Category: pharmacological
Aliases: Jakafi, Jakavi, INCB018424
JAK1/JAK2 inhibitor — first JAK inhibitor approved (2011). Indications: myelofibrosis, polycythemia vera (HU-resistant), steroid-refractory acute + chronic GVHD. CYP3A4 substrate. Discontinuation of ruxolitinib in MF requires a slow taper to avoid cytokine-rebound systemic inflammatory response. PK (Jakafi label, 20 mg PO bid IR): Cmax 205-7100 nM across single-dose range (linear), Tmax 1-2 h, F ≥95%, t½ 3.0 h IR formulation (5.4 h newer ER once-daily formulation), Vss 72 L. CYP3A4 substrate; no significant food effect.
PO: 3h