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General Description:

Relatlimab, identified by CAS number 1673516-98-7, is a notable compound with significant therapeutic applications. Relatlimab is a human IgG4 monoclonal antibody and novel immune checkpoint inhibitor that targets lymphocyte activation gene-3 (LAG-3). It was the first commercially developed anti-LAG-3 antibody, entering clinical trials in 2013, and has garnered interest in the treatment of a variety of cancers, including leukemia and melanoma. As immune checkpoint inhibitors have limited efficacy when used alone, drugs like relatlimab have been trialed in combination with other checkpoint inhibitors - for example, PD-1 inhibitors like or CTLA-4 inhibitors like - to enhance their efficacy. Relatlimab received FDA approval in March 2022, alongside the PD-1 inhibitor in the combination product Opdualag (Bristol-Myers Squibb), for the treatment of unresectable or metastatic melanoma. It was the first anti-LAG-3 antibody demonstrate benefit in a Phase 3 study, as well as the first to receive FDA approval.

Indications:

This drug is primarily indicated for: Relatlimab is indicated in combination with , in the combination product Opdualag, for the treatment of adult and pediatric patients ≥12 years old with unresectable or metastatic melanoma. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Relatlimab undergoes metabolic processing primarily in: As with other therapeutic proteins, the metabolism of relatlimab likely occurs via non-specific catabolism to smaller peptides and amino acids. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Relatlimab are crucial for its therapeutic efficacy: Following once-monthly administration alongside , steady-state concentrations of relatlimab were reached after 16 weeks. At the recommended dosage, the C_max and C_avg of relatlimab at steady-state were 62.2 µg/mL and 28.8 µg/mL, respectively. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Relatlimab is an important consideration for its dosing schedule: The geometric mean effective half-life of relatlimab, when administered alongside nivolumab, is 26.2 days. This determines the duration of action and helps in formulating effective dosing regimens.

Volume of Distribution:

Relatlimab is distributed throughout the body with a volume of distribution of: The geometric mean volume of distribution of relatlimab at steady-state is 6.6 liters. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Relatlimab is a critical factor in determining its safe and effective dosage: At steady-state, the geometric mean clearance of relatlimab is 5.5 mL/h. Clearance at steady-state appears to be approximately 10% lower than after the first dose. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Relatlimab exerts its therapeutic effects through: Relatlimab is administered with nivolumab at 4-week intervals via a 30-minute infusion. Infusion-related reactions are uncommon but can be severe - infusion may be interrupted or slowed in patients with mild-to-moderate reactions, but should be discontinued in patients experiencing severe reactions. The combination of relatlimab and nivolumab can cause severe and fatal immune-mediated adverse reactions, including pneumonitis, colitis, hepatitis, myocarditis, and hypophysitis. The early identification and management of immune-mediated adverse reactions is essential for the safe use of this therapy. Additionally, the combination of relatlimab and nivolumab is likely to cause fetal harm when administered to pregnant patients. Females of reproductive potential should be advised to use effective contraception throughout treatment and for at least 5 months following the last dose. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Relatlimab functions by: Lymphocyte-activation gene 3 (LAG-3) - also known as CD223 - is a type I transmembrane protein belonging to the immunoglobulin superfamily. Its expression on activated T-cells is induced following antigen stimulation, and they serve a number of functions including the inhibition of Th1 cell proliferation and the reduction of cytokine production - such as IL-2, IFNγ, and TNF - in these activated T-cells. Ligands of LAG-3 include antigen-presenting cells such as MHC class II molecules and liver sinusoidal endothelial cell lectin (LSECtin), the latter of which has been shown to promote tumor progression when expressed on melanoma cells by inhibiting anti-tumor T-cell responses. As LAG-3 expression is tied to antