rozanolixizumab

Action and Spectrum

Actions and Spectrum: 

rozanolixizumab is a monoclonal antibody that targets and inhibits the neonatal Fc receptor (FcRn) activity.  

Action:  

rozanolixizumab binds to the FcRn receptor, rescuing immunoglobulin G (IgG) antibodies from degradation. By blocking FcRn, rozanolixizumab prevents the recycling of IgG antibodies, leading to increased degradation of IgG. This action results in a reduction of circulating IgG levels in the body. 

Spectrum:  

The spectrum of rozanolixizumab’s action includes various conditions associated with elevated IgG antibody levels. It has primarily been studied and developed for treating autoimmune diseases, especially those mediated by pathogenic IgG antibodies. Some examples of conditions in which rozanolixizumab has been investigated include: 

• Myasthenia Gravis (MG): rozanolixizumab has shown promising results in reducing IgG levels and improving symptoms in patients with generalized MG who have not responded well to conventional treatments. 
• Immune Thrombocytopenia (ITP): ITP is a condition characterized by low platelet counts due to increased destruction by the immune system. rozanolixizumab has demonstrated efficacy in increasing platelet counts and reducing bleeding symptoms in patients with ITP. 
• Chronic Inflammatory Demyelinating Polyneuropathy (CIDP): CIDP is a chronic autoimmune disorder affecting the peripheral nerves. rozanolixizumab has shown potential in reducing IgG levels and improving neurological function in patients with CIDP. 
• Guillain-Barré Syndrome (GBS): GBS is an acute autoimmune disorder affecting the peripheral nerves. Studies have explored using rozanolixizumab as a potential treatment option for GBS. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Diarrhea (20%) 

URT infection (8-17%) 

Headache (44%) 

Hypersensitivity reactions (11%) 

Pyrexia (17%) 

Any infection (23%) 

1-10% 

Herpes simplex infection (6%) 

Serious infections (4%) 

Arthralgia (7%) 

Urinary tract infections (9%) 

Abdominal pain (8%) 

Arthralgia (7%) 

Nausea (10%) 

Urinary tract infections (9%) 

Herpes simplex infection (6%) 

Abdominal pain (8%) 

Serious infections (4%) 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: Individuals with known hypersensitivity or severe allergic reaction to rozanolixizumab or its components should not receive the medication. 
• Active Infections: A person with an active and severe infection may be a contraindication to initiating rozanolixizumab treatment. This is because monoclonal antibodies can suppress the immune response and potentially exacerbate the infection. 
• Pregnancy and Breastfeeding: Using rozanolixizumab during pregnancy or breastfeeding may have potential risks to the fetus or the nursing infant. Therefore, it is typically not recommended unless the potential benefits outweigh the potential risks. It is essential to discuss this with a healthcare professional. 
• Other Medical Conditions: Certain medical conditions or comorbidities may require caution or careful evaluation before initiating treatment with rozanolixizumab. These could include individuals with a history of immunosuppression, active malignancy, or severe cardiovascular or pulmonary diseases. Close monitoring and individual assessment are necessary in such cases. 

Caution 

• Infections: Monoclonal antibody therapies, including rozanolixizumab, can affect the immune response and may increase the risk of infections. It is crucial to consider the patient’s overall infection risk and monitor for signs of infection during treatment. Pre-existing infections should ideally be resolved before initiating rozanolixizumab therapy. 
• Immunization: Live vaccines should generally be avoided while receiving monoclonal antibody treatment due to the potential for reduced vaccine efficacy. Consult with a healthcare professional regarding appropriate immunization schedules and the timing of vaccinations. 
• Hypersensitivity Reactions: While uncommon, hypersensitivity reactions may occur with monoclonal antibody therapies. Appropriate medical support and management should be readily available. 
• Pregnancy and Breastfeeding: Using rozanolixizumab during pregnancy or breastfeeding may have potential risks to the fetus or the nursing infant. The decision to use rozanolixizumab should be carefully evaluated, considering the potential benefits and risks, and discussed with a healthcare professional. 
• Other Medical Conditions: Patients with pre-existing medical conditions, such as immunodeficiency or a history of malignancy, may require careful consideration and individual assessment before initiating rozanolixizumab treatment. Close monitoring and appropriate medical management should be provided. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• 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: 

rozanolixizumab is a monoclonal antibody that selectively binds to the neonatal Fc receptor (FcRn) and inhibits its activity. FcRn plays a crucial role in rescuing immunoglobulin G (IgG) antibodies from degradation, thereby extending their half-life in circulation. By binding to FcRn, rozanolixizumab blocks the recycling process, leading to increased degradation of IgG antibodies.

