Difference between revisions of "Pacritinib (Vonjo)"
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==Mechanism of action== | ==Mechanism of action== | ||
| − | From the [ | + | From the [https://www.cancer.gov/drugdictionary?CdrID=609888 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 [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3256753/ Hart et al. 2011] pacritinib is a tyrosine kinase inhibitor (TKI) with equipotent activity against FLT3 (IC<sub>50</sub>=22 n) and Janus kinase 2 (JAK2, IC<sub>50</sub>=23 n). |
==Diseases for which it is used== | ==Diseases for which it is used== | ||
| Line 17: | Line 17: | ||
[[Category:FLT3 inhibitors]] | [[Category:FLT3 inhibitors]] | ||
| − | [[Category: | + | [[Category:JAK2 inhibitors]] |
[[Category:Myelofibrosis medications]] | [[Category:Myelofibrosis medications]] | ||
[[Category:FDA approved in 2022]] | [[Category:FDA approved in 2022]] | ||
Latest revision as of 20:21, 27 June 2024
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