Rituximab (Rituxan/MabThera)

Non-Hodgkin's lymphoma (NHL) — relapsed or refractory low-grade or follicular CD20-positive B-cell; previously untreated follicular CD20-positive B-cell (with chemotherapy); non-progressing low-grade CD20-positive B-cell after first-line CVP; previously untreated diffuse large B-cell CD20-positive (with CHOP or other anthracycline-based regimen); Chronic lymphocytic leukemia (CLL) — previously untreated and previously treated (with fludarabine and cyclophosphamide)

NHL: 375 mg/m² IV as single agent or in combination, schedules vary by indication
CLL: Cycle 1: 375 mg/m² IV Day 0; Cycles 2-6: 500 mg/m² IV Day 1 every 28 days
First infusion: Start at 50 mg/h; may increase by 50 mg/h every 30 min (max 400 mg/h)
Subsequent infusions: Start at 100 mg/h; may increase by 100 mg/h every 30 min (max 400 mg/h)
Pre-medication: Acetaminophen and antihistamine before each infusion

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

None listed.

• Infusion Reactions: 77% (Grade 3-4: 10%). Most common during first infusion. Pre-medicate.
• Tumor Lysis Syndrome: Within 12-24 hours of first infusion. Monitor renal function and electrolytes.
• Infections: Serious (some fatal) bacterial, fungal, and new or reactivated viral infections. Screen for HBV before treatment.
• Cardiac Arrhythmias and Angina: Discontinue infusion for serious or life-threatening cardiac arrhythmias.
• Renal Toxicity: Tumor lysis syndrome leading to acute renal failure.
• Bowel Obstruction/Perforation: Evaluate abdominal pain complaints.
• Immunization: Do not administer live viral vaccines. Assess vaccination status before treatment.

Infusion reactions (77%), fever (53%), lymphopenia (48%), chills (33%), infection (31%), asthenia (26%), nausea (23%), headache (19%), angioedema (11%), pruritus (14%), rash (15%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Rituximab is a chimeric murine/human IgG1κ monoclonal antibody directed against the CD20 antigen found on the surface of pre-B and mature B lymphocytes. It binds CD20 and mediates B-cell lysis through complement-dependent cytotoxicity (CDC), antibody-dependent cell-mediated cytotoxicity (ADCC), and induction of apoptosis. CD20 is not shed from the cell surface and is not found in free form in circulation.

Half-life: 22 days (range 6.1-52 days). Serum levels inversely correlated with tumor burden. Detectable for 3-6 months after treatment completion.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• GELA LNH-98.5 — R-CHOP vs. CHOP in elderly patients with DLBCL. Phase III, n=399.
  🔬 NCT00003270 ↗ 📄 Primary Publication ↗

Rituximab (Rituxan/MabThera) has FDA-approved indications across the following cancer types covered on PipelineEvidence: