ruxolitinib (Rx)

Brand and Other Names:Jakafi
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 5mg
  • 10mg
  • 15mg
  • 20mg
  • 25mg

Myelofibrosis

Kinase inhibitor indicated for treatment of patients with intermediate or high-risk myelofibrosis (MF), including primary MF, post-polycythemia vera MF and post-essential thrombocythemia MF

Initial dose

  • Platelet count >200 x10^9/L: 20 mg PO BID
  • Platelet count 100-200 x10^9/L: 15 mg PO BID
  • Platelet count 50 to <100 x10^9/L: 5 mg PO BID

Insufficient response for patients starting treatment with a platelet count ≥100 X 10^9/L

  • If response is insufficient and platelet count and ANC are adequate, dose may be increased in 5 mg BID increments; not to exceed 25 mg PO BID
  • Do not increase dose during the first 4 weeks of therapy and no more frequently than q2Weeks
  • Consider dose increases in patients who meet all of the following conditions:
    • Failure to achieve a reduction from pretreatment baseline in either palpable spleen length of 50% or a 35% reduction in spleen volume as measured by CT or MRI
    • Platelet count >125 x10^9/L at 4 weeks and never <100 x10^9/L
    • ANC levels >0.75 x10^9/L
    • Long-term maintenance at 5 mg BID has not shown responses and limit continued use at this dose to patients in whom the benefits outweigh the potential risks
    • Discontinue if there is no spleen size reduction or symptom improvement after 6 months of therapy

Insufficient response for patients starting treatment with a platelet count 50 x 10^9/L to <100 x 10^9/L

  • If response is insufficient and platelet count and ANC are adequate, doses may be increased by increments of 5 mg qDay to up to 10 mg BID
  • Do not increase dose during the first 4 weeks of therapy and no more frequently than q2Weeks
  • Consider dose increases in patients who meet all of the following conditions:
    • Platelet count has remained at least 40 x 10^9/L
    • Platelet count has not fallen by >20% in the prior 4 weeks
    • ANC >1 x 10^9/L
    • No dose reduction or interruption for an adverse event or hematological toxicity in the prior 4 weeks
  • Continuation of treatment for >6 months should be limited to patients in whom the benefits outweigh the potential risks
  • Discontinue treatment if there is no spleen size reduction or symptom improvement after 6 months of therapy

Polycythemia Vera

Indicated for polycythemia vera in patients who have had an inadequate response to or are intolerant of hydroxyurea

Initial: 10 mg PO BID

Increasing dose for insufficient response

  • If response is insufficient and platelet, hemoglobin, and neutrophil counts are adequate, doses may be increased in 5 mg BID increments to a maximum of 25 mg BID
  • Doses should not be increased during the first 4 weeks of therapy and not more frequently than q2Week
  • Consider dose increases in patients who meet all of the following criteria:
    • Inadequate efficacy as demonstrated by ≥1 of the following: continued need for phlebotomy, WBC > ULN, platelet count >ULN, palpable spleen that is reduced by <25% from baseline
    • Platelet count ≥140 x10^9/L
    • Hemoglobin ≥2 g/dL
    • ANC ≥1.5 x 10^9/L

Acute Graft versus Host Disease

Indicated for treatment of steroid-refractory acute graft-versus-host disease (GVHD)

Initial dose: 5 mg PO BID; may increase to 10 mg BID after at least 3 days if ANC and platelet counts have not decreased by ≥50% compared to baseline

Consider tapering after 6 months in patients with response who have discontinued therapeutic doses of corticosteroids

Tapering dose

  • Taper by 1 dose level ~q8Weeks (eg, 10 mg BID to 5 mg BID to 5 mg qDay)
  • Patients unable to tolerate 5 mg qDay: Interrupt treatment until clinical and/or laboratory parameters recover
  • If acute GVHD signs or symptoms recur during or after taper, consider retreatment

Dosage Modifications (MF)

Dosage modification for bleeding (regardless of platelet count)

  • Interrupt treatment until bleeding resolved; consider resuming at prior dose if underlying cause of bleeding has resolved or at a reduced dose if underlying cause of bleeding persists

Treatment interruptions in patients starting treatment with a platelet count ≥100 x 10^9/L

