Pacritinib (also known as SB1518 or SB-1518) is an orally available small molecule inhibitor of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase 3 (FLT3). JAK2 and FLT3 are both involved in the regulation of cellular growth and differentiation, and their dysregulation has been implicated in various diseases, including certain forms of cancer. The chemical name of pacritinib is (S)-3-(2-chloro-6-methylphenyl)-2-((1-(tetrahydro-2H-pyran-4-yl)azetidin-3-yl)amino)propanamide, and its molecular formula is C21H27ClN2O2. Its formula weight is 382.91 g/mol, and its CAS number is 937272-79-2.
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Synonyms for Pacritinib include (S)-3-(2-Chloro-6-methylphenyl)-2-[1-(tetrahydro-2H-pyran-4-yl)azetidin-3-ylamino]propanamide, SB 1518, and SB-1518.
Health benefits of Pacritinib:
Pacritinib's potential health benefits are focused on its ability to inhibit JAK2 and FLT3. JAK2 inhibitors have shown promise in treating certain hematological malignancies, such as myelofibrosis, a rare blood cancer that disrupts the normal production of blood cells. FLT3 inhibitors, on the other hand, have been investigated as a potential treatment for acute myeloid leukemia, a type of cancer that affects white blood cells.
Preclinical studies of pacritinib have demonstrated its potential as an anti-tumor agent, particularly against cancers that involve JAK2 or FLT3 activation. This includes myelofibrosis and acute myeloid leukemia, as well as some solid tumors. Additionally, pacritinib has shown potential in treating inflammatory diseases, such as rheumatoid arthritis.
The primary mechanism of action of pacritinib is inhibition of JAK2 and FLT3, two proteins that are involved in cellular growth and differentiation. By inhibiting these proteins, pacritinib can reduce the growth and proliferation of cancer cells and potentially slow the progression of diseases like myelofibrosis and acute myeloid leukemia. In addition, inhibition of JAK2 and FLT3 may also modulate immune responses and reduce inflammation in certain conditions.
As with any medication or potential treatment, there is always the possibility of adverse effects. Pacritinib has been associated with some risk of cardiovascular and pulmonary toxicity in clinical trials, although this appears to be rare. Additional studies will be necessary to fully understand the safety profile of this compound.
Common side effects of pacritinib reported in clinical trials include gastrointestinal disturbances, such as nausea, diarrhea, and vomiting. Additional side effects may include fatigue, dizziness, headache, and respiratory infections.
Currently, pacritinib is not yet approved by regulatory agencies for clinical use. However, it has undergone multiple clinical trials for various indications, and dosing information may be available based on those studies. As with any medication, dosing should be determined by a healthcare professional based on individual patient factors.
Pacritinib has shown promise as a potential treatment for various hematological malignancies, particularly myelofibrosis and acute myeloid leukemia. Its ability to inhibit JAK2 and FLT3 makes it a promising candidate for targeted therapies, and preclinical studies have demonstrated its potential as an anti-tumor agent. However, additional research is needed to fully understand the safety profile of pacritinib and to establish appropriate dosing regimens. Further clinical trials will be necessary before it can be considered a viable treatment option for these indications