This mechanism reduces circulating IgG levels, which is beneficial in autoimmune disorders characterized by elevated pathogenic IgG antibodies. By modulating IgG levels, rozanolixizumab aims to alleviate the disease manifestations associated with excessive IgG-mediated immune responses. 

Pharmacodynamics: 

Mechanism of action: rozanolixizumab is a monoclonal antibody that works through a specific mechanism of action. Its primary target is the neonatal Fc receptor (FcRn), crucial in rescuing immunoglobulin G (IgG) antibodies from degradation and extending their half-life in circulation.  

• Binding to FcRn: rozanolixizumab selectively binds to the FcRn receptor, expressed on the surface of cells in various tissues, including endothelial cells. This binding is specific to the Fc region of IgG antibodies. 
• Blocking Recycling: By binding to FcRn, rozanolixizumab interferes with the interaction between FcRn and IgG antibodies. FcRn is responsible for recycling IgG antibodies, preventing lysosome degradation, and extending their lifespan in circulation. rozanolixizumab inhibits this recycling process, increasing IgG antibody lysosomal degradation. 
• Reduction of Circulating IgG: As a consequence of blocking FcRn-mediated recycling, rozanolixizumab leads to a reduction in the levels of circulating IgG antibodies. This reduction benefits autoimmune diseases where pathogenic IgG antibodies contribute to disease pathology. 

By modulating IgG levels, rozanolixizumab aims to decrease the burden of pathogenic IgG antibodies and potentially alleviate the symptoms and disease activity associated with certain autoimmune disorders. 

Pharmacokinetics: 

Absorption 

Monoclonal antibodies like rozanolixizumab are typically administered via intravenous infusion, resulting in immediate and complete bioavailability. 

Distribution 

Once in the bloodstream, rozanolixizumab is expected to distribute throughout the body, including extravascular tissues. The distribution may follow the general pattern observed for monoclonal antibodies, with limited penetration into specific tissues, such as the central nervous system. 

Metabolism 

Monoclonal antibodies are primarily eliminated intact and are not significantly metabolized by metabolic enzymes in the body. Metabolic processes are typically not a significant route of elimination for monoclonal antibodies like rozanolixizumab. 

Elimination and Excretion 

The primary route of elimination for monoclonal antibodies is through the reticuloendothelial system, mainly via catabolism and subsequent clearance by the liver and spleen. Some elimination may also occur through renal excretion, but it is usually a minor pathway. 

Adminstartion

Administration: 

Subcutaneous administration 

• Route of Administration: Monoclonal antibodies are typically administered via subcutaneous/intravenous infusion. 
• Healthcare Setting: The administration of rozanolixizumab is usually performed in a healthcare setting, such as a hospital, clinic, or infusion center, under the supervision of healthcare professionals experienced in delivering SC medications. 
• Dosing Schedule: The dosing schedule for rozanolixizumab may vary depending on the treated condition and individual patient factors. It is essential to follow the prescribed dosing regimen the healthcare professional provides. 
• Pre-Medication: Some patients may require pre-medication to help manage the potential risk of infusion-related reactions or hypersensitivity. These pre-medications, if necessary, will be determined by the healthcare professional and administered before the infusion of rozanolixizumab. 
• During medication administration, patients are monitored for signs of hypersensitivity or other adverse events. Vital signs, such as blood pressure and heart rate, may be monitored regularly. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: rozanolixizumab 

Why do we use rozanolixizumab? 

rozanolixizumab is a monoclonal antibody primarily investigated for treating certain autoimmune disorders. While the specific approved uses of rozanolixizumab may vary by country, here are some potential uses based on clinical trials and ongoing research: 

• Myasthenia Gravis (MG): rozanolixizumab has shown promising results in clinical trials to treat generalized MG. It may be considered a therapeutic option for patients with MG who have not responded well to conventional treatments or require additional immunosuppressive therapy. 
• Immune Thrombocytopenia (ITP): ITP is a condition characterized by low platelet counts due to increased destruction by the immune system. Clinical studies have evaluated the use of rozanolixizumab in ITP patients who have not responded to or have relapsed after initial treatments. It has demonstrated efficacy in increasing platelet counts and reducing bleeding symptoms. 
• Chronic Inflammatory Demyelinating Polyneuropathy (CIDP): CIDP is a chronic autoimmune disorder affecting the peripheral nerves. rozanolixizumab has been studied as a potential treatment option for CIDP, and preliminary results have shown improvements in neurological function and a reduction in IgG levels. 
• Guillain-Barré Syndrome (GBS): GBS is an acute autoimmune disorder affecting the peripheral nerves. Research is being conducted to explore the use of rozanolixizumab as a potential treatment for GBS, although further studies are needed to establish its efficacy and safety in this condition.