  • Interrupt treatment for platelet count <50 x 10^9/L or ANC <0.5 x 10^9/L
  • After recovery of platelet counts >50 x 10^9/L and ANC >0.75 X 10^9/L, restart dose
  • Restart doses after interruption are as follows
    • Restart dose at least 5 mg BID below the dose at interruption; maximum doses listed below
    • Platelet count ≥125 x10^9/L: 20 mg BID
    • Platelet count 100 to <125 x10^9/L: 15 mg BID
    • Platelet count 75 to <100 x10^9/L: 10 mg BID for at least 2 weeks; if stable, may increase to 15 mg BID
    • Platelet count 50 to <75 x10^9/L: 5 mg BID for at least 2 weeks; if stable, may increase to 10 mg BID
    • Platelet count <50 x10^9/L: Continue to hold dose
    • After ANC recovers to ≥0.75 X 10^9/L, restart at the higher of 5 mg qDay or 5 mg BID below the largest dose in the week before treatment interruption
  • Dosage modifications for thrombocytopenia
    • Platelet count 100 to <125 x10^9/L: if taking 25 mg BID, decrease to 20 mg BID; if taking 20 mg BID, decrease to 15 mg BID; do not change dose if taking lower doses
    • Platelet count 75 to <100 x10^9/L: 10 mg BID; do not change dose if taking 5 mg BID
    • Platelet count 50 to <75 x10^9/L: 5 mg BID
    • Platelet count <50 x10^9/L: Hold dose
    • Long-term maintenance at a 5 mg BID dose has not shown responses and continued use at this dose should be limited to patients in whom the benefits outweigh the potential risks

Treatment interruption in patients starting treatment with a platelet count 50 to <75 x10^9/L

  • Interrupt treatment for platelet count <25 x 10^9/L or ANC less than 0.5 X 10^9/L
  • After recovery of platelet count >35 X 10^9/L and ANC >0.75 X 10^9/L, dosing may be restarted
  • Restart at the higher of 5 mg qDay or 5 mg BID below the largest dose in the week before treatment interruption
  • Dosage modifications for thrombocytopenia
    • Platelet count<25 x 10^9/L: Interrupt dose
    • Platelet count 25 x 10^9/L to <35 X 10^9/L AND the decrease in platelet count is <20% during the prior 4 weeks: Decrease dose by 5 mg qDay; for patients on 5 mg qDay, maintain current dose
    • Platelet count 25 x 10^9/L to <35 X 10^9/L AND the decrease in platelet count is ≥20%during the prior 4 weeks: Decrease dose by 5 mg BID; for patients on 5 mg BID, decrease dose to 5 mg qDay; for patients on 5 mg qDay, maintain current dose

Renal impairment

  • Moderate-to-severe (CrCl 15-59 mL/min)
    • Platelet count >150 x10^9/L: No dosage adjustment necessary
    • Platelet count 100-150 x10^9/L: Starting dose is 10 mg BID
    • Platelet count 50 to <100 x10^9/L: Starting dose is 5 mg qDay
    • Platelet count <50 x10^9/L: Avoid use
  • ESRD (CrCl <15 mL/min)
    • On dialysis and platelet count 100-200 x10^9/L: 15 mg once following dialysis session
    • On dialysis and platelet count >200 x10^9/L: 20 mg once following dialysis session
    • Not on dialysis: Avoid use

Hepatic impairment (any severity)

  • Platelet count >150 x10^9/L: No dosage adjustment necessary
  • Platelet count 100-150 x10^9/L: Starting dose is 10 mg BID
  • Platelet count 50 to <100 x10^9/L: Starting dose is 5 mg qDay
  • Platelet count <50 x10^9/L: Avoid use

Coadministration with strong CYP3A4 inhibitors or fluconazole

  • Reduce dose when coadministered with strong CYP3A4 inhibitors or fluconazole (≤200 mg/day)
  • Avoid fluconazole doses >200 mg/day concomitantly with ruxolitinib
  • Closely monitor blood cell counts for toxicity and adjust ruxolitinib dose if necessary when coadministered with itraconazole
  • Starting dose for patients with myelofibrosis based on platelet count
    • Platelet count ≥100 x 10^9/L: 10 mg BID
    • Platelet counts 50 to <100 x 10^9/L: 5 mg BID
  • If stable on 10 mg BID, reduce by 50% (round up to the closest available tablet strength)
  • If stable on 5 mg BID, reduce 5 mg qDay
  • If stable on 5 mg qDay, avoid strong CYP3A4 inhibitor or fluconazole treatment or interrupt ruxolitinib for the duration of strong CYP3A4 inhibitor or fluconazole use

