tocilizumab

REMS

Moderately to severely active rheumatoid arthritis in patients who have not responded to ≥1 disease-modifying antirheumatic drug [DMARD] (as monotherapy or in combination with methotrexate or other non-biologic DMARDs).
Active systemic juvenile idiopathic arthritis (as monotherapy or in combination with methotrexate).
Active polyarticular juvenile idiopathic arthritis (as monotherapy or in combination with methotrexate).
Giant cell arteritis.
Chimeric antigen receptor T cell-induced severe or life-threatening cytokine release syndrome.
Systemic sclerosis-associated interstitial lung disease (ILD).
Coronavirus disease 2019 (COVID-19) in hospitalized patients who are receiving systemic corticosteroids and require supplemental oxygen, noninvasive or invasive mechanical ventilation, or extracorporeal membrane oxygenation.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Active infection (for all indications other than COVID-19);
Active hepatic disease/impairment;
Absolute neutrophil count (ANC) <2000/mm³ (<500/mm³ while on therapy) or platelet count below 100,000/mm³ (<50,000/mm³ while on therapy) (for rheumatoid arthritis, giant cell arteritis, systemic sclerosis-associated ILD, polyarticular juvenile idiopathic arthritis, and systemic juvenile idiopathic arthritis);
ANC <1000/mm³ or platelet count below 50,000/mm³ (for COVID-19);
Lactation: Lactation.

Use Cautiously in:

Patients at risk for GI perforation, including patients with diverticulitis;
Renal impairment;
Hepatic impairment;
Patients with risk factors for tuberculosis (TB);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Children <2 yr (safety and effectiveness not established);
Geri: ↑risk of adverse reactions in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension

Derm: rash, STEVENS-JOHNSON SYNDROME

EENT: nasopharyngitis

GI: ↑liver enzymes, GI PERFORATION, HEPATOTOXICITY

Hemat: NEUTROPENIA, THROMBOCYTOPENIA

Metab: hyperlipidemia

Neuro: headache, dizziness

Misc: infection (including tuberculosis, disseminated fungal infections and infections with opportunistic pathogens), HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), infusion reactions

Interactions ⬆ ⬇

Drug-drug:

May alter the activity of CYP450 enzymes; the effects of the following drugs should be monitored: cyclosporine, theophylline, warfarin, hormonal contraceptives, atorvastatin, and lovastatin.
Concurrent use of other hepatotoxic medications, including methotrexate, may ↑ risk of hepatotoxicity.
May ↓ antibody response to and ↑ risk of adverse reactions to live virus vaccines; do not administer concurrently.

Availability ⬆ ⬇

Solution for intravenous injection: 20 mg/mL
Solution for SUBQ injection (autoinjectors or prefilled syringes): 162 mg/0.9 mL

Route/Dosage ⬆ ⬇

Rheumatoid Arthritis

IV (Adults ): 4 mg/kg every 4 wk; may ↑ to 8 mg/kg every 4 wk based on clinical response.
SC (Adults ≥100 kg): 162 mg once weekly.
SC (Adults <100 kg): 162 mg every 2 wk, may ↑ to every wk based on clinical response.

Systemic Juvenile Idiopathic Arthritis

IV (Children ≥2 yr and ≥30 kg): 8 mg/kg every 2 wk.
IV (Children ≥2 yr and <30 kg): 12 mg/kg every 2 wk.
SC (Children ≥2 yr and ≥30 kg): 162 mg once weekly.
SC (Children ≥2 yr and <30 kg): 162 mg every 2 wk.

Polyarticular Juvenile Idiopathic Arthritis

IV (Children ≥2 yr and ≥30 kg): 8 mg/kg every 4 wk.
IV (Children ≥2 yr and <30 kg): 10 mg/kg every 4 wk.
SC (Children ≥2 yr and ≥30 kg): 162 mg every 2 wk.
SC (Children ≥2 yr and <30 kg): 162 mg every 3 wk.

Giant Cell Arteritis

IV (Adults ): 6 mg/kg (max = 600 mg/dose) every 4 wk (with a tapering course of corticosteroids).
SC (Adults ): 162 mg once weekly (with a tapering course of corticosteroids); may also consider giving 162 mg every 2 wk (with a tapering course of corticosteroids) based on clinical response.

Cytokine Release Syndrome

IV (Adults and Children ≥2 yr and ≥30 kg): 8 mg/kg (max = 800 mg/dose) initially; if patient does not clinically improve after initial dose, up to 3 additional doses may be administered every 8 hr
IV (Adults and Children ≥2 yr and <30 kg): 12 mg/kg initially; if patient does not clinically improve after initial dose, up to 3 additional doses may be administered every 8 hr

Systemic Sclerosis-Associated Interstitial Lung Disease

SC (Adults ): 162 mg once weekly.

COVID-19

IV (Adults ): 8 mg/kg (max = 800 mg) as single dose; if clinical signs/symptoms worsen or do not improve, may administer another 8 mg/kg (max = 800 mg) dose ≥8 hr after initial dose.

US Brand Names ⬆ ⬇

Actemra, Actemra ACTPen

Action ⬆ ⬇

Acts as an inhibitor of interleukin-6 (IL-6) receptors by binding to them. IL-6 is a mediator of various inflammatory processes.

Therapeutic effects:

Slowed progression of rheumatoid arthritis, systemic/polyarticular juvenile idiopathic arthritis, giant cell arteritis.
Resolution of cytokine release syndrome.
Slowing in rate of decline in pulmonary function in systemic sclerosis-associated ILD.
Reduced mortality and prolonged time to mechanical ventilation in COVID-19.

Classifications ⬆ ⬇

Therapeutic Classification: antirheumatics, Immunosuppressant agents

Pharmacologic Classification: interleukin antagonists

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability; 80% absorbed following SUBQ administration.

Distribution: Minimally distributed to tissues.

Metabolism/Excretion: Unknown.

Half-Life: 4 mg/kg dose: up to 11 days; 8 mg/kg: up to 13 days.

Time/Action Profile ⬆ ⬇

(improvement)

ROUTE	ONSET	PEAK	DURATION
IV	within 1 mo	4 mo	unknown
SUBQ	unknown	unknown	unknown

Patient/Family Teaching ⬆ ⬇

Instruct patient on the purpose for tocilizumab. If a dose is missed, contact health care professional to schedule next infusion. Instruct patient and caregiver in correct technique for SUBQ injections and care and disposal of equipment. Advise patient and caregiver to read Medication Guide before starting therapy and with each Rx refill in case of changes.
Caution patient to notify health care professional immediately if signs of infection (fever, sweating, chills, muscle aches, cough, shortness of breath, blood in phlegm, weight loss, warm, red or painful skin or sores, diarrhea or stomach pain, burning on urination, urinary frequency, feeling tired), fever and stomach-area pain that does not go away, change in bowel habits, severe rash, swollen face, or difficulty breathing occurs while taking. If signs and symptoms of anaphylaxis occur, discontinue injections and notify health care professional immediately.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Instruct patient to notify health care professional of medication regimen prior to treatment or surgery.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Inform patient of pregnancy exposure registry that monitors pregnancy outcomes in women exposed to tocilizumab during pregnancy. Register patient by calling 1-877-311-8972; health care professional or patient can call to register.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

50242- Genentech, Inc.
- 50242-135- ACTEMRA
  - 50242-135-01- 1 VIAL, SINGLE-USE in 1 BOX (50242-135-01) > 4 mL in 1 VIAL, SINGLE-USE

50242- Genentech, Inc.
- 50242-136- ACTEMRA
  - 50242-136-01- 1 VIAL, SINGLE-USE in 1 BOX (50242-136-01) > 10 mL in 1 VIAL, SINGLE-USE

50242- Genentech, Inc.
- 50242-137- ACTEMRA
  - 50242-137-01- 1 VIAL, SINGLE-USE in 1 BOX (50242-137-01) > 20 mL in 1 VIAL, SINGLE-USE

50242- Genentech, Inc.
- 50242-138- Actemra
  - 50242-138-01- 1 SYRINGE, GLASS in 1 BOX (50242-138-01) > .9 mL in 1 SYRINGE, GLASS

50242- Genentech, Inc.
- 50242-138- Actemra
  - 50242-138-86- 1 SYRINGE, GLASS in 1 BOX (50242-138-86) > .9 mL in 1 SYRINGE, GLASS

50242- Genentech, Inc.
- 50242-143- Actemra ACTPen
  - 50242-143-01- 1 SYRINGE, GLASS in 1 BOX (50242-143-01) > .9 mL in 1 SYRINGE, GLASS

50242- Genentech, Inc.
- 50242-143- Actemra ACTPen
  - 50242-143-86- 1 SYRINGE, GLASS in 1 BOX (50242-143-86) > .9 mL in 1 SYRINGE, GLASS

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Indications ⬇