Tocilizumab

What is Tocilizumab?

• Tocilizumab (ACTEMRA) is an interleukin-6 (IL-6) receptor antagonist used in the therapy of rheumatoid arthritis and other autoinflammatory conditions.

What are the uses of this medicine?

• ACTEMRA is a prescription medicine called an Interleukin-6 (IL-6) receptor antagonist. ACTEMRA is used:

• To treat adults with moderately to severely active rheumatoid arthritis (RA), after at least one other medicine called a Disease-Modifying Anti-Rheumatic Drug (DMARD) has been used and did not work well.
• To treat adults with giant cell arteritis (GCA).
• For slowing the rate of decline in lung function in adults with systemic sclerosis-associated interstitial lung disease (SSc-ILD) (also known as scleroderma associated ILD).
• To treat people with active Polyarticular Juvenile Idiopathic Arthritis (PJIA) ages 2 and above.
• To treat people with active Systemic Juvenile Idiopathic Arthritis (SJIA) ages 2 and above.
• To treat people age 2 years and above who experience severe or life-threatening Cytokine Release Syndrome (CRS) following chimeric antigen receptor (CAR) T cell treatment.

How does this medicine work?

• Tocilizumab (toe” si liz’ ue mab) is humanized IgG1 monoclonal antibody to the IL-6 receptor that is used largely as therapy of refractory rheumatoid arthritis and other inflammatory arthridites.
• Tocilizumab blocks the action of IL-6, which is a key proinflammatory cytokine that mediates a wide spectrum of biologic activities including activation of T cells, differentiation of B cells, induction of acute phase reactants, proliferation of fibroblasts, and damage to cartilage and joints.
• IL-6 levels are elevated in patients with active rheumatoid arthritis.
• In controlled trials and open label studies, tocilizumab therapy led to improvements in symptoms and laboratory abnormalities associated with several forms of inflammatory arthritis.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to tocilizumab, or any of the ingredients in ACTEMRA.

What drug interactions can this medicine cause?

• ACTEMRA has not been studied in combination with biological DMARDs such as TNF antagonists.
• Exercise caution when coadministering ACTEMRA with CYP3A4 substrate drugs where decrease in effectiveness is undesirable, e.g., oral contraceptives, lovastatin, atorvastatin, etc.
• Avoid use of live vaccines concurrently with ACTEMRA.

Is this medicine FDA approved?

• Tocilizumab was approved for use in the United States in 2010 and current indications include rheumatoid arthritis and both the polyarticular and systemic forms of juvenile idiopathic arthritis (formerly juvenile rheumatoid arthritis).
• Tocilizumab is considered a disease modifying antirheumatic drug (DMARD) and improves signs and symptoms of disease and decreases cartilage and tissue destruction.

How should this medicine be used?

Recommended dosage: Rheumatoid Arthritis: Recommended Adult Intravenous Dosage:

• When used in combination with DMARDs or as monotherapy the recommended starting dose is 4 mg per kg every 4 weeks followed by an increase to 8 mg per kg every 4 weeks based on clinical response.

Recommended Adult Subcutaneous Dosage:

• Patients less than 100 kg weight:162 mg administered subcutaneously every other week, followed by an increase to every week based on clinical response
• Patients at or above 100 kg weight:162 mg administered subcutaneously every week

Giant Cell Arteritis: Recommended Adult Subcutaneous Dosage:

• The recommended dose of ACTEMRA for adult patients with GCA is 162 mg given once every week as a subcutaneous injection, in combination with a tapering course of glucocorticoids.
• A dose of 162 mg given once every other week as a subcutaneous injection, in combination with a tapering course of glucocorticoids, may be prescribed based on clinical considerations.
• ACTEMRA can be used alone following discontinuation of glucocorticoids.

Systemic Sclerosis-Associated Interstitial Lung Disease (SSc-ILD): Recommended Adult Subcutaneous Dosage:

• The recommended dose of ACTEMRA for adult patients with SSc-ILD is 162 mg given once every week as a subcutaneous injection.

