relatlimab (Pending FDA Approval)

Action and Spectrum

Actions and spectrum: 

relatlimab is a monoclonal antibody that targets the protein LAG-3 (lymphocyte activation gene 3). It acts as an immune checkpoint inhibitor, blocking the interaction between LAG-3 and its ligands. By doing so, it enhances the activation and function of T cells, leading to enhanced anti-tumor immune responses. 

The spectrum of relatlimab’s action is primarily focused on cancer immunotherapy. It is being investigated for the use in treatment of various types of cancers like melanoma, lung cancer, and other solid tumors. It is used in combination with immune checkpoint inhibitors or targeted therapies to improve the efficacy of cancer treatment and enhance the anti-tumor immune response. 

Drug Interaction

Adverse Reaction

none

Black Box Warning

Black Box Warning: 

there are no black box warnings specifically associated with relatlimab 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Known hypersensitivity: relatlimab is contraindicated in individuals with hypersensitivity or severe allergic reaction to relatlimab or any of its components. 
• Severe immune-mediated adverse reactions: relatlimab should not be used in patients with severe immune-mediated adverse reactions requiring immunosuppressive treatment or who have experienced a severe or life-threatening immune-mediated adverse reaction with any other antibody therapy. 
• Combined use with ipilimumab: relatlimab is contraindicated in combination with ipilimumab due to an increased risk of severe and potentially fatal immune-mediated adverse reactions.

Caution: 

• Immune-related adverse reactions: relatlimab can cause immune-related adverse reactions, which may be severe or life-threatening.  
• Infusion-related reactions: Infusion-related reactions, including fever, chills, rash, and hypotension, have been reported with relatlimab.  
• Immunosuppression: relatlimab may lead to immunosuppression, increasing the risk of infections.  
• Gastrointestinal perforation: relatlimab has been associated with gastrointestinal perforation.  
• Hepatotoxicity: relatlimab can cause hepatotoxicity, including elevated liver enzymes and hepatocellular injury.  
• Endocrine dysfunction: relatlimab may cause endocrine dysfunction, including hypophysitis, adrenal insufficiency, and thyroid disorders.  
• Fertility: The effects of relatlimab on fertility are unknown. Patients should be advised to discuss fertility preservation options before starting treatment.

Comorbidities: 

There are no specific comorbidities associated with relatlimab 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A  

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: 

relatlimab is a monoclonal antibody that targets and binds to the protein called LAG-3 (lymphocyte activation gene-3). LAG-3 is expressed on the surface of certain immune cells, including T cells, and plays a role in regulating immune responses. By binding to LAG-3, relatlimab blocks its interaction with MHC class II molecules on the antigen-presenting cells, which helps to enhance the activity of T cells and promote an anti-tumor immune response. 

The pharmacology of relatlimab involves its ability to modulate the immune system and promote T cell-mediated immune responses against cancer cells. It can potentially enhance the immune recognition and elimination of tumor cells. relatlimab is being investigated for its therapeutic potential in various cancers, including melanoma, and is typically used in combination with other anti-cancer therapies.  

Pharmacodynamics: 

The pharmacodynamics of relatlimab involves its interaction with the immune system, specifically targeting the LAG-3 protein. By binding to LAG-3, relatlimab blocks its interaction with MHC class II molecules of antigen-presenting cells. This blockade helps to prevent the inhibition of T cell activity and promotes an enhanced anti-tumor immune response. 

The binding of relatlimab to LAG-3 on T cells may lead to several pharmacodynamic effects, including increased T cell activation, proliferation, and cytokine production. These effects can contribute to the recognition & elimination of tumor cells by the immune system.  

Pharmacokinetics: 

Absorption 

relatlimab is administered intravenously, which allows for rapid and complete absorption into the systemic circulation. 

Distribution 

After absorption, relatlimab is distributed throughout the body via the bloodstream. It may distribute into various tissues and organs, including tumor sites, where it exerts its therapeutic effects. 

Metabolism 

relatlimab is a monoclonal antibody, and as such, it is primarily metabolized by enzymatic degradation in cells and tissues of the body. Specific details about the metabolism of relatlimab are not readily available. 

Elimination and excretion 

The elimination of relatlimab from the body occurs through several routes. It can be excreted unchanged or undergo metabolic breakdown to smaller peptides and amino acids, which are eliminated via urine or feces. The exact excretion pathways and elimination half-life of relatlimab are still being investigated. 

Adminstartion

Administration: 

relatlimab is administered intravenously (IV) by a healthcare professional. The medication is typically given as an infusion over a specific time period, can range from several minutes to hours. The exact dosage, infusion rate, and treatment schedule will depend on the specific indication and individual patient factors. 

Before starting relatlimab treatment, premedication with corticosteroids, antipyretics, and antihistamines may be given to help manage potential infusion-related reactions. The healthcare provider will closely monitor the patient during and after the infusion for any adverse reactions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: relatlimab 

Pronounced: (reh-LAT-li-mab)  

Why do we use relatlimab? 

relatlimab is a monoclonal antibody used for the treatment of certain types of cancer. It is used to treat metastatic or unresectable melanoma. relatlimab is used in combination with nivolumab, another immune checkpoint inhibitor, for this indication. 

The combination of relatlimab and nivolumab works by targeting and blocking the PD-1 (programmed cell death protein 1) pathway, which helps the immune system recognize and attack cancer cells.