rituximab (Rx)

Brand and Other Names:Rituxan, Rituxan Hycela
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

solution for IV (Rituxan)

  • 10mg/mL

solution for SC (Rituxan Hycela)

  • Ready-to-use SC solution contains rituximab and hyaluronidase human
  • (120mg/2000 units)/mL
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Non-Hodgkin Lymphoma

Indications

  • Relapsed or refractory, low-grade or follicular, CD20-positive, B-cell NHL as a single agent
  • Previously untreated follicular, CD20-positive, B-cell NHL in combination with first line chemotherapy and, in patients achieving a complete or partial response to rituximab in combination with chemotherapy, as single-agent maintenance therapy
  • Nonprogressing (including stable disease), low-grade, CD20-positive, B-cell NHL as a single agent after first-line cyclophosphamide, vincristine, and prednisone (CVP) chemotherapy
  • Previously untreated diffuse large B-cell, CD20-positive NHL in combination with CHOP or other anthracycline-based chemotherapy regimens

IV dose for NHL

  • 375 mg/m² IV infusion according to the following schedules 
  • Relapsed or refractory low-grade or follicular, CD20-positive, B-cell NHL: Once weekly x4-8 doses
  • Retreatment for relapsed or refractory, low-grade or follicular, CD20-positive, B-cell NHL: Once weekly x4 doses
  • Previously untreated, follicular, CD20-positive, B-cell NHL: Administer on Day 1 of each chemotherapy cycle for up to 8 doses; with complete or partial response, initiate maintenance 8 weeks following completion of combination chemotherapy as a single-agent q8weeks for 12 doses
  • Nonprogressing, low-grade, CD20-positive, B-cell NHL, after first-line CVP chemotherapy: Following completion of 6-8 cycles of CVP chemotherapy, administer once weekly for 4 doses at 6-month intervals to a maximum of 16 doses
  • Diffuse large B-cell NHL: Administer on Day 1 of each cycle of chemotherapy for up to 8 infusions

SC dose (Rituxan Hycela) for follicular lymphoma

  • Must receive at least 1 full dose of rituximab by IV infusion before starting SC administration to evaluate tolerability
  • 1400 mg/23,400 units SC according to the following schedules
  • Relapsed or refractory follicular lymphoma: Once weekly x 3 or 7 weeks following a full dose of rituximab IV at week 1 (ie, 4 or 8 weeks total)
  • Retreatment for relapsed or refractory follicular lymphoma: Once weekly x 3 weeks following a full dose of rituximab IV at week 1 (ie, 4 weeks total)
  • Nonprogressing, follicular lymphoma after first-line CVP chemotherapy: Following completion of 6–8 cycles of CVP chemotherapy and a full dose of a rituximab IV at week 1, administer once weekly for 3 weeks (ie, 4 weeks in total) at 6 month intervals to a maximum of 16 doses
  • Previously untreated follicular lymphoma: Administer on Day 1 of Cycles 2–8 of chemotherapy (every 21 days), for up to 7 cycles following a full dose of a rituximab IV on Day 1 of Cycle 1 of chemotherapy (ie, up to 8 cycles in total)
  • Previously untreated follicular lymphoma maintenance
    • In patients with complete or partial response, initiate maintenance SC treatment 8 weeks following completion rituximab SC in combination with chemotherapy
    • Administer as single-agent q8wk x 12 doses

SC dose (Rituxan Hycela) for diffuse large B-cell lymphoma

  • Must receive at least 1 full dose of rituximab by IV infusion before starting SC administration to evaluate tolerability
  • 1400 mg/23,400 units SC according to the following schedule
  • Initiate on Day 1 of cycles 2-8 of CHOP chemotherapy for up to 7 cycles following a full dose of rituximab IV (Day 1, cycle 1) of CHOP (up to 6-8 cycles)

Chronic Lymphocytic Leukemia

Indicated for untreated and previously treated CD20-positive CLL; combined therapy with fludarabine and cyclophosphamide (FC)

375 mg/m² IV infusion on day 1 of 1st cycle (for 1st cycle, administer 1 day before chemotherapy with FC), THEN  

500 mg/m² IV on day 1 of subsequent cycles (administer on same day as chemotherapy with FC)

Repeat q28 days x6 cycles

Fludarabine & cyclophosphamide dosage

  • Fludarabine: 25 mg/m² IV qDay x 3 days
  • Cyclophosphamide: 250 mg/m² IV qDay x3 days
  • Repeat q28 days x 6 cycles

SC administration (Rituxan Hycela) for CLL

  • Must receive at least 1 full dose of rituximab by IV infusion before starting SC administration to evaluate tolerability
  • 1600 mg/26,800 units SC according to the following schedule
  • Initiate on Day 1 of cycles 2-6 (every 28 days) of FC chemotherapy for a total of 5 cycles following a full dose of rituximab IV (Day 1, cycle 1) up to 6 cycles in total

Rheumatoid Arthritis

1000 mg IV infusion, repeat after 2 week (2 infusions separated by 2 week is 1 course)

Repeat course q24weeks or based on clinical evaluation (but no sooner than 16 weeks)