Polyarticular Juvenile Idiopathic Arthritis: Recommended Intravenous PJIA Dosage Every 4 Weeks:

• Patients less than 30 kg weight:10 mg per kg
• Patients at or above 30 kg weight:8 mg per kg

Recommended Subcutaneous PJIA Dosage:

• Patients less than 30 kg weight:162 mg once every three weeks
• Patients at or above 30 kg weight:162 mg once every two weeks

Systemic Juvenile Idiopathic Arthritis: Recommended Intravenous SJIA Dosage Every 2 Weeks:

• Patients less than 30 kg weight:12 mg per kg
• Patients at or above 30 kg weight:8 mg per kg

Recommended Subcutaneous SJIA Dosage:

• Patients less than 30 kg weight:162 mg every two weeks
• Patients at or above 30 kg weight:162 mg every week

Cytokine Release Syndrome: Recommended Intravenous CRS Dosage:

• Patients less than 30 kg weight:12 mg per kg
• Patients at or above 30 kg weight:8 mg per kg

Administration: Into a vein (IV or intravenous infusion) for Rheumatoid Arthritis, PJIA, SJIA, or CRS:

• If your healthcare provider prescribes ACTEMRA as an IV infusion, you will receive ACTEMRA from a healthcare provider through a needle placed in a vein in your arm. The infusion will take about 1 hour to give you the full dose of medicine.
• For rheumatoid arthritis or PJIA you will receive a dose of ACTEMRA about every 4 weeks.
• For SJIA you will receive a dose of ACTEMRA about every 2 weeks.
• For CRS you will receive a single dose of ACTEMRA, and if needed, additional doses.
• While taking ACTEMRA, you may continue to use other medicines that help treat your rheumatoid arthritis, PJIA, or SJIA such as methotrexate, non-steroidal anti-inflammatory drugs (NSAIDs) and prescription steroids, as instructed by your healthcare provider.
• Keep all of your follow-up appointments and get your blood tests as ordered by your healthcare provider.

Under the skin (SC or subcutaneous injection) for Rheumatoid Arthritis, Giant Cell Arteritis, SSc-ILD, PJIA or SJIA:

• ACTEMRA is available as a single-dose Prefilled Syringe or single-dose prefilled ACTPen® autoinjector.
• You may also receive ACTEMRA as an injection under your skin (subcutaneous). If your healthcare provider decides that you or a caregiver can give your injections of ACTEMRA at home, you or your caregiver should receive training on the right way to prepare and inject ACTEMRA. Do not try to inject ACTEMRA until you have been shown the right way to give the injections by your healthcare provider.
• For PJIA or SJIA, you may self-inject with the Prefilled Syringe or prefilled ACTPen® autoinjector, or your caregiver can give you ACTEMRA, if both your healthcare provider and parent/legal guardian find it appropriate.
• Your healthcare provider will tell you how much ACTEMRA to use and when to use it.

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

This medicine is available in fallowing doasage form: As Intravenous Infusion

• Injection: 80 mg/4 mL (20 mg/mL), 200 mg/10 mL (20 mg/mL), 400 mg/20 mL (20 mg/mL) in single-dose vials for further dilution prior to intravenous infusion

Subcutaneous Injection

• Injection: 162 mg/0.9 mL in a single-dose prefilled syringe or single-dose prefilled ACTPen® autoinjector

This medicine is available in fallowing brand namesː

• ACTEMRA

What side effects can this medication cause?

The most common side effects of this medicine include:

• upper respiratory tract infections (common cold, sinus infections)
• headache
• increased blood pressure (hypertension)
• injection site reactions

ACTEMRA can cause serious side effects, including:

• Serious Infections
• Tears (perforation) of the stomach or intestines
• Liver problems (Hepatotoxicity)
• Changes in certain laboratory test results
• Cancer
• Hepatitis B infection
• Serious Allergic Reactions
• Nervous system problems

What special precautions should I follow?