Coadministration with CYP3A4 inducers

  • No dose adjustment recommended; however, closely monitor and titrate dose based on safety and efficacy

Dosage Modifications (PV)

Dose reductions

  • Hgb ≥12 g/dL AND platelet count ≥100 x10^9/L: No change required
  • Hgb 10 to <12 g/dL AND platelet count 75 to <100 x10^9/L: Consider dose reduction with the goal of avoiding dose interruptions for anemia and thrombocytopenia
  • Hgb 8 to <10 g/dL OR platelet count 50 to < 75 x10^9/L: Reduce dose by 5 mg BID; if already on 5 mg BID, then reduce dose to 5 mg qDay
  • Hgb <8 g/dL OR platelet count <50 x10^9/L: Interrupt dosing

Treatment interruption and restarting dosing

  • Interrupt treatment for hgb <8 g/dL, platelet counts <50 x10^9/L, or ANC <1 x10^9/L
  • After recovery to acceptable levels, dosing may be restarted
  • Use most severe category for individual parameters
    • Hgb <8 g/dL OR platelet count <50 x10^9/L OR ANC <1 x10^9/L: Continue to hold dosing
    • Hgb 8 to <10 g/dL OR platelet count 50 to <75 x10^9/L OR ANC 1 to <1.5 x10^9/L: 5 mg BID, or not to exceed 5 mg BID less than the dose which resulted in dose interruption
    • Hgb 10 to <12 g/dL OR platelet count 75 to <100 x10^9/L OR ANC 1.5 to <2 x10^9/L: 10 mg BID or not to exceed 5 mg BID less than the dose which resulted in dose interruption
    • Hgb ≥12 g/dL OR platelet count ≥100 x 10^9/L OR ANC ≥2 x10^9/L: 15 mg BID or not to exceed 5 mg BID less than the dose which resulted in dose interruption
    • Reinitiated doses: Continue dose for at least 2 weeks; if stable, may increase dose 5 mg BID
    • Patients receiving a dose of 5 mg BID and required dose interruption, may restart at 5 mg BID or 5 mg qDay, but not higher, once hemoglobin ≥10 g/dL, platelet count ≥75 x 10^9/L, and ANC ≥1.5 x 10^9/L

Renal impairment

  • Moderate-to-severe (CrCl 15-59 mL/min) with any platelet count: Starting dose is 5 mg BID
  • ESRD (CrCl <15 mL/min) on dialysis: 10 mg once after dialysis session
  • ESRD (CrCl <15 mL/min) not on dialysis: Avoid use

Hepatic impairment

  • Mild, moderate, or severe (Child-Pugh A, B, C) with any platelet count: Starting dose is 5 mg BID

Concomitant use with strong CYP3A4 inhibitors

  • Dose reductions for patients with PV on concomitant strong CYP3A4 inhibitors or fluconazole doses ≤200 mg
  • Avoid fluconazole doses >200 mg/day concomitantly with ruxolitinib
  • Closely monitor blood cell counts for toxicity and adjust ruxolitinib dose if necessary when coadministered with itraconazole
  • Starting dose for patients with PV
    • Stable on ≥10 mg BID: Reduce dose by 50% (rounded up to the closest available tablet strength)
    • Stable on 5 mg BID: Reduce to 5 mg qDay
    • Stable on 5 mg PO qDay: Avoid coadministration with strong CYP3A4 inhibitors or fluconazole treatment or interrupt ruxolitinib treatment for the duration of strong CYP3A4 inhibitor or fluconazole use

Coadministration with CYP3A4 inducers

  • No dose adjustment recommended; however, closely monitor and titrate dose based on safety and efficacy

Dose Modifications (Acute GVHD)

Taper by 1 dose level (eg, 10 mg BID to 5 mg BID to 5 mg qDay)

Clinically significant thrombocytopenia after supportive measures: Reduce dose by 1 dose level; when platelets recover to previous values, restart dose to prior dose level

ANC <1 X 10^9/L (dose-related): Hold dose for up to 14 days; resume at 1 dose level lower upon recovery

