pacritinib   Click here for help

GtoPdb Ligand ID: 7793

Synonyms: SB-1518 | SB1518 | Vonjo®
Approved drug PDB Ligand
pacritinib is an approved drug (FDA (2022))
Compound class: Synthetic organic
Comment: Pacritinib is an orally bioavailable and somewhat selective inhibitor of Janus kinase 2 (JAK2) and the JAK2 gain-of-function mutant JAK2V617F [3]. At clinically relevant concentrations, pacritinib does not inhibit JAK1. It also has some inhibitory activity against FMS-like tyrosine kinase 3 (FLT3).
Click here for help
2D Structure
Click here for help
Click here for structure editor
Physico-chemical Properties
Click here for help
Hydrogen bond acceptors 6
Hydrogen bond donors 1
Rotatable bonds 4
Topological polar surface area 68.74
Molecular weight 472.25
XLogP 4.16
No. Lipinski's rules broken 0
Click here for help
Canonical SMILES C1C=CCOCc2cc(ccc2OCCN2CCCC2)Nc2nc(c3cc(CO1)ccc3)ccn2
Isomeric SMILES C1/C=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nc(c3cc(CO1)ccc3)ccn2
InChI InChI=1S/C28H32N4O3/c1-2-13-32(12-1)14-17-35-27-9-8-25-19-24(27)21-34-16-4-3-15-33-20-22-6-5-7-23(18-22)26-10-11-29-28(30-25)31-26/h3-11,18-19H,1-2,12-17,20-21H2,(H,29,30,31)/b4-3+
No information available.
Summary of Clinical Use Click here for help
Pacritinib was advanced to Phase 3 clinical trial for the treatment of myelofibrosis with thrombocytopenia. In February 2022 the FDA granted approval for pacritinib's use as a treatment for patients with intermediate or high-risk primary or secondary cytopenic myelofibrosis [1].
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Inhibition of JAK2 by pacritinib leads to dampening of the JAK-STAT signalling pathway and has potent anti-proliferative effects on myeloid and lymphoid cell lines driven by mutant or wild-type JAK2 [2].
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03165734 A Phase 3 Study of Pacritinib in Patients With Primary Myelofibrosis, Post Polycythemia Vera Myelofibrosis, or Post-Essential Thrombocythemia Myelofibrosis Phase 3 Interventional CTI BioPharma