Used in combo with methotrexate

Premedicate with glucocorticoids 30 minutes before infusion to reduce infusion rxn

Not to exceed 1000 mg/dose

Wegener Granulomatosis

375 mg/m² IV qWeek x4 weeks 

Administration

  • Premedicate with acetaminophen and antihistamine before rituximab infusion
  • Administer methylprednisolone 1 g IV/day x1-3 days, then prednisone 1 mg/kg/day PO; not to exceed 80 mg/day and taper as clinically needed
  • Initiate glucocorticoids within 14 days prior to or with initiation or rituximab; may continue during and after the 4-week rituximab treatment course
  • Concomitant use of immunosuppressants other than corticosteroids has not been studied in Wegener granulomatosis
  • Safety and efficacy of subsequent courses of rituximab not established

Microscopic Polyangiitis

375 mg/m² IV qWeek x4 weeks 

Administration

  • Premedicate with acetaminophen and antihistamine before rituximab infusion
  • Administer methylprednisolone 1 g IV/day x1-3 days, then prednisone 1 mg/kg/day PO; not to exceed 80 mg/day and taper as clinically needed
  • Initiate glucocorticoids within 14 days prior to or with initiation or rituximab; may continue during and after the 4-week rituximab treatment course
  • Concomitant use of immunosuppressants other than corticosteroids has not been studied in microscopic polyangiitis
  • Safety and efficacy of subsequent courses of rituximab not established

Orphan Designations

Treatment of immune thrombocytopenic purpura (ITP)

Treatment of pemphigus vulgaris

Sponsor

  • Genentech, Inc; 1 DNA Way; South San Francisco, CA 94080-4990

Rasmussen Encephalitis (Orphan)

Orphan designation for treatment of Rasmussen encephalitis

Sponsor

  • Keck Graduate Institute of Applied Life Sciences; 535 Watson Drive; Claremont, California 91711

Safety and efficacy not established

Rheumatoid Arthritis: Safety and effectiveness not established; FDA has not required pediatric studies in polyarticular juvenile idiopathic arthritis (PJIA) patients <16 years due to concerns regarding the potential for prolonged immunosuppression as a result of B-cell depletion in the developing juvenile immune system

Wegener Granulomatosis: Safety and effectiveness not established

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Interactions

Interaction Checker

and rituximab

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            NHL

            • Angioedema (11%), hypotension (10%)
            • Asthenia (26%), chills (33%), dizziness (10%), fever (53%), headache (19%)
            • Pruritus (14%), rash (15%)
            • Abdominal pain (14%), diarrhea (10%), nausea (23%), vomiting (10%)
            • Leukopenia (14%), lymphopenia (48%), neutropenia (14%), thrombocytopenia (12%)
            • Back pain (10%), myalgia (10%)
            • Cough (13%), rhinitis (12%)
            • Infection (31%), night sweats (15%)

            1-10%

            NHL

            • Edema
            • Flushing
            • Hypertension
            • Anxiety
            • Anemia
            • Elevated LDH
            • Hyperglycemia
            • Bronchospasm, dyspnea, sinusitis, throat irritation, urticaria

            RA (Rituximab+Methotrexate vs Methotrexate Alone)

            • Hypertension
            • Anxiety, asthenia, chills, migraine, paresthesia, pyrexia
            • Pruritus, urticaria
            • Dyspepsia, nausea, upper abd pain
            • Hypercholesterolemia
            • Arthralgia
            • Rhinitis, throat irritation, URI

            Frequency Not Defined

            Tumor lysis syndrome

            Lymphoid malignancies

            Hypogammaglobulinemia

            Postmarketing Reports

            Grade 3-4 prolonged or late-onset neutropenia

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            Warnings

            Black Box Warnings

            Fatal infusion reaction

            • Can result in serious, including fatal reactions
            • Deaths within 24 hours of infusion have occurred
            • Approximately 80% of fatal infusion reactions occurred in association with the first infusion
            • Carefully monitor patients during infusion
            • In patients with Non-Hodgkin’s Lymphoma (NHL) receiving rituximab monotherapy, NCI-CTC Grade 3 and 4 cytopenias reported; reactions included lymphopenia, neutropenia, leukopenia, anemia, and thrombocytopenia; discontinue infusion and provide medical treatment for grade 3 or 4 reactions

            Mucocutaneous reactions (severe)

            • Severe, including fatal, mucocutaneous reactions reported including paraneoplastic pemphigus, Stevens-Johnson syndrome, lichenoid dermatitis, vesiculobullous dermatitis, and toxic epidermal necrolysis

            Progressive multifocal leukoencephalopathy

            • John Cunningham virus infection resulting in progressive multifocal leukoencephalopathy and death has been reported in patients treated with rituximab

