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administration Oral Legal status Investigational CAS Number 937272-79-2 Molar mass 472.58 g/mol | ATC code None Synonyms SB1518 PubChem CID 46216796 | |
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John mascarenhas md ms continuing to evaluate pacritinib for myelofibrosis
Pacritinib (INN) is a macrocyclic Janus kinase inhibitor that is being developed for the treatment of myelofibrosis. It mainly inhibits Janus kinase 2 (JAK2) and Fms-like tyrosine kinase 3 (FLT3). The drug was in Phase III clinical trials as of 2013. The drug was discovered in Singapore at the labs of S*BIO Pte Ltd. It is a potent JAK2 inhibitor with activity of IC50 = 23 nM for the JAK2WT variant and 19 nM for JAK2V617F with very good selectivity against JAK1 and JAK3 (IC50 = 1280 and 520 nM, respectively).
Contents
- John mascarenhas md ms continuing to evaluate pacritinib for myelofibrosis
- Current research into jak inhibitors specifially ruxolitinib pacritinib and momelotinib
- References
The drug was acquired by Cell Therapeutics, Inc. (CTI) and Baxter International and could effectively address an unmet medical need for patients living with myelofibrosis who face treatment-emergent thrombocytopenia on marketed JAK inhibitors. When Shire Pharmaceuticals purchased Baxalta, a spin-off of Baxter Pharmaceuticals, they halted the development of the drug and ended their partnership with CTI.
The drug was given fast-track status in 2014. In 2016, the FDA placed a full clinical hold on pacritinib due to increased mortality in patients receiving the drug in the "PERSIST-2" trial.