Canakinumab

Trade Names:Ilaris- Injection, lyophilized powder for solution 180 mg (150 mg/mL after reconstitution)

Pharmacology

Neutralizes the biologic activity of interleukin-1beta (IL-1beta) by binding to IL-1beta and blocking its interaction with IL-1 receptors.

Pharmacokinetics

Absorption

Bioavailability is 70%; C _max is 16 mcg/mL and T _max is 7 days.

Distribution

The Vd _ss is 6.01 L in a 70 kg patient.

Elimination

Half-life is 26 days

Special Populations

No formal studies have been conducted.

No formal studies have been conducted.

T _max is 2 to 7 days and half-life ranged from 22.9 to 25.7 days.

Indications and Usage

Treatment of cryopyrin-associated periodic syndromes, including familial cold autoinflammatory syndrome and Muckle-Wells syndrome.

Contraindications

Standard considerations.

Dosage and Administration

Subcutaneous Dose based on weight.

2 mg/kg

150 mg

Subsequent doses given every 8 wk.

Subcutaneous Dose based on weight.

2 mg/kg; if response is not adequate, may increase to 3 mg/kg

150 mg.

Subsequent doses given every 8 wk.

General Advice

• For subcutaneous injection only.
• Never inject into areas where the skin is swollen or red, or into scar tissue.
• Discard any unused portion. Do not save unused solution for later administration.

Storage/Stability

Store unopened vials in refrigerator, between 36° and 46°F. Do not freeze. Protect from light. After reconstitution, solution may be kept at room temperature if used within 60 min of reconstitution. Reconstituted solution should be refrigerated between 36° and 46°F and used within 4 h of reconstitution.

Drug Interactions

Increased risk of infection.

May decrease efficacy of live vaccines. Do not give concurrently.

Closely monitor CYP-450 substrates with a narrow therapeutic index (eg, warfarin) after initiating canakinumab.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (14%); vertigo (11%).

EENT

Nasopharyngitis (34%); rhinitis (17%); pharyngitis (11%).

GI

Diarrhea (20%); nausea (14%); gastroenteritis (11%).

Local

Mild injection-site reactions (9%).

Respiratory

Bronchitis (11%).

Miscellaneous

Influenza (17%); musculoskeletal pain, weight increased (11%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 4 yr of age.

Immunosuppression

May result in an increase in malignancies.

Infection

Serious infections may occur. Monitor patient for signs and symptoms of infection (eg, cellulitis, persistent fever, sore throat). Discontinue therapy if a serious infection develops or is suspected.

Tuberculosis

Prior to initiating canakinumab, test for latent tuberculosis (TB). Treat patients testing positive in TB screening with standard medical therapy prior to treatment with canakinumab.

Vaccinations

Do not give live vaccines concomitantly.

Patient Information

• Instruct patients to inform health care provider if they have signs of an infection; have a chronic or active infection, including HIV or hepatitis B or C; or take other medications that affect their immune system.
• Advise patient to report symptoms of intolerable or persistent injection-site reactions (eg, pain, redness, swelling) to health care provider.
• Advise patient to inform health care provider before receiving live vaccines.

Copyright © 2009 Wolters Kluwer Health.