Total bilirubin elevation, no liver GVHD

  • Total bilirubin 3-5x ULN: Continue at 1 dose level lower until recovery
  • Total bilirubin >5-10x ULN: Hold dose for up to 14 days until bilirubin ≤1.5x ULN; resume at current dose upon recovery
  • Total bilirubin >10x ULN: Hold dose for up to 14 days until bilirubin ≤1.5x ULN; resume at 1 dose level lower upon recovery

Total bilirubin elevation with liver GVHD

  • Total bilirubin >3x ULN: Continue at 1 dose level lower until recovery

Renal impairment

  • Moderate or severe (CrCl 15-59 mL/min): Reduce dose to 5 mg qDay
  • ESRD (CrCl <15 mL/min) on dialysis: 5 mg once after dialysis session

Hepatic impairment

  • Mild, moderate, or severe (Child-Pugh A, B, C) with any platelet count: No dosage adjustment necessary
  • Stage 3 or 4 GvHD: Monitor blood cell counts more frequently for toxicity and consider 5 mg qDay

Concomitant use with strong CYP3A4 inhibitors

  • Dose reductions for patients with acute GvHD on concomitant strong CYP3A4 inhibitors or fluconazole doses of ≥200 mg
  • Avoid fluconazole doses >200 mg/day concomitantly with ruxolitinib
  • Coadministered with ketoconazole: Reduce dose 5 mg PO qDay
  • Coadministered with other CYP3A4 inhibitors: No dosage adjustment necessary
  • Closely monitor blood cell counts for toxicity and adjust ruxolitinib dose if necessary when coadministered with itraconazole

Coadministration with CYP3A4 inducers

  • No dose adjustment recommended; however, closely monitor and titrate dose based on safety and efficacy

Dosing Considerations

Perform complete blood cell count (CBC) and platelet count before initiating therapy, q2-4Weeks until doses are stabilized, and then as clinically indicated

Orphan Designations

Pancreatic cancer

Orphan sponsor

  • Incyte Corporation; 1801 Augustine Cut-Off; Wilmington, Delaware 19803

Dosage Forms & Strengths

tablet

  • 5mg
  • 10mg
  • 15mg
  • 20mg
  • 25mg

Acute Graft versus Host Disease

Indicated for treatment of steroid-refractory acute graft-versus-host disease (GVHD) in adults and children (≥12 years)

<12 years: Safety and efficacy not established

≥12 years

  • Initial dose: 5 mg PO BID; may increase to 10 mg BID after at least 3 days if ANC and platelet counts have not decreased by ≥50% compared to baseline
  • Consider tapering after 6 months of treatment in patients with response who have discontinued therapeutic doses of corticosteroids
  • Tapering dose
    • Taper by 1 dose level ~q8Weeks (eg, 10 mg BID to 5 mg BID to 5 mg qDay)
    • Patients unable to tolerate 5 mg qDay: Interrupt treatment until clinical and/or laboratory parameters recover
    • If acute GVHD signs or symptoms recur during or after taper, consider retreatment

Dose Modifications (Acute GVHD)

Clinically significant thrombocytopenia after supportive measures: Reduce dose by 1 dose level; when platelets recover to previous values, restart dose to prior dose level

ANC <1 X 10^9/L (dose-related): Hold dose for up to 14 days; resume at 1 dose level lower upon recovery

Total bilirubin elevation, no liver GVHD

  • Total bilirubin 3-5x ULN: Continue at 1 dose level lower until recovery
  • Total bilirubin >5-10x ULN: Hold dose for up to 14 days until bilirubin ≤1.5x ULN; resume at current dose upon recovery
  • Total bilirubin >10x ULN: Hold dose for up to 14 days until bilirubin ≤1.5x ULN; resume at 1 dose level lower upon recovery

Total bilirubin elevation with liver GVHD

  • Total bilirubin >3x ULN: Continue at 1 dose level lower until recovery

Renal impairment

  • Moderate or severe (CrCl 15-59 mL/min): Reduce dose to 5 mg qDay
  • ESRD (CrCl <15 mL/min) on dialysis: 5 mg once after dialysis session

Hepatic impairment

  • Mild, moderate, or severe (Child-Pugh A, B, C) with any platelet count: No dosage adjustment necessary
  • Stage 3 or 4 GvHD: Monitor blood cell counts more frequently for toxicity and consider 5 mg qDay

