Difference between revisions of "Pacritinib (Vonjo)"

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==Mechanism of action==
 
==Mechanism of action==
  
From the [http://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 [http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3256753/ 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).  
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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).  
  
==Preliminary data==
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==Diseases for which it is used==
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*[[Myelofibrosis]]
  
===[[Myelofibrosis]]===
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==History of changes in FDA indication==
# Komrokji RS, Seymour JF, Roberts AW, Wadleigh M, To LB, Scherber R, Turba E, Dorr A, Zhu J, Wang L, Granston T, Campbell MS, Mesa RA. Results of a phase 2 study of pacritinib (SB1518), a JAK2/JAK2(V617F) inhibitor, in patients with myelofibrosis. Blood. 2015 Apr 23;125(17):2649-55. Epub 2015 Mar 11. [http://www.bloodjournal.org/content/125/17/2649.long link to original article] [http://www.ncbi.nlm.nih.gov/pubmed/25762180 PubMed]
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*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 10<sup>9</sup>/L. ''(Based on PERSIST-2)''
  
[[Category:Drug index]]
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==Also known as==
[[Category:Chemotherapy]]
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*'''Code name:''' SB-1518
[[Category:Oral chemotherapy]]
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*'''Brand name:''' Vonjo
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[[Category:Drugs]]
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[[Category:Oral medications]]
  
[[Category:Kinase inhibitors]]
 
 
[[Category:FLT3 inhibitors]]
 
[[Category:FLT3 inhibitors]]
[[Category:JAK inhibitors]]
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[[Category:JAK2 inhibitors]]
  
 
[[Category:Myelofibrosis medications]]
 
[[Category:Myelofibrosis medications]]
  
[[Category:Investigational]]
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[[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