What are B cell targeted therapies? RTX (Rituxan): chimeric mouse–human IgG1κ monoclonal antibody directed against extracellular domain of CD20 antigen on B cells. B cells are eliminated by complement-mediated lysis, antibody-dependent cell-mediated cytotoxicity, or apoptosis. All peripheral B cells are eliminated within days. Patients who fail to deplete their B cells respond less well. Notably, Ig …
What bDMARDs are available to inhibit IL 17 in the rheumatic diseases? Secukinumab (Cosentyx) is a human IgG1κ monoclonal antibody which blocks IL-17A. It is FDA-approved to treat psoriasis, PsA, and AS. Not effective for RA. • Available formulations: 150 mg/mL solution in a single-use Sensoready pen or prefilled syringe that is self-administered. There is also a …
What is ustekinumab and why is it effective in PsA? Ustekinumab (Stelara) is a human IgG1κ monoclonal antibody that binds to the p40 subunit of both IL-12 and IL-23 preventing their binding to their shared cell surface receptor chain, IL-12β. The inhibition of IL-12 signaling abrogates Th1 response with reduction in TNF-α, IFN-γ, and IL-2 production. …
What biologics can inhibit IL 5? What are its uses and toxicities? Mepolizumab (Nucala) is a humanized IgG1κ monoclonal antibody that binds to IL-5. This antibody inhibits IL-5 which profoundly affects the activation and survival of eosinophils. Half-life with subcutaneous administration is 16 to 22 days. • Available formulations: 100 mg of lyophilized powder in single-dose vial …
What biologics can inhibit IL 6? What are its uses and toxicities? Tocilizumab (Actemra) is a humanized IgG1κ monoclonal antibody that binds to the soluble and membrane-bound forms of the IL-6 receptor (IL-6R). This antibody inhibits IL-6 signaling of cells that constitutively express IL-6R as well as cells that bind the soluble form of IL-6R that …
How are IL 1 inhibitors supplied and used? What are their indications and toxicities? • Anakinra (Kineret). Available formulation: single-use vial of 100 mg. Dosage: adults 100 mg SC daily; children 1 to 2 mg/kg (up to 8 mg/kg) daily. Follow-up: CBC monthly for 3 months, then every 3 months. Adverse reactions: serious infections (2%), neutropenia …
What biologics are currently available to inhibit TNF α? ETN (Enbrel): a bioengineered molecule derived from Chinese hamster ovary cells, which consist of a fusion protein created by linking the extracellular binding regions from two TNF-RII (p75) receptors to the Fc portion of human immunoglobulin G1 (IgG1). This molecule is a dimeric soluble TNF receptor that …
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