Concomitant use with strong CYP3A4 inhibitors

  • Dose reductions for patients with acute GvHD on concomitant strong CYP3A4 inhibitors or fluconazole doses of ≥200 mg
  • Avoid fluconazole doses >200 mg/day concomitantly with ruxolitinib
  • Coadministered with ketoconazole: Reduce dose 5 mg PO qDay
  • Coadministered with other CYP3A4 inhibitors: No dosage adjustment necessary
  • Closely monitor blood cell counts for toxicity and adjust ruxolitinib dose if necessary when coadministered with itraconazole

Coadministration with CYP3A4 inducers

  • No dose adjustment recommended; however, closely monitor and titrate dose based on safety and efficacy
Next:

Interactions

Interaction Checker

and ruxolitinib

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 
            Previous
            Next:

            Adverse Effects

            >10% (MF and PV)

            Anemia (96.1%)

            Thrombocytopenia (69.7%)

            Increased ALT, grade 1 (25.2%)

            Bruising (23.2%)

            Neutropenia (18.7%)

            Dizziness (18.1%)

            Increased AST, grade 1 (17.1%)

            Increased cholesterol, grade 1 (16.8%)

            Headache (14.8%)

            >10% (GvHD)

            Anemia (75%)

            Thrombocytopenia (75%)

            Thrombocytopenia, Grade 3-4 (61%)

            Neutropenia (58%)

            Infections (55%)

            Edema (51%)

            Hemorrhage (49%)

            Anemia, Grade 3-4 (45%)

            Infections, Grade 3-4 (41%)

            Neutropenia (40%)

            Elevated ALT/AST (48%)

            Fatigue (37%)

            Bacterial infections (32%)

            Bacterial infections, Grade 3-4 (28%)

            Hemorrhage, Grade 3-4 (20%)

            Fatigue, Grade 3-4 (14%)

            Edema, Grade 3-4 (13%)

            Hypertriglyceridemia (11%)

            1-10% (MF and PV)

            Urinary tract infection (9%)

            Weight gain (7.1%)

            Flatulence (5.2%)

            Herpes zoster (1.9%)

            Increased ALT, grade 2 (1.9%)

            Increased ALT, grade 3 (1.3%)

            1-10% (GvHD)

            Elevated ALT/AST, Grade 3-4 (6-8%)

            Hypertriglyceridemia, Grade 3-4 (1%)

            <1%

            Increased AST, grade 2 (0.6%)

            Increased cholesterol, grade 2 (0.6%)

            Previous
            Next:

            Warnings

            Contraindications

            None

            Cautions

            Nonmelanoma skin cancers reporrted including basal cell, squamous cell, and Merkel cell carcinoma

            Thrombocytopenia, anemia, & neutropenia

            • Perform CBC before initiating therapy and monitor as clinically indicated and dosing adjusted as required
            • Patients with platelet counts <200 x10^9/L at the start of therapy are more likely to develop thrombocytopenia during treatment
            • Thrombocytopenia was generally reversible and was usually managed by reducing the dose or temporarily withholding dose (see Adult Dosing); if clinically indicated, platelet transfusions may be administered
            • Anemia may require blood transfusions; dose modifications may also be considered
            • Neutropenia (ANC <0.5 x10^9/L) was generally reversible and was managed by temporarily withholding dose

            Infections

            • Assess for the risk of developing serious bacterial, mycobacterial, fungal, and viral infections
            • Active serious infections should have resolved before starting therapy
            • Tuberculosis (TB) infection has been reported; before initiating, evaluate patients for TB risk factors, and those at higher risk should be tested for latent infection
            • Carefully observe patients for signs and symptoms of infection and initiate appropriate treatment promptly
            • Herpes zoster: Inform patients about early signs and symptoms of herpes zoster and advise to seek treatment as early as possible
            • Progressive multifocal leukoencephalopathy (PML): Reported with ruxolitinib treatment for myelofibrosis; if suspected, discontinue drug and evaluate
            • Hepatitis B viral load (HBV-DNA titer) increases, with or without associated elevations in alanine aminotransferase and aspartate aminotransferase, reported in patients with chronic HBV infection; effect of ruxolitinib on viral replication unknown; treat and monitor patients with chronic HBV infection according to clinical guidelines

