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Product Description
Composition: Each tablet contains Ruxolitinib 5 mg as Ruxolitinib
Phosphate INN.
Mechanism of Action: Ruxolitinib, a kinase inhibitor, inhibits Janus
Associated Kinases (JAKs) JAK1 and JAK2 which mediate the signaling of a
number of cytokines and growth factors that are important for hematopoiesis
and immune function. JAK signaling involves recruitment of STATs (signal
transducers and activators of transcription) to cytokine receptors, activation
and subsequent localization of STATs to the nucleus leading to modulation
of gene expression. Myelofibrosis (MF) is a myeloproliferative neoplasm
(MPN) known to be associated with dysregulated JAK1 and JAK2 signaling.
Oral administration of ruxolitinib prevented splenomegaly, preferentially
decreased JAK2V617F mutant cells in the spleen and decreased circulating
inflammatory cytokines (eg, TNF-α, IL-6).
Pharmacokinetics:
Absorption: Ruxolitinib is rapidly absorbed after oral Ruxolitinib
administration with maximal plasma concentration (Cmax) achieved within 1
to 2 hours post-dose. Oral absorption of ruxolitinib was estimated to be at
least 95%. Distribution: The mean volume of distribution of ruxolitinib at
steady-state is 72 L in patient with MF and PV in myelofibrosis patients.
Half-lives: the mean half-life of ruxolitinib & metabolites is approximately 5.8
hours. Elimination half-life: The mean elimination half-life of ruxolitinib is
approximately 3 hours AUC: Mean ruxolitinib Cmax and total exposure
(AUC) increased proportionally over a single dose range of 5 to 200 mg.
The plasma protein binding: 97%, mostly to albumin. Metabolism:
Ruxolitinib is metabolized by CYP3A4 and to a lesser extent by CYP2C9.
Excretion: Following a single oral dose of radio labeled ruxolitinib in healthy
adult subjects, elimination was predominately through metabolism with 74%
of radioactivity excreted in urine and 22% excretion via feces. Unchanged
drug accounted for less than 1% of the excreted total radioactivity.
Indications:
Myelofibrosis: Ruxolitinib is indicated for treatment of intermediate or
high-risk myelofibrosis (MF), including primary MF, post-polycythemia vera
MF and post-essential thrombocythemia MF in adults.
Polycythemia Vera: Ruxolitinib is indicated for treatment of polycythemia
vera (PV) in adults who have had an inadequate response to or are
intolerant of hydroxyurea.
Acute Graft-Versus-Host Disease: Ruxolitinib is indicated for treatment of
steroid-refractory acute graft-versus-host disease (GVHD) in adult and
pediatric patients 12 years and older.
Dosage & Administration:
Myclofibrosis: The recommended starting dose of Ruxolitinib is based on
platelet count. A complete blood count (CBC) and platelet count must be
performed before initiating therapy, every 2 to 4 weeks until doses are
stabilized, and then as clinically indicated. Doses may be titrated based on
safety and efficacy.
