JAKAVI is a potent JAK inhibitor
Dysregulated JAK/STAT pathway is a key driver of PV1-5
- JAK signalling pathways have been shown in vitro to control the differentiation, growth, development, and survival of haematopoietic cells by activating the transcription factor STAT2
- JAK signalling is increased in PV, with ~99% of patients exhibiting an activating JAK2 mutation in either JAK2V617F exon 14 or JAK2 exon 123,4
- Dysregulated JAK signalling leads to proliferation of haematopoietic cells and a chronic inflammatory state caused by overproduction of cytokines1,5
JAKAVI inhibits both JAK1 and JAK26,7
- JAKAVI has been shown in vitro to bind to the kinase domain of JAK1 and JAK2 and inhibit JAK1 and JAK2 signalling6,7
- JAKAVI inhibits JAK stimulation of STAT and downstream effects on cellular proliferation6
JAKAVI mechanism of action6
