Action and Spectrum

Actions and Spectrum:  

rilonacept is a recombinant fusion protein that acts as a soluble receptor, binding to and neutralizing the pro-inflammatory cytokines interleukin-1 alpha (IL-1α) and interleukin-1 beta (IL-1β). This results in the prevention of their interaction with cell surface receptors, ultimately reducing the pro-inflammatory effects of these cytokines. 

Regarding its spectrum, rilonacept has been shown to effectively reduce systemic inflammation in patients with various inflammatory disorders, including cryopyrin-associated periodic syndromes (CAPS) and familial Mediterranean fever (FMF). Additionally, rilonacept has demonstrated efficacy in the treatment of gout, as it reduces the frequency of gout flares in patients with a history of these painful and debilitating events 

Drug Interaction

Adverse Reaction

Black Box Warning

Black Box Warning:  

Patients treated with Rilonacept are at increased risk for serious infections, including bacterial, viral, and fungal infections. These infections can be life-threatening and may require hospitalization. Rilonacept should be discontinued in patients who develop a serious infection. 

Contraindication / Caution

Contraindication/Caution:  

rilonacept is contraindicated in patients who have a known hypersensitivity to the medication or any of its components. Hypersensitivity reactions can range from mild to severe, and may include symptoms such as rash, itching, swelling, and difficulty breathing. Patients who experience any of these symptoms should seek immediate medical attention. 

rilonacept is also contraindicated in patients with active infections, as the medication may interfere with the body’s ability to fight off the infection. Patients should inform their healthcare provider have a history of recurrent infections or if they are currently experiencing symptoms of an infection, such as fever, chills, or cough. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category  

Pharmacology

Pharmacology: 

rilonacept is a prescription medication that belongs to a class of drugs known as biologic response modifiers. It is a recombinant fusion protein composed of two soluble interleukin-1 receptor components and human immunoglobulin G1 (IgG1) Fc portion. The drug acts as a competitive inhibitor of interleukin-1 (IL-1), which is a pro-inflammatory cytokine that plays a critical role in the pathogenesis of various inflammatory diseases. 

Pharmacodynamics: 

rilonacept is a recombinant fusion protein that binds to and neutralizes the activity of interleukin-1 (IL-1), a pro-inflammatory cytokine that plays a key role in the body’s immune and inflammatory responses. IL-1 is produced by a variety of cells in response to infection, injury, or other stimuli, and binds to the IL-1 receptor on target cells to initiate a cascade of downstream signaling events. 

MOA:  

rilonacept is a recombinant fusion protein that works by blocking the activity of interleukin-1 (IL-1), a pro-inflammatory cytokine that is involved in the body’s immune and inflammatory responses. IL-1 is produced by a variety of cells in response to infection, injury, or other stimuli, and binds to the IL-1 receptor on target cells to initiate a cascade of downstream signaling events. 

Pharmacokinetics: 

Absorption 

rilonacept is administered by subcutaneous injection and is rapidly absorbed into the bloodstream, with a bioavailability of approximately 81%. 

Distribution 

The drug is distributed throughout the body, including into the synovial fluid of joints. The volume of distribution of rilonacept is estimated to be approximately 8.5 L. 

Metabolism 

rilonacept is metabolized by proteolysis, primarily within the liver. The drug undergoes enzymatic degradation into smaller peptides and amino acids. 

 Excretion and Elimination 

 rilonacept is eliminated from the body via renal and non-renal routes. The drug is primarily excreted in the urine, with a half-life of approximately 6 days. 

Adminstartion

Administration:  

rilonacept is a prescription medication that is administered by subcutaneous injection. Patients or their caregivers can be trained by a healthcare provider to administer the injections at home, after which the patient should be monitored for any adverse reactions. 

The recommended dosage of rilonacept is 160 mg administered once weekly. The medication is supplied in a prefilled syringe or autoinjector, and should be injected subcutaneously into the thigh, abdomen, or upper arm. The injection site should be rotated with each injection to avoid tissue damage or irritation. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: rilonacept 

Why do we use rilonacept ?  

rilonacept is a prescription medication used to treat certain autoinflammatory diseases, including cryopyrin-associated periodic syndromes (CAPS) such as Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS). 

CAPS are a group of rare genetic disorders that are characterized by recurrent episodes of inflammation, which can lead to a range of symptoms such as fever, rash, joint pain, and fatigue. rilonacept works by blocking the activity of interleukin-1 (IL-1), a protein that is involved in the body’s inflammatory response. By reducing the levels of IL-1 in the body, rilonacept can help to prevent or reduce the frequency and severity of CAPS flare-ups.