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Ustekinumab (Stelara)
Ustekinumab, marketed under the brand name Stelara, is a monoclonal antibody biologic medication that targets interleukin (IL)-12 and IL-23, key cytokines involved in inflammatory and immune responses. It is used to treat autoimmune conditions such as psoriasis, psoriatic arthritis, Crohn’s disease, and ulcerative colitis. This article synthesizes information from the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to provide a detailed overview of ustekinumab, including its mechanism, uses, dosing, side effects, precautions, and drug interactions.
Ustekinumab binds to the p40 subunit shared by IL-12 and IL-23, inhibiting their interaction with cell surface receptors. This action:
- Reduces inflammation: Suppresses Th1 and Th17 lymphocyte activation, which drive inflammatory pathways in autoimmune diseases (Lippincott, Lange).
- Modulates immune response: Decreases production of pro-inflammatory cytokines (e.g., TNF-α, IL-17, IL-22), alleviating symptoms and slowing disease progression (BNF).
Administered subcutaneously or intravenously, ustekinumab has a half-life of approximately 15–32 days, allowing for extended dosing intervals (Lippincott).
- Plaque Psoriasis:
- Treats moderate to severe psoriasis in adults and adolescents (≥12 years) (BNF).
- Psoriatic Arthritis:
- Reduces joint inflammation and inhibits structural damage (Lippincott).
- Crohn’s Disease:
- Induces and maintains remission in adults with moderate to severe disease (Lange).
- Ulcerative Colitis:
- Approved for adults with moderate to severe active disease (BNF).
- Plaque Psoriasis:
- Initial dose: 45 mg (≤100 kg) or 90 mg (>100 kg) subcutaneously, followed by 45–90 mg every 12 weeks (BNF).
- Psoriatic Arthritis:
- 45 mg subcutaneously at weeks 0, 4, and every 12 weeks thereafter (Lippincott).
- Crohn’s Disease:
- Weight-based intravenous induction: ~6 mg/kg at week 0, followed by 90 mg subcutaneously at week 8, then every 8–12 weeks (Lange).
- Ulcerative Colitis:
- Similar induction and maintenance regimen as Crohn’s disease (BNF).
Administration:
- Subcutaneous injections should be rotated between the thighs, abdomen, or upper arms.
- Intravenous infusions require clinical supervision (Lippincott).
- Common: Upper respiratory infections, headache, fatigue, and injection-site reactions (Lippincott).
- Serious:
- Infections: Increased risk of bacterial, viral (e.g., herpes zoster), and fungal infections (Lange).
- Malignancies: Potential risk of skin and other cancers (BNF).
- Hypersensitivity Reactions: Rare cases of anaphylaxis or serum sickness-like reactions (Lippincott).
- Active Infections: Avoid use in patients with active TB, sepsis, or opportunistic infections. Screen for TB and hepatitis B before initiation (BNF).
- Pregnancy/Lactation: Use only if benefits outweigh risks; limited human data available (Lippincott).
- Live Vaccines: Contraindicated during treatment due to immunosuppression (Lange).
- Heart Failure: Monitor patients with pre-existing cardiac conditions (BNF).
- Immunosuppressants (e.g., corticosteroids, methotrexate): Increased risk of infections (Lippincott).
- Live Vaccines (e.g., MMR, yellow fever): Avoid concurrent use; administer vaccines ≥4 weeks before starting ustekinumab (Lange).
- CYP450 Substrates: Ustekinumab may affect drugs metabolized by cytochrome P450 enzymes in chronic inflammation states (BNF).
Ustekinumab is the generic name for this medication. It is marketed under the brand name Stelara®. Biosimilar versions are under development but not yet widely available as of 2023.
