Polpharma API characteristics:

• Stable polymorphic form allowing first generic launch – form I
• Good control of impurity profile by handling 6 chemical steps
• GMP process validation planned for January 2019

Drug description:

Baricitinib belongs to antineoplastic and immunomodulating agents; is a selective immunosuppressant.
Baricitinib is indicated for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease-modifying anti-rheumatic drugs. Baricitinib may be used as monotherapy or in combination with methotrexate.
It is formulated as film-coated tablets for oral route of administration.

Mechanism of action:

Baricitinib is a selective and reversible inhibitor of Janus kinase 1 (JAK1) and Janus kinase 2 (JAK2).
Janus kinases (JAKs) are enzymes that transduce intracellular signals from cell surface receptors for a number of cytokines and growth factors involved in hematopoiesis, inflammation and immune function. Within the intracellular signaling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs), which activate gene expression within the cell. Baricitinib modulates these signaling pathways by partially inhibiting JAK1 and JAK2 enzymatic activity, thereby reducing the phosphorylation and activation of STATs.