            Symptoms with dose interruption, dose tapering, or discontinuing

            • Following discontinuation/interruption, myelofibrosis symptoms may be exacerbated and general return to pretreatment levels after 1 week
            • Other adverse effects reported include fever, respiratory distress, hypotension, DIC, or multiorgan failure
            • If these symptoms occur after discontinuation or dose tapering, evaluate and treat any intercurrent illness and consider restarting ruxolitinib or increase the dose
            • Instruct patients not to interrupt or discontinue ruxolitinib without consulting their physician
            • When discontinuing or interrupting therapy for reasons other than thrombocytopenia or neutropenia, consider tapering the dose gradually rather than discontinuing abruptly

            Hyperlipidemia

            • Treatment has been associated with increases in lipid parameters including total cholesterol, low density lipoprotein, and triglycerides; assess lipid parameters approximately 8-12 weeks following initiation of therapy; monitor according to clinical guidelines for management of hyperlipidemia

            Drug interactions overview

            • CYP3A4 inhibitors
              • Ruxolitinib is predominantly metabolized by CYP3A4
              • Strong CYP3A4 inhibitors increase ruxolitinib Cmax and AUC 33% and 91%, respectively
              • Dose modification recommended when coadministered with strong CYP3A4 inhibitors (such as but not limited to boceprevir, clarithromycin, conivaptan, grapefruit juice, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, voriconazole)
            • CYP3A4 inducers
              • Coadministration with strong CYP3A4 inducers may decrease ruxolitinib exposure
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy

            When pregnant rats and rabbits were administered ruxolitinib during organogenesis adverse developmental outcomes occurred at doses associated with maternal toxicity

            There are no studies with use in pregnant women to inform drug-associated risks

            Lactation

            No data are available regarding the presence of ruxolitinib in human milk, the effects on the breast fed child, or the effects on milk production

            Ruxolitinib and/or its metabolites were present in the milk of lactating rats

            Because many drugs are present in human milk and because of the potential for thrombocytopenia and anemia shown for ruxolitinib in human studies, discontinue breastfeeding during treatment and for 2 weeks after final dose

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

            Previous
            Next:

            Pharmacology

            Mechanism of Action

            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

            Absorption

            Bioavailability: 95%

            Peak plasma time: 1-2 hr

            Distribution

            Protein bound: 97% (mostly albumin)

            Vd at steady-state: 72 L (MF); 75 L (PV)

            Metabolism

            Ruxolitinib is the predominant entity in humans representing approximately 60% of the drug-related material in circulation

            Metabolized by CYP3A4 (major)

            Metabolites: 2 major active metabolites identified representing 25% and 11% of parent AUC; these 2 metabolites have 20% and 50% of ruxolitinib’s pharmacological activity, respectively; the sum total of all active metabolites contributes 18% of the overall pharmacodynamics of ruxolitinib

            Elimination

            Half-life: 2.8- 3 hr (ruxolitinib); 5.8 hr (ruxolitinib plus metabolites); 5 hr (hepatic impairment)

            Clearance: 17.7 L/hr (women, MF); 22.1 L/hr (males, MF); 12.7 L/hr (PV); 11.9 L/hr (acute GvHD)

            Excretion: feces (22%), urine (74%); unchanged drug accounted for <1%

            Previous
            Next:

            Administration

            Oral Administration

            Take with or without food

            If a dose is missed, patients do not take an additional dose, but take the next usual prescribed dose

            When discontinuing for reasons other than thrombocytopenia, consider gradual tapering the dose (eg, by 5 mg q12hr per week)

            NG tube administration

            • If unable to ingest tablets, can be administered through a nasogastric tube (8 French or greater) as follows
              • Suspend 1 tablet in ~40 mL of water with stirring for ~10 minutes
              • Administer suspension within 6 hr after the tablet has dispersed through NG using an appropriate syringe
              • Rinse NG tube with ~75 mL of water
              • Effect of tube feeding preparations on ruxolitinib exposure during administration through NG has not been evaluated

            Storage

            Tablet: Store at room temperature 20-25°C (68-77°F); excursions permitted between 15-30°C (59-86°F)

            Suspension for NG tube: Store at room temperature 20-25°C (68-77°F) for up to 6 hr

            Previous
            Next:

            Images

            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.