Rituximab

What is Rituximab?

• Rituximab (Rituxan) is a CD20-directed cytolytic antibody used to treat certain autoimmune diseases and types of cancer.

Rituximab

Rituximab mechanisms of action

Rituxima Binding to CD20 on a B Cell Surface

What are the uses of this medicine?

Rituximab Rituxan is a prescription medicine used to treat:

• Adults with Non-Hodgkin's Lymphoma (NHL): alone or with other chemotherapy medicines.
• Children 6 months of age and older with mature B-cell Non-Hodgkin's Lymphoma (NHL) and mature B-cell acute leukemia (B-AL): in combination with chemotherapy medicines.
• Adults with Chronic Lymphocytic Leukemia (CLL): with the chemotherapy medicines fludarabine and cyclophosphamide.
• Adults with Rheumatoid Arthritis (RA): with another prescription medicine called methotrexate, to reduce the signs and symptoms of moderate to severe active RA in adults, after treatment with at least one other medicine called a Tumor Necrosis Factor (TNF) antagonist has been used and did not work well
• Adults and children 2 years of age and older with Granulomatosis with Polyangiitis (GPA) (Wegener's Granulomatosis) and Microscopic Polyangiitis (MPA): with glucocorticoids, to treat GPA and MPA.
• Adults with Pemphigus Vulgaris (PV): to treat moderate to severe PV.

How does this medicine work?

• Rituximab (ri tux’ i mab) is a human mouse chimeric monoclonal immunoglobulin G1 antibody to the cell surface antigen CD20 (also known as human B lymphocyte restricted differentiation antigen: Bp35) which is found on mature B cells as well as 90% of B cell neoplasms such as non-Hodgkin lymphoma and chronic lymphocytic leukemia.
• CD20 is not present on pro-B cells, hematopoietic stem cells, normal plasma cells or other normal lymphocytes, circulating cells or tissues.
• Engagement of rituximab with CD20 leads to B cell lysis and depletion of circulating and tissue B cells for an extended period, up to 6 to 8 months.
• There is an accompanying decrease in IgG and IgM levels, but in only 10% to 15% of patients do immunoglobulin levels fall below the normal range.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Formal drug interaction studies have not been performed with Rituxan.

Is this medicine FDA approved?

• Rituximab was approved for use in non-Hodgkin lymphoma and chronic lymphocyte leukemia in the United States in 1997, and indications were subsequently expanded to severe autoimmune conditions including refractory rheumatoid arthritis and Wegener granulomatosis (granulomatosis with polyangiitis). Rituximab is used off-label and is under active investigation in several other malignant conditions and autoimmune diseases. Rituximab is available in liquid solution in single use vials of 100 and 500 mg (10 mg/mL) under the brand name Rituxan.

How should this medicine be used?

Recommended dosage:

• The dose for adult and pediatric B-cell NHL is 375 mg/m2.
• The dose for CLL is 375 mg/m2 in the first cycle and 500 mg/m2 in cycles 2–6, in combination with FC, administered every 28 days .
• The dose as a component of Zevalin® (ibritumomab tiuxetan) Therapeutic Regimen is 250 mg/m2 .
• The dose for RA in combination with methotrexate is two-1,000 mg intravenous infusions separated by 2 weeks (one course) every 24 weeks or based on clinical evaluation, but not sooner than every 16 weeks. Methylprednisolone 100 mg intravenous or equivalent glucocorticoid is recommended 30 minutes prior to each infusion.
• The induction dose for adult patients with active GPA and MPA in combination with glucocorticoids is 375 mg/m2 once weekly for 4 weeks. The follow up dose for adult patients with GPA and MPA who have achieved disease control with induction treatment, in combination with glucocorticoids is two 500 mg intravenous infusions separated by two weeks, followed by a 500 mg intravenous infusion every 6 months thereafter based on clinical evaluation .
• The induction dose for pediatric patients with GPA and MPA in combination with glucocorticoids is 375 mg/m2 once weekly for 4 weeks. The follow up dose for pediatric patients with GPA and MPA who have achieved disease control with induction treatment, in combination with glucocorticoids is two 250 mg/m2 intravenous infusions separated by two weeks, followed by a 250 mg/m2 intravenous infusion every 6 months thereafter based on clinical evaluation.
• The dose for PV is two-1,000 mg intravenous infusions separated by 2 weeks in combination with a tapering course of glucocorticoids, then a 500 mg intravenous infusion at Month 12 and every 6 months thereafter or based on clinical evaluation. Dose upon relapse is a 1,000 mg intravenous infusion with considerations to resume or increase the glucocorticoid dose based on clinical evaluation. Subsequent infusions may be no sooner than 16 weeks after the previous infusion . Methylprednisolone 100 mg intravenous or equivalent glucocorticoid is recommended 30 minutes prior to each infusion.

Administration:

• Rituxan is given by infusion through your or your child's central catheter or through a needle placed in a vein (intravenous infusion), in your or your child's arm.
• Talk to your healthcare provider about how you or your child will receive Rituxan.
• Your healthcare provider may prescribe medicines before each infusion of Rituxan to reduce infusion side effects such as fever and chills.
• Your healthcare provider should do blood test regularly to check for side effects to Rituxan.
• Before each Rituxan treatment, your healthcare provider or nurse will ask you questions about your or your child's general health. Tell your healthcare provider or nurse about any new symptoms.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection: 100 mg/10 mL (10 mg/mL) and 500 mg/50 mL (10 mg/mL) solution in single-dose vials

This medicine is available in fallowing brand namesː

• Rituxan; Riabni; Ruxience; Truxima

What side effects can this medication cause?

The most common side effects of Rituxan include:

• infusion-related reactions
• infections (may include fever, chills)
• body aches
• tiredness
• nausea

In adults with GPA or MPA the most common side effects of Rituxan also include:

• low white and red blood cells
• swelling
• diarrhea
• muscle spasms

In children with B-cell NHL or B-AL who receive Rituxan with chemotherapy, the most common side effects include:

• decreased white blood cells with fever
• mouth sores
• inflammation of the upper intestine
• serious infection throughout the body and organs (sepsis)
• changes in liver function blood tests
• low level of potassium in the blood

Other side effects with Rituxan include:

• aching joints during or within hours of receiving an infusion
• more frequent upper respiratory tract infection

TYKERB may cause serious side effects, including:

• heart problems
• liver problems
• diarrhea
• lung problems
• severe skin reactions

Rituxan can cause serious side effects, including:

• Infusion-related reactions
• Severe skin and mouth reactions
• Hepatitis B virus (HBV) reactivation
• Progressive Multifocal Leukoencephalopathy (PML)
• Tumor Lysis Syndrome (TLS)
• Serious infections
• Heart problems
• Kidney problems
• Stomach and Serious bowel problems that can sometimes lead to death

What special precautions should I follow?

• Rituxan can cause severe, including fatal, infusion-related reactions. Premedicate patients with an antihistamine and acetaminophen prior to dosing.
• Mucocutaneous reactions, some with fatal outcome, can occur in patients treated with Rituxan. Discontinue Rituxan in patients who experience a severe mucocutaneous reaction. The safety of re-administration of Rituxan to patients with severe mucocutaneous reactions has not been determined.
• Hepatitis B virus (HBV) reactivation, in some cases resulting in fulminant hepatitis, hepatic failure and death, can occur in patients treated with drugs classified as CD20-directed cytolytic antibodies, including Rituxan. Monitor patients with evidence of current or prior HBV infection for clinical and laboratory signs of hepatitis or HBV reactivation during and for several months following Rituxan therapy. HBV reactivation has been reported up to 24 months following completion of Rituxan therapy.
• JC virus infection resulting in PML and death can occur in Rituxan. Discontinue Rituxan and consider discontinuation or reduction of any concomitant chemotherapy or immunosuppressive therapy in patients who develop PML.
• Acute renal failure, hyperkalemia, hypocalcemia, hyperuricemia, or hyperphosphatemia from tumor lysis, sometimes fatal, can occur. Administer aggressive intravenous hydration and anti-hyperuricemic therapy in patients at high risk for TLS.
• Serious, including fatal, bacterial, fungal, and new or reactivated viral infections can occur during and following the completion of Rituxan-based therapy. Discontinue Rituxan for serious infections and institute appropriate anti-infective therapy . Rituxan is not recommended for use in patients with severe, active infections.
• Severe, including fatal, renal toxicity can occur after Rituxan administration. Monitor closely for signs of renal failure and discontinue Rituxan in patients with a rising serum creatinine or oliguria.
• Abdominal pain, bowel obstruction and perforation, in some cases leading to death, can occur in patients receiving Rituxan in combination with chemotherapy.
• The safety of immunization with live viral vaccines following Rituxan therapy has not been studied and vaccination with live virus vaccines is not recommended before or during treatment.
• Based on human data, Rituxan can cause fetal harm due to B-cell lymphocytopenia in infants exposed to rituximab in-utero. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception.

What to do in case of emergency/overdose?

In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Based on human data, Rituxan can cause adverse developmental outcomes.
• Advise pregnant women of the risk to a fetus.

Can this medicine be used in children?

• Rituxan is indicated for the treatment of GPA and MPA in pediatric patients 2 years of age and older with GPA and MPA.
• Rituxan is not indicated in pediatric patients less than 2 years of age with GPA or MPA.

What are the active and inactive ingredients in this medicine?

• Active ingredient: rituximab
• Inactive ingredients: polysorbate 80, sodium chloride, sodium citrate dihydrate, and water for injection, USP.

Who manufactures and distributes this medicine?

• Manufactured by: Genentech, Inc., A Member of the Roche Group, 1 DNA Way, South San Francisco, CA
• Rituxan® is a registered trademark of Biogen.

What should I know about storage and disposal of this medication?

• Store Rituxan vials refrigerated at 2°C to 8°C (36°F to 46°F).
• Rituxan vials should be protected from direct sunlight. Do not freeze or shake.

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• Dailymed label info on Rituximab
• FDA Rituximab

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