable under normal storage conditions, typically at room temperature in a dry and dark place. But exposure to high humidity, extreme temperatures, or strong light can potentially cause degradation, which may affect its efficacy.

Common side effects include upper respiratory tract infections, nasopharyngitis, headache, and diarrhea. There is also an increased risk of serious infections, as the drug suppresses the immune system. Other risks include increased cholesterol levels, liver function abnormalities, and a small risk of blood clots. Baricitinib may interact with other medications, especially those that also affect the immune system or are metabolized by the same enzymes. For example, it should not be used in combination with strong immunosuppressants without careful consideration due to the additive risk of infection.