RODRIGO SOUZA
Biocatalysis and Organic Synthesis Group, Chemistry Institute, Federal University of Rio de Janeiro, Rio de Janeiro, Brazils

The third molecule which we are going to present here at “API of the Month” is pacritinib, a selective oral Janus kinase inhibitor (JAK2) used for the treatment of adults with intermediate or high-risk myelofibrosis with a platelet count below 50 × 109/L. Pacritinib sold under the brand name Vonjo (CTI BioPharma) was approved on 28th of February 2022 with an oral, 200 mg dose, twice daily (1, 2).

As mentioned last month, protein kinases are families of enzymes that catalyze the phosphorylation of specific residues in proteins, where inappropriate tyrosine kinase activity (JAK1, JAK2, JAK3, and Tyk2) can lead to a variety of biological cellular responses related to already known autoimmune and hematological disorders (3). With its selective inhibition of JAK2 without accessing JAK1, VONJO is the first approved therapy that specifically addresses the needs of patients with cytopenic myelofibrosis
Synthetic strategies towards pacritinib are focused on the synthe ... ...