• Serious and sometimes fatal infections due to bacterial, mycobacterial, invasive fungal, viral, protozoal, or other opportunistic pathogens have been reported in patients receiving immunosuppressive agents including ACTEMRA. Do not administer ACTEMRA during an active infection, including localized infections. If a serious infection develops, interrupt ACTEMRA until the infection is controlled.
• Evaluate patients for tuberculosis risk factors and test for latent infection prior to initiating ACTEMRA.
• Viral reactivation has been reported with immunosuppressive biologic therapies and cases of herpes zoster exacerbation were observed in clinical studies with ACTEMRA.
• Events of gastrointestinal perforation have been reported in clinical trials, primarily as complications of diverticulitis in patients treated with ACTEMRA. use with caution in patients who may be at increased risk.
• Serious cases of hepatic injury have been observed in patients taking intravenous or subcutaneous ACTEMRA. Monitor patients for signs and symptoms of hepatic injury. Modify or discontinue ACTEMRA if abnormal liver tests persist or worsen or if clinical signs and symptoms of liver disease develop.
• Laboratory monitoring—recommended due to potential consequences of treatment-related changes in neutrophils, platelets, lipids, and liver function tests.
• Hypersensitivity reactions, including anaphylaxis and death have occurred. Do not administer ACTEMRA to patients with known hypersensitivity to ACTEMRA
• Avoid use of live vaccines concurrently with ACTEMRA as clinical safety has not been established.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• No adverse drug reactions were observed.

Treatment of overdosage:

• In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions.
• Patients who develop adverse reactions should receive appropriate symptomatic treatment.

Can this medicine be used in pregnancy?

• The limited available data with ACTEMRA in pregnant women are not sufficient to determine whether there is a drug-associated risk for major birth defects and miscarriage.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ACTEMRA during pregnancy. Physicians are encouraged to register patients and pregnant women are encouraged to register themselves by calling 1-877-311-8972.

Can this medicine be used in children?

ACTEMRA by intravenous use is indicated for the treatment of pediatric patients with:

• Active systemic juvenile idiopathic arthritis in patients 2 years of age and older
• Active polyarticular juvenile idiopathic arthritis in patients 2 years of age and older
• Severe or life-threatening CAR T cell-induced cytokine release syndrome (CRS) in patients 2 years of age and older.

ACTEMRA by subcutaneous use is indicated for the treatment of pediatric patients with:

• Active polyarticular juvenile idiopathic arthritis in patients 2 years of age and older
• Active systemic juvenile idiopathic arthritis in patients 2 years of age and older

• The safety and effectiveness of ACTEMRA in pediatric patients with conditions other than PJIA, SJIA or CRS have not been established. The safety and effectiveness in pediatric patients below the age of 2 have not been established in PJIA, SJIA, or CRS.

What are the active and inactive ingredients in this medicine?

• Active ingredient: tocilizumab.
• Inactive ingredients of Intravenous ACTEMRA: disodium phosphate dodecahydrate/sodium dihydrogen phosphate dihydrate buffered solution, polysorbate 80, sucrose, and water for Injection.
• Inactive ingredients of Subcutaneous ACTEMRA: L-arginine hydrochloride, L-histidine, L-histidine hydrochloride monohydrate, L-methionine, polysorbate 80, and water for Injection.

Who manufactures and distributes this medicine?

Manufactured by: Genentech, Inc. A Member of the Roche Group 1 DNA Way South San Francisco, CA

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

• Do not use beyond expiration date on the container, package, prefilled syringe, or autoinjector.
• ACTEMRA must be refrigerated at 36°F to 46°F (2ºC to 8ºC).
• Do not freeze.
• Protect the vials, syringes, and autoinjectors from light by storage in the original package until time of use, and keep syringes and autoinjectors dry.

antirheumatic agents

• gold preparations
  • auranofin, gold salts, gold sodium thiomalate

• interleukin receptor antagonists
  • anakinra, canakinumab, rilonacept, sarilumab, tocilizumab

• major immunosuppressive agents (also used in transplant medicine)
  • cyclosporine, mycophenylate, sirolimus, tacrolimus

• monoclonal antibodies
  • adalimumab, canakinumab, certolizumab, golimumab, infliximab, rituximab, sarilumab, tocilizumab, ustekinumab

• thiopurines
  • azathioprine, mercaptopurine, thioguanine

• tumor necrosis factor antagonists
  • adalimumab, certolizumab, etanercept, golimumab, infliximab

• tyrosine (janus) kinase inhibitors
  • baricitinib, tofacitinib

• miscellaneous
  • abatacept, flavocoxid, hydroxychloroquine, leflunomide, methotrexate, penicillamine

• Dailymed label info on Tocilizumab
• FDA Tocilizumab

Tocilizumab Resources
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