Generic
Rituximab
6 brands available in the market
At a glance
Rituximab is a chimeric murine/human monoclonal antibody directed against the CD20 antigen. It is used for non-Hodgkin lymphoma (NHL), chronic lymphocytic leukemia (CLL), rheumatoid arthritis (RA), granulomatosis with polyangiitis (GPA), microscopic polyangiitis (MPA), and pemphigus vulgaris.
Description
Rituximab is a genetically engineered chimeric murine/human monoclonal IgG1 kappa antibody directed against the CD20 antigen. It binds to the CD20 antigen on cell surfaces, which regulates cell cycle initiation. It activates complement-dependent B-cell cytotoxicity and mediates cell killing through antibody-dependent cellular toxicity.
Indications
- Non-Hodgkin lymphoma (NHL) - relapsed or refractory, low-grade or follicular, CD20-positive, B-cell NHL
- Chronic lymphocytic leukemia (CLL) - previously untreated and treated CD20-positive CLL
- Rheumatoid arthritis (RA) - in combination with methotrexate
- Granulomatosis with polyangiitis (GPA) and microscopic polyangiitis (MPA) - with glucocorticoids
- Pemphigus vulgaris (PV) - moderate to severe
Therapeutic class
Cytotoxic immunosuppressants
Pharmacological class
Monoclonal Antibody (CD20)
Pharmacology
Rituximab binds to the CD20 antigen found on B-lymphocytes. It activates complement-dependent cytotoxicity (CDC) and antibody-dependent cellular cytotoxicity (ADCC), leading to B-cell depletion. Reduction of CD20-positive B-cells provides therapeutic effects in autoimmune and malignant conditions.
Mechanism of action
Depletes B-cells by binding to CD20 antigen on B-cell surfaces.
Dosage
Adult Dose (IV):
- NHL (relapsed/refractory): 375 mg/m² once weekly for 4-8 doses
- NHL (previously untreated follicular): 375 mg/m² on Day 1 of each chemo cycle (up to 8 doses); maintenance every 8 weeks for 12 doses
- DLBCL: 375 mg/m² on Day 1 of each chemo cycle (up to 8 infusions)
- CLL: 375 mg/m² (Cycle 1, day before FC); 500 mg/m² (Cycles 2-6, Day 1); q28 days x6 cycles
- RA: 1000 mg (2 infusions separated by 2 weeks); repeat q24 weeks; with methotrexate
- GPA/MPA: 375 mg/m² once weekly for 4 weeks; with glucocorticoids
- PV: 1000 mg (2 infusions separated by 2 weeks); with glucocorticoids
- Pediatric (NHL/B-AL, ≥6 months): 6 infusions with LMB chemotherapy
Administration
- IV infusion only; do not administer as IV push or bolus
- First infusion: Start at 50 mg/hr, increase by 50 mg/hr every 30 min (max 400 mg/hr)
- Subsequent infusions: Start at 100 mg/hr, increase by 100 mg/hr every 30 min (max 400 mg/hr)
- Pre-medication (glucocorticoids, antihistamines, analgesics) before each infusion
Missed dose
If you miss a dose, consult your doctor.
Side effects
Side Effects:
- Infusion-related reactions (fever, chills, rash, dyspnea, hypotension)
- Hepatitis B virus reactivation
- Infections (bacterial, fungal, viral)
- Neutropenia, thrombocytopenia, anemia
- Progressive Multifocal Leukoencephalopathy (PML)
- Tumor Lysis Syndrome (TLS)
- Severe mucocutaneous reactions (SJS, TEN)
- Headache, weakness, edema, hair loss
Precautions & warnings
- Infusion reactions can be fatal; pre-medication and monitoring required
- Hepatitis B testing before treatment; do not use in active HBV
- Discontinue if PML symptoms (new-onset neurologic manifestations) occur
- Discontinue for serious infections
- Embryo-fetal toxicity: Use effective contraception
Contraindications
- Hypersensitivity to rituximab or any component
- Active, severe infections
Drug interactions
- Cisplatin: Increased risk of renal toxicity
- Live vaccines: Decreased efficacy and increased risk of infections
Food interactions
Caution is advised when consuming alcohol with Rituximab.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects; in-utero exposure may cause B-cell lymphocytopenia; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Excreted at low concentrations in human milk; due to potential serious adverse reactions in breastfed children, do not breastfeed during treatment and for 6 months after the last dose.
Pediatric use
Indicated for pediatric NHL/B-AL (≥6 months); safety not established for other indications.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; dose adjustment may not be needed; consult your doctor.
Hepatic Impairment: Limited information on use in liver disease; do not use in active liver disease or viral hepatitis (risk of reactivation); consult your doctor.
Overdose effects
No overdose information available; consult your doctor if overused.
Storage conditions
Store vials in original carton at 2-8°C in a refrigerator; do not freeze; protect from light; keep out of reach of children.
Chemical structure
Rituximab