Etanercept (1 brand name, 2 dosage forms, 1 route)
Available dosage forms: SYRINGE, VIAL.
Routes of administration: SUBCUTANEOUS.
Brand Names
- ENBREL
Contraindications
Enbrel is contraindicated in patients with sepsis.
Adverse Reactions
The following serious adverse reactions are discussed in greater detail in other sections of the labeling: Serious Infections [see Warnings and Precautions (5.1)] Neurologic Reactions [see Warnings and Precautions (5.2)] Malignancies [see Warnings and Precautions (5.3)] Patients with Heart Failure [see Warnings and Precautions (5.4)] Hematologic Reactions [see Warnings and Precautions (5.5)] Hepatitis B Reactivation [see Warnings and Precautions (5.6)] Allergic Reactions [see Warnings and Precautions (5.7)] Autoimmunity [see Warnings and Precautions (5.9)] Immunosuppression [see Warnings and Precautions (5.10)]
Drug Interactions
Specific drug interaction studies have not been conducted with Enbrel.
Mechanism of Action
TNF is a naturally occurring cytokine that is involved in normal inflammatory and immune responses. It plays an important role in the inflammatory processes of RA, polyarticular JIA, PsA, and AS and the resulting joint pathology. In addition, TNF plays a role in the inflammatory process of PsO. Elevated levels of TNF are found in involved tissues and fluids of patients with RA, JIA, PsA, AS, and PsO. Two distinct receptors for TNF (TNFRs), a 55 kilodalton protein (p55) and a 75 kilodalton protein (p75), exist naturally as monomeric molecules on cell surfaces and in soluble forms. Biological activity of TNF is dependent upon binding to either cell surface TNFR. Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind TNF molecules. Etanercept inhibits binding of TNF-α and TNF-β (lymphotoxin alpha [LT-α]) to cell surface TNFRs, rendering TNF biologically inactive. In in vitro studies, large complexes of etanercept with TNF-α were not detected and cells expressing transmembrane TNF (that binds Enbrel) are not lysed in the presence or absence of complement.
Overdosage
No dose-limiting toxicities have been observed during clinical trials of Enbrel. Single IV doses up to 60 mg/m2 (approximately twice the recommended dose) have been administered to healthy volunteers in an endotoxemia study without evidence of dose-limiting toxicities.