- March 15, 2022
- Newsletter
- 617-430-5616
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Brand Name :
Jakafi
Synonyms :
ruxolitinib
Class :
Hematologics and Janus Kinase Inhibitors
Dosage forms & Strengths
Tablet
5mg
10mg
15mg
20mg
25mg
20
mg
Oral
twice a day
Tablet
10
mg
Oral
twice a day
Tablet
acute graft versus host disease
5
mg
Oral
twice a day
Tablet
ruxolitinib is indicated to treat polycythemia vera in patients who are intolerant to hydroxyurea and show inadequate response to the same
A dose of 10 mg orally twice daily is specified initially
chronic graft-versus-host disease
ruxolitinib is a therapeutic agent for the treatment of cGVHD in the patients who have failed the treatment of systemic therapy
A dose of 10 mg is administered orally twice daily, which can be reduced after six months of the therapy
The safety and efficacy of ruxolitinib are not found for pediatric (<12 years) dosing
Children more than 12 years are started with the treatment of 10 mg twice daily
Refer adult dosing
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it decreases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism conivaptan
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
palifermin, when administered with ruxolitinib, simultaneously increases the toxicity of each other
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
immunosuppressants increase the effect of immunosuppression of ruxolitinib
immunosuppressants increase the effect of immunosuppression of ruxolitinib
immunosuppressants increase the effect of immunosuppression of ruxolitinib
immunosuppressants increase the effect of immunosuppression of ruxolitinib
immunosuppressants increase the effect of immunosuppression of ruxolitinib
may have an increased immunosuppressive effect when combined with ruxolitinib
may have an increased immunosuppressive effect when combined with ruxolitinib
may have an increased immunosuppressive effect when combined with ruxolitinib
ruxolitinib: they may increase the immunosuppressive effect of immunostimulants
ruxolitinib: they may increase the immunosuppressive effect of immunostimulants
ruxolitinib: they may increase the immunosuppressive effect of immunostimulants
ruxolitinib: they may increase the immunosuppressive effect of immunostimulants
ruxolitinib: they may increase the immunosuppressive effect of immunostimulants
when both drugs are combined, there may be an increase in immunosuppressive activity and the risk of severe infection
may increase the immunosuppressive effect of immunosuppressants
may increase the immunosuppressive effect of immunosuppressants
may increase the immunosuppressive effect of immunosuppressants
may increase the immunosuppressive effect of Immunosuppressive agents
may increase the immunosuppressive effect of immunosuppressants
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when both drugs are combined, there may be an increased risk or severity of adverse effects
when both drugs are combined, there may be an increased metabolism of ruxolitinib
when both the drugs are combined, the risk or severity of adverse effects increases
lapatinib increases the effect of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when both drugs are combined, there may be an increase in adverse/toxic effects of immunosuppression and the risk of severe infection
when both drugs combine ruxolitinib will increase the effect of ifosfamide by affecting the enzyme CYP3A4 metabolism.
ruxolitinib effect of action increased by affecting enzyme CYP3A4 metabolism.
methimazole increases the effect of ruxolitinib by altering CYP3A4 intestinal/hepatic metabolism
Actions and Spectrum:
Actions:
Spectrum:
Frequency defined:
>10%
Anemia
Thrombocytopenia
Increased ALT
Bruising
Neutropenia
Dizziness
Increased AST
Increased cholesterol
Headache
1-10%
Urinary tract infection
Weight gain
Flatulence
Herpes zoster
Increased ALT
<1%
Increased AST
Increased cholesterol
Black Box Warning:
The FDA requires a black box warning on the label of ruxolitinib due to the risk of severe and life-threatening infections.
Contraindication/Caution:
Pregnancy consideration: The drug is toxic and unsafe for pregnant women and the developing fetus.
Breastfeeding warnings: No data on the excretion of ruxolitinib in breast milk is available. Because of possible serious effects, women are advised to breastfeed two weeks after the last dose of ruxolitinib.
Pregnancy category:
Pharmacology:
ruxolitinib is a medication that belongs to a class of drugs known as Janus kinase (JAK) inhibitors. It works by selectively inhibiting the activity of JAK1 and JAK2 enzymes, which play a critical role in the signaling pathways of many cytokines and growth factors involved in the pathogenesis of certain blood disorders.
Pharmacodynamics:
By inhibiting JAK1 and JAK2, ruxolitinib blocks the downstream effects of these signaling pathways, including the production of inflammatory cytokines and growth factors. This leads to a reduction in the size of the spleen and an improvement in disease-related symptoms in patients with myelofibrosis and polycythemia vera.
ruxolitinib has also been shown to reduce the risk of thrombotic events in patients with polycythemia vera, possibly by reducing the number of circulating blood cells.
In addition to its effects on JAK enzymes, ruxolitinib has been shown to inhibit other cellular pathways, including the signal transducer and activator of the transcription (STAT) pathway and the mitogen-activated protein kinase (MAPK) pathway. These pathways are involved in cell proliferation, differentiation, and survival, and their dysregulation has been implicated in the pathogenesis of various cancers.
Pharmacokinetics:
Absorption
The bioavailability is 95%
The peak plasma concentration is achieved in 1-2 hours
Distribution
The bound protein is 97% (primarily albumin)
The volume of distribution at steady-state is 72 L (for myelofibrosis) and 75 L (for polycythemia vera)
Metabolism
ruxolitinib is metabolized majorly by CYP3A4
Elimination and Excretion
The half-life is 2.8-3 hours (for ruxolitinib); 5.8 hours (for ruxolitinib with metabolites); 5 hours (in case of hepatic impairment)
The rate of clearance is 17.7 L/hr (for women with myelofibrosis); 22.1 L/hr (for males with, myelofibrosis); 12.7 L/hr (for polycythemia vera); 11.9 L/hr (for acute GvHD)
The drug is excreted in feces (22%), in urine (74%); and the unchanged drug is less than 1%
Administration:
ruxolitinib is available as a tablet for oral administration. The tablets should be swallowed whole with water and taken with or without food. The recommended starting dose of ruxolitinib varies depending on the indication and patient characteristics. For the treatment of myelofibrosis, the starting dose is typically 20 mg twice daily.
While treating polycythemia vera, the starting dose is typically 10 mg twice daily. Adjust the dose based on the patient’s response and tolerance to the medication. Patients should be monitored closely for adverse effects and changes in blood counts during treatment.
Patient information leaflet
Generic Name: ruxolitinib (Rx)
Pronounced: RUX-oh-LI-ti-nib
Why do we use ruxolitinib?
ruxolitinib is a hematologic agent of the JAK Inhibitor class. It is used to treat myelofibrosis and polycythemia vera, two types of blood disorders. It works by selectively inhibiting JAK enzymes, which are involved in the pathogenesis of these disorders.
ruxolitinib has been shown to reduce spleen size and symptoms in patients with myelofibrosis. It also reduces the risk of thrombotic events and improves symptoms in polycythemia vera patients.