            Reactivation of hepatitis B

            • Reactivation of hepatitis B virus (HBV) infection reported, including deaths
            • Screen all patients for HBV infection before initiating drug by measuring hepatitis B surface antigen (HBsAg) and hepatitis B core antibody (anti-HBc)
            • Consult with hepatitis experts regarding monitoring and use of HBV antiviral therapy when screening identifies patients at risk of HBV reactivation due to evidence of prior HBV infection
            • Monitor patients with evidence of prior HBV infection for clinical and laboratory signs of hepatitis B or HBV reactivation during therapy and for several months thereafter, since reactivations have occurred several months following completion of therapy
            • In patients who develop reactivation of HBV, immediately discontinue the drug and start appropriate HBV treatment, also discontinue any chemotherapy until the HBV infection is controlled or resolved
            • Because of insufficient data, no recommendation can be made regarding the resumption of the drug in patients who develop HBV reactivation hepatitis

            Contraindications

            Hypersensitivity to any component, murine proteins

            Cautions

            Cardiac arrhythmia, angina, high tumor burden, concomitant cisplatin

            Infusion reactions may occur and are potentially fatal; reactions may resolve with slowing or suspending infusion; risk diminishes with subsequent infusions

            Risk of potentially fatal mucocutaneous reactions

            Risk of potentially fatal tumor lysis syndrome

            Increased risk of potentially fatal hepatitis B virus reactivation

            Potential risk of progressive multifocal leukoencephalopathy

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: not known if excreted in breast milk, do not nurse

            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.

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            Pharmacology

            Mechanism of Action

            Humanized monoclonal antibody, binds to CD20 antigen, inducing complement- or antibody-mediated cytolysis

            Elimination

            Half-life: 59.8 hr (1st dose); 174 hr (4th dose)

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            Administration

            IV Preparation

            Reconstitution: withdraw necessary amount of rituximab and dilute to a final concentration of 1-4 mg/mL into an infusion bag containing either NS or D5W

            IV Administration

            Consider premedication (ie, acetaminophen, diphenhydramine, and/or glucocorticoids for RA) before each infusion

            Premedication with diphenhydramine and acetaminophen may attenuate infusion-related events

            Because transient hypotension may occur during infusion, consider withholding antihypertensive medications 12 hr prior to infusion

            Administer by slow IV infusion only; do not administer as an IV

            First IV infusion rate: Start 50 mg/hr; increase by 50 mg/hr q30min, not to exceed 400 mg/hr

            Drug is associated with hypersensitivity reactions which may respond to adjustments in infusion rate

            Subsequent IV infusions (90 minutes)

            • Standard IV infusions: Start 100 mg/hr, increase by 100 mg/hr q30min, not to exceed 400 mg/hr; institutional protocols may allow faster increments
            • Previously untreated patients with follicular NHL or diffuse large B-cell lymphoma: If patients did not experience a Grade 3 or 4 infusion related adverse event during Cycle 1, a 90-minute infusion can be administered in Cycle 2 with a glucocorticoid-containing chemotherapy regimen
            • Initiate at a rate of 20% of the total dose given in the first 30 minutes and the remaining 80% of the total dose given over the next 60 minutes
            • If tolerated in Cycle 2, the same rate can be used when administering the remainder of the treatment regimen (through Cycle 6 or 8)
            • Patients who have clinically significant cardiovascular disease or who have a circulating lymphocyte count ≥5000/mm³ before Cycle 2 should not be administered the 90-minute infusion

            Infusion-related adverse effects

            • Hypotension, bronchospasm, and angioedema have occurred as part of an infusion-related symptom complex
            • Interrupt infusion for severe reactions and resume at a 50% reduction in rate (eg, from 100 to 50 mg/hr) when symptoms have completely resolved
            • Treatment of these symptoms with diphenhydramine and acetaminophen is recommended
            • Additional treatment with bronchodilators or IV saline may be indicated
            • Discontinue infusions if serious or life-threatening cardiac arrhythmias

            SC Preparation

            Solution for SC is ready to use

            SC Administration

            Consider premedication (ie, acetaminophen, diphenhydramine, and/or glucocorticoids)

            Premedication with acetaminophen and diphenhydramine may attenuate infusion-related reactions

            Observe patients for 15 minutes after SC administration

            If administration is interrupted, administer at the same site or at a different site along the abdomen

            Avoid coadministering other SC medications at the same site

            Avoid injections into areas where skin appears red, bruised, tender, or hard

            Avoid injections in areas where there are moles or scars

            No data available on other injection sites

            Injection Rate

            • Inject SC in abdomen
            • 1400 mg/23,400 IU/vial (1400 mg rituximab and 23,400 Units hyaluronidase human): SC over ~5 minutes
            • 1600 mg/26,800 Units vial (1600 mg rituximab and 26,800 Units hyaluronidase human): SC over ~7 minutes

            Storage

            IV

            • Store under refrigeration
            • Protect vials from direct sunlight
            • Solutions for infusion are stable at 2-8°C (36-46°F) for 24 hr

            SC

            • Store unopened vials under refrigeration
            • Protect vials from direct sunlight
            • Solutions for SC injection are stable at 2-8°C (36-46°F) for 48 hr
            • Solutions for SC injection in direct light are stable up to 30°C (86°F) for 8 hr
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            Formulary

            FormularyPatient Discounts

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            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.
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            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.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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