Mechanism of action
From the NCI Drug Dictionary: An orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis. Also, per Hart et al. 2011 pacritinib is a tyrosine kinase inhibitor (TKI) with equipotent activity against FLT3 (IC50=22 n) and Janus kinase 2 (JAK2, IC50=23 n).
Diseases for which it is used
History of changes in FDA indication
- 2022-03-01: Granted accelerated approval for the treatment of adults with intermediate or high-risk primary or secondary (post-polycythemia vera or post-essential thrombocythemia) myelofibrosis with a platelet count below 50 x 109/L. (Based on PERSIST-2)
Also known as
- Code name: SB-1518
- Brand name: Vonjo