Rituximab (Rituxan)

General information

Class/mechanism: Anti-CD20 antibody, chimeric murine/human monoclonal IgG1 kappa, which binds to CD20 (human B-lymphocyte-restricted differentiation antigen, Bp35), which is expressed on B-cells. The Fc domain recruits immune effector functions to mediate B-cell lysis. Possible mechanisms of cell lysis include complement-dependent cytotoxicity (CDC) and antibody-dependent cell mediated cytotoxicity (ADCC).
Route: IV
Extravasation: neutral

• Rituximab (Rituxan) desensitization protocol

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• Acquired coagulopathy
• Immune thrombocytopenia (ITP)
• B-cell acute lymphoblastic leukemia
• Burkitt lymphoma
• Castleman disease
• Chronic lymphocytic leukemia
• CNS lymphoma
• Cold agglutinin disease
• Diffuse large B-cell lymphoma
• Follicular lymphoma
• Hairy cell leukemia
• HIV-associated lymphoma
• Hodgkin lymphoma
• Hodgkin lymphoma, nodular lymphocyte-predominant
• Inherited coagulopathy with inhibitor
• Mantle cell lymphoma
• Marginal zone lymphoma
• Mediastinal gray-zone lymphoma
• Post-transplant lymphoproliferative disorder
• Primary mediastinal B-cell lymphoma
• Thrombotic thrombocytopenic purpura
• Transformed lymphoma
• Waldenström macroglobulinemia

Patient drug information

• Rituximab (Rituxan) package insert
• Rituximab (Rituxan) patient drug information (Chemocare)
• Rituximab (Rituxan) patient drug information (UpToDate)

History of changes in FDA indication

Note: there is a gap in FDA labels between 1997 and 2006 on the FDA website; there are likely missing indications issued during that time period.

Chronic lymphocytic leukemia

• 2/18/2010: Approved in combination with fludarabine and cyclophosphamide (FC), for the treatment of previously untreated and previously treated patients with chronic lymphocytic leukemia (CLL). (New disease entity)

Diffuse large B-cell lymphoma

• 2/10/2006: Approved for use in the first‑line treatment of patients with diffuse large B-cell, CD20‑positive, non-Hodgkin's lymphoma in combination with CHOP or other anthracycline‑based chemotherapy regimens. (new disease entity added; scope expanded to first-line treatment; combination therapy required)
• 10/19/2012: Approved for 90-minute infusion in previously untreated diffuse large B-cell lymphoma (DLBCL) starting with cycle 2:
  • Patients who do not experience a grade 3 or 4 infusion related adverse event during cycle 1 may undergo a 90-minute infusion when used as part of a glucocorticoid-containing chemotherapy regimen. In cycle 2, 20% of the total dose is to be given over the first 30 minutes, and the remaining 80% of the total dose is to be given over the last 60 minutes. If this 90-minute infusion is tolerated, the same rate can be used for remaining cycles of the treatment.

Follicular lymphoma

• 11/26/1997: Initial FDA approval for the treatment of patients with relapsed or refractory follicular, CD20 positive, B-cell non-Hodgkin’s lymphoma.
• 9/29/2006: Approved for the first-line treatment of patients with follicular, CD20-positive B-cell non-Hodgkin’s lymphoma. (scope expanded to first-line treatment)
• 1/28/2011: Approved for maintenance therapy for patients with previously untreated follicular, CD-20 positive, B-cell non-Hodgkin lymphoma who achieve a response to rituximab in combination with chemotherapy. (Approval extended to maintenance setting)
• 10/19/2012: Approved for 90-minute infusion in previously untreated follicular Non-Hodgkin lymphoma (NHL) starting with cycle 2:
  • Patients who do not experience a grade 3 or 4 infusion related adverse event during cycle 1 may undergo a 90-minute infusion when used as part of a glucocorticoid-containing chemotherapy regimen. In cycle 2, 20% of the total dose is to be given over the first 30 minutes, and the remaining 80% of the total dose is to be given over the last 60 minutes. If this 90-minute infusion is tolerated, the same rate can be used for remaining cycles of the treatment.

Indolent (Low grade) lymphoma

• 11/26/1997: Initial FDA approval for the treatment of patients with relapsed or refractory low-grade, CD20 positive, B-cell non-Hodgkin’s lymphoma.
• 9/29/2006: Approved for the first-line treatment of patients with low grade, CD20-positive B-cell non-Hodgkin’s lymphoma. (scope expanded to first-line treatment)

Also known as

• Code names: BI 695500, IDEC-102, IDEC-C2B8, PF-05280586, RTXM83
• Brand names: Ikgdar, Mabtas, MabThera, Reditux, Ristova, Rituxan, Rituxim, Transera-Kit