Drug reference

Tocilizumab

Monoclonal Antibody · Immunosuppressant, Anti-rheumatic, Anti-inflammatory

Also known as Actemra, RoActemra

Monoclonal AntibodyImmunosuppressant, Anti-rheumatic, Anti-inflammatoryATC L04AC07

CDSCO approvedSchedule HATC L04AC07

Pharmacokineticsplasma · t hours

ONSET: 3w · Clinical improvement can be observed within 2-4 weeks in RA. For CRS, effects can be seen within hours.
PEAK: 2.5d · IV: At the end of the infusion (around 1 hour). SC: 2-3 days.
t½: 6.5d · Dose-dependent. For RA: Approximately 11 days (4 mg/kg IV) to 13 days (8 mg/kg IV). For SJIA: 5-8 days. For CRS: around 1.5-2 days in high dose situations.
DURATION: 3w · Weeks, depending on dose and indication (e.g., 2-4 weeks between doses for chronic conditions).

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA Pregnancy Category C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

FDA category + note

Top interactionssee all 12 →

AbataceptSevereDatabaseDDInter
AdalimumabSevereDatabaseDDInter
AnakinraSevereDatabaseDDInter
BaricitinibSevereDatabaseDDInter

Mechanism

Tocilizumab is a recombinant humanized anti-human interleukin-6 (IL-6) receptor monoclonal antibody. It specifically binds to both soluble and membrane-bound IL-6 receptors (sIL-6R and mIL-6R), thereby inhibiting IL-6-mediated signaling. This inhibition reduces inflammatory responses driven by IL-6, a key cytokine involved in various inflammatory and autoimmune diseases.

Indications

Rheumatoid Arthritis (moderate to severe active, in adults inadequate response to other DMARDs)Giant Cell Arteritis (GCA) in adultsPolyarticular Juvenile Idiopathic Arthritis (PJIA) in patients 2 years of age and olderSystemic Juvenile Idiopathic Arthritis (SJIA) in patients 2 years of age and olderCytokine Release Syndrome (CRS) severe or life-threatening due to CAR T-cell therapy in adults and pediatric patients 2 years and olderCOVID-19 associated pneumonia requiring supplemental oxygen or mechanical ventilation (Conditional approval/Emergency Use Authorization for specific severe cases)rheumatoid arthritis in patients who do not adequately respond to one or more disease-modifying agentssystemic juvenile idiopathic arthritisgiant cell arteritispolyarticular juvenile idiopathic arthritiscytokine release syndrome

Dosing

Adult: RA (IV): 4 mg/kg followed by 8 mg/kg every 4 weeks. Doses over 800mg per infusion are not recommended. RA (SC): 162 mg every week or 162 mg every two weeks (for patients <100kg or >=100kg respectively). GCA (SC): 162 mg every week or 162 mg every two weeks.…
Pediatric: SJIA (IV): >=30 kg: 8 mg/kg every 2 weeks. <30 kg: 10 mg/kg every 2 weeks. SJIA (SC): >=30 kg: 162 mg every 2 weeks. <30 kg: 162 mg every 3 weeks. PJIA (IV): >=30 kg: 8 mg/kg every 4 weeks. <30 kg: 10 mg/kg every 4 weeks. PJIA (SC): >=30 kg: 162 mg every 2 weeks. CRS (IV): 8 mg/kg for patients >=30 kg, 12 mg/kg for patients <30 kg.
Renal adjustment: No specific dose adjustment is required for mild to moderate renal impairment. Use with caution in severe renal impairment (CrCl < 30 mL/min) due to lack of data.
Hepatic adjustment: No formal studies in patients with hepatic impairment. Use with caution in patients with pre-existing liver disease or transaminase elevations. Avoid initiation in patients with ALT/AST > 5 times ULN. Monitor liver enzymes regularly.
Geriatric: No specific dose adjustment is required. However, geriatric patients may be at a higher risk of serious infections; monitor closely.
Max dose: Generally, a single IV dose for RA or CRS should not exceed 800 mg.

Pharmacokinetics

Onset

Clinical improvement can be observed within 2-4 weeks in RA. For CRS, effects can be seen within hours.

Peak effect

IV: At the end of the infusion (around 1 hour). SC: 2-3 days.

Duration

Weeks, depending on dose and indication (e.g., 2-4 weeks between doses for chronic conditions).

Half-life

Dose-dependent. For RA: Approximately 11 days (4 mg/kg IV) to 13 days (8 mg/kg IV). For SJIA: 5-8 days. For CRS: around 1.5-2 days in high dose situations.

Bioavailability

Subcutaneous: 79% for 162 mg once weekly, 81% for 162 mg every 2 weeks. Intravenous: 100%.

Protein binding

Not applicable in the traditional sense for monoclonal antibodies, as it is a large protein.

Metabolism

Eliminated via two pathways: target-mediated elimination (binding to soluble and membrane-bound IL-6 receptors) and non-specific catabolism like other endogenous proteins (reticuloendothelial system). Not metabolized by cytochrome P450 enzymes.

Excretion

Elimination primarily occurs via target-mediated disposition (binding to IL-6 receptors) and non-specific catabolism of immunoglobulins.

Contraindications

Known hypersensitivity to tocilizumab or any of its excipients
Patients with active severe infections (e.g., tuberculosis, sepsis, serious opportunistic infections)
live vaccines

Side effects

Common

Upper respiratory tract infectionsNasopharyngitisHeadacheHypertensionIncreased alanine aminotransferase (ALT)Increased aspartate aminotransferase (AST)Injection site reactions (for SC administration)Hyperlipidemia

Serious

Serious infections (e.g., tuberculosis, bacterial, invasive fungal, viral, opportunistic infections)
Gastrointestinal perforation
Hypersensitivity reactions (including anaphylaxis)
Hepatotoxicity (liver injury)
Neutropenia
Thrombocytopenia
Demyelinating disorders
Increased risk of malignancy (theoretical but not consistently proven)
increased risk of serious infections
serious cases of hepatoxicity

Pregnancy & lactation

Pregnancy

Lactation

It is unknown whether tocilizumab is excreted in human milk. Human IgG is excreted in milk, and the potential for absorption and harm to the infant is unknown. A decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.