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Upon cessation, ruxolitinib discontinuation syndrome develops in some patients. Clinical manifestations include rebound splenomegaly, cytopenias, acute respiratory distress syndrome, and systemic inflammatory response syndrome.
Ruxolitinib is metabolized primarily by CYP3A4, with a half-life of approximately 3 hours. Ruxolitinib is not removed by dialysis, although some active metabolites may be removed; therefore, the drug should be administered after dialysis.
Ruxolitinib is a pregnancy category C teratogen. Although there is no evidence of teratogenicity, in animal studies, pregnant rats given this medication have shown approximately 9% reduction in foetal weight at the highest and maternally toxic dose of 60 mg/kg/day23.
Ruxolitinib has a short terminal half-life of approximately 3 h for doses up to 100 mg [43], suggesting that twice-daily (b.i.d.) administration of ruxolitinib is preferable to once-daily dosing.
Ruxolitinib pharmacokinetics can be described with a two-compartment model and linear elimination. Volume of distribution differs between men and women, likely related to bodyweight differences. Metabolism is mainly hepatic via CYP3A4 and can be altered by CYP3A4 inducers and inhibitors.
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After oral administration, ruxolitinib shows rapid absorption, with more than 95% of the administered dose absorbed. Plasma concentration then declines rapidly in a biphasic manner, with a terminal half-life of 23 h.
In a study performed by Shi et al., ruxolitinib was administered in doses of 5200 mg twice daily. Elimination half-life (T) was approximately 3 h and clearance (CL/F) was 20 L/h and dose independent.
It is highly soluble in water, most soluble at low pH (pH 3.3) at 37oC. The pKa is 4.3 and 11.8. The BCS is Class 1. Jakavi tablets contain 5 mg, 15 mg and 20 mg of ruxolitinib as the phosphate salt.

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