Ruxolitinib (Oral)

Uses

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 ... Read more

Dosage

Ruxolitinib (Oral) dosage

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. Platelet count greater than 200 X 10 9 /L: Starting dose 20 mg orally twice daily. Platelet count 100 X 10 9 /L to 200 X 10 9 /L: Starting dose 15 mg orally twice daily. Platelet count 50 X 10 9 /L to less than 100 X 10 9 /L: Starting dose 5 mg orally twice daily. Polycythemia Vera: The recommended starting dose of Ruxolitinib is 10 mg twice daily. Doses may be titrated based on safety and efficacy. Consider decreasing the dose to 5 mg twice daily if the hemoglobin count 8 to less than 12g/dL and the platelet count 50 to less than 75 X 10 9 L.Acute Graft-Versus-Host Disease: The recommended dose of Ruxolitinib is 5 mg twice daily. Consider increasing the dose to 10 mg twice daily after at least 3 days of treatment if the ANC and platelet counts are not decreased by 50% or more relative to the first day of dosing with ruxolitinib. Or as directed by the registered physician. Ruxolitinib is to be taken orally, with or without food. If a dose is missed, the patient should not take an additional dose, but should take the next usual prescribed dose.

Side Effects

The most common side effects are- Thrombocytopenia, Anemia and Neutropenia Risk of Infection, bruising, dizziness, headache Symptom Exacerbation Following Interruption or Discontinuation of treatment with Ruxolitinib Non-Melanoma Skin Cancer

Precaution

Thrombocytopenia, Anemia And Neutropenia: Treatment with Ruxolitinib can cause thrombocytopenia, anemia and neutropenia. Manage thrombocytopenia by reducing the dose or temporarily interrupting Ruxolitinib. Platelet transfusions may be necessary.Patients developing anemia may require blood transfusions and/or dose modifications of Ruxolitinib.Severe neutropenia (ANC less than 0.5 X 109/L) was generally reversible by withholding Ruxolitinib until recovery.Perform a pre-treatment complete blood count (CBC) and monitor CBCs every 2 to 4 weeks until doses are stabilized, and then as clinically indicated.Risk of Infection: Serious bacterial, mycobacterial, fungal and viral infections have occurred. Delay starting therapy with Ruxolitinib until active serious infections have resolved. Observe patients receiving Ruxolitinib for signs and symptoms of infection and manage promptly.Tuberculosis: Tuberculosis infection has been reported in patients receiving Ruxolitinib. Observe patients receiving Ruxolitinib for signs and symptoms of active tuberculosis and manage promptly. Prior to initiating Ruxolitinib, patients should be evaluated for tuberculosis risk factors, and those at higher risk should be tested for latent infection. Risk factors include, but are not limited to, prior residence in or travel to countries with a high prevalence of tuberculosis, close contact with a person with active tuberculosis, and a history of active or latent tuberculosis where an adequate course of treatment cannot be confirmed. For patients with evidence of active or latent tuberculosis, consult a physician with expertise in the treatment of tuberculosis before starting Ruxolitinib. The decision to continue Ruxolitinib during treatment of active tuberculosis should be based on the overall risk-benefit determination.Progressive Multifocal Leukoencephalopathy: Progressive multifocal leukoencephalopathy (PML) has occurred with Ruxolitinib treatment. If PML is suspected, stop Ruxolitinib and evaluate.Herpes Zoster: Advise patients about early signs and symptoms of herpes zoster and to seek treatment as early as possible if suspected.Hepatitis B: Hepatitis B viral load (HBV-DNA titer) increases, with or without associated elevations in alanine aminotransferase and aspartate aminotransferase, have been reported in patients with chronic HBV infections taking Ruxolitinib. The effect of Ruxolitinib on viral replication in patients with chronic HBV infection is unknown. Patients with chronic HBV infection should be treated and monitored according to clinical guidelines.Symptom Exacerbation Following Interruption or Discontinuation Of Treatment With Ruxolitinib: Following discontinuation of Ruxolitinib, symptoms from myeloproliferative neoplasms may return to pretreatment levels over a period of approximately one week. Some patients with MF have experienced one or more of the following adverse events after discontinuing Ruxolitinib: fever, respiratory distress, hypotension, DIC, or multi organ failure. If one or more of these occur after discontinuation of, or while tapering the dose of Ruxolitinib, evaluate for and treat any intercurrent illness and consider restarting or increasing the dose of Ruxolitinib. Instruct patients not to interrupt or discontinue Ruxolitinib therapy without consulting their physician. When discontinuing or interrupting therapy with Ruxolitinib for reasons other than thrombocytopenia or neutropenia, consider tapering the dose of Ruxolitinib gradually rather than discontinuing abruptly.Non-Melanoma Skin Cancer: Non-melanoma skin cancers including basal cell, squamous cell, and Merkel cell carcinoma have occurred in patients treated with Ruxolitinib. Perform periodic skin examinations.Lipid Elevations: Treatment with Ruxolitinib has been associated with increases in lipid parameters including total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides. The effect of these lipid parameter elevations on cardiovascular morbidity and mortality has not been determined in patients treated with Ruxolitinib. Assess lipid parameters approximately 8-12 weeks following initiation of Ruxolitinib therapy. Monitor and treat according to clinical guidelines for the management of hyperlipidemia.

Interaction

Fluconazole: Concomitant administration of Ruxolitinib with fluconazole greater than 200 mg daily may increase ruxolitinib exposure due to inhibition of both the CYP3A4 and CYP2C9 metabolic pathways. Increased exposure may increase the risk of exposure-related adverse reactions. Avoid the concomitant use of Ruxolitinib with fluconazole doses of greater than 200 mg daily except in patients with acute GVHD.Strong CYP3A4 Inhibitors: Concomitant administration of Ruxolitinib with strong CYP3A4 inhibitors increases ruxolitinib exposure. Increased exposure may increase the risk of exposure-related adverse reactions. Consider dose reduction when administering Ruxolitinib with strong CYP3A4 inhibitors. In patients with acute GVHD, reduce Ruxolitinib dose as recommended only when coadministered with ketoconazole, and monitor blood counts more frequently for toxicity and adjust the dose if necessary when coadministered with itraconazole.Strong CYP3A4 Inducers: Concomitant administration of Ruxolitinib with strong CYP3A4 inducers may decrease ruxolitinib exposure. No dose adjustment is recommended; however, monitor patients frequently and adjust the Ruxolitinib dose based on safety and efficacy.

Pregnancy & Breastfeeding use

There are no adequate and well-controlled studies in pregnant women. It is not known whether Ruxolitinib is excreted in human milk. Because many drugs are excreted in human milk, breastfeeding should be discontinued during treatment with Ruxolitinib and for two weeks after the final dose.

Contraindication

It is contraindicated in patients with a history of hypersensitivity to Ruxolitinib or any other components of this product.

Special Warning

Use in children: The safety and effectiveness of Ruxolitinib in pediatric patients have not been established.

Acute Overdose

There is no known antidote for overdoses with Ruxolitinib. Single doses up to 200 mg have been given with acceptable acute tolerability. Higher than recommended repeat doses are associated with increased myelosuppression including leukopenia, anemia and thrombocytopenia. Appropriate supportive treatment should be given. Hemodialysis is not expected to enhance the elimination of Ruxolitinib.

Storage Condition

Store below 30°C in a dry place, away from sunlight. Keep out of reach of children.

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