| Injection, for intravenous infusion
Initial U.S. Approval: 2010
ACTEMRA (tocilizumab) is a recombinant humanized anti-human interleukin 6 (IL-6) receptor monoclonal antibody of the immunoglobulin IgG1 (gamma 1, kappa) subclass with a typical H2L2 polypeptide structure. Each light chain and heavy chain consists of 214 and 448 amino acids, respectively. The four polypeptide chains are linked intra- and inter-molecularly by disulfide bonds. ACTEMRA has a molecular weight of approximately 148 kDa.
ACTEMRA is supplied as a sterile, preservative-free solution for intravenous (IV) infusion at a concentration of 20 mg per mL. ACTEMRA is a colorless to pale yellow liquid, with a pH of about 6.5. Single-use vials are available containing 80 mg per 4 mL, 200 mg per 10 mL, or 400 mg per 20 mL of ACTEMRA. Injectable solutions of ACTEMRA are formulated in an aqueous solution containing disodium phosphate dodecahydrate and sodium dihydrogen phosphate dehydrate (as a 15 mmol per L phosphate buffer), polysorbate 80 (0.5 mg per mL), and sucrose (50 mg per mL).
| CLINICAL PHARMACOLOGY
Mechanism of Action
Tocilizumab binds specifically to both soluble and membrane-bound IL-6 receptors (sIL-6R and mIL-6R), and has been shown to inhibit IL-6-mediated signaling through these receptors. IL-6 is a pleiotropic pro-inflammatory cytokine produced by a variety of cell types including T- and B-cells, lymphocytes, monocytes and fibroblasts. IL-6 has been shown to be involved in diverse physiological processes such as T-cell activation, induction of immunoglobulin secretion, initiation of hepatic acute phase protein synthesis, and stimulation of hematopoietic precursor cell proliferation and differentiation. IL-6 is also produced by synovial and endothelial cells leading to local production of IL-6 in joints affected by inflammatory processes such as rheumatoid arthritis.
Indications and usage
| INDICATIONS AND USAGE
Rheumatoid Arthritis (RA)
Systemic Juvenile Idiopathic Arthritis (SJIA)
ACTEMRA should not be administered to patients with known hypersensitivity to ACTEMRA
| WARNINGS AND PRECAUTIONS
| ADVERSE REACTIONS
Most common adverse reactions (incidence of at least 5%): upper respiratory tract infections, nasopharyngitis, headache, hypertension, increased ALT.
To report SUSPECTED ADVERSE REACTIONS, contact Genentech at 1-888-835-2555 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
Dosage and administration
| DOSAGE AND ADMINISTRATION
ACTEMRA may be used as monotherapy or concomitantly with methotrexate or other DMARDs. The recommended dose of ACTEMRA for adult patients given once every 4 weeks as a 60-minute single intravenous drip infusion is:
Systemic Juvenile Idiopathic Arthritis
ACTEMRA may be used alone or in combination with methotrexate. The recommended dose of ACTEMRA for SJIA patients given once every 2 weeks as a 60-minute single intravenous drip infusion is:
General Considerations for Administration:
ACTEMRA for intravenous infusion should be diluted by a healthcare professional using aseptic technique as follows:
ACTEMRA treatment should be interrupted if a patient develops a serious infection until the infection is controlled.
Systemic Juvenile Idiopathic Arthritis:
| DOSAGE FORMS AND STRENGTHS
Single-use vials of ACTEMRA (20 mg per mL):
80 mg per 4 mL
HOW SUPPLIED/STORAGE AND HANDLING
Individually packaged, single-use vials:
NDC 50242-135-01 providing 80 mg per 4 mL
NDC 50242-136-01 providing 200 mg per 10 mL
NDC 50242-137-01 providing 400 mg per 20 mL
Box of 4 single-use vials:
NDC 50242-135-04 providing 80 mg per 4 mL
NDC 50242-136-04 providing 200 mg per 10 mL
NDC 50242-137-04 providing 400 mg per 20 mL
Storage and Stability: Do not use beyond expiration date on the container. ACTEMRA must be refrigerated at 2°C to 8°C (36°F to 46°F). Do not freeze. Protect the vials from light by storage in the original package until time of use. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. If visibly opaque particles, discoloration or other foreign particles are observed, the solution should not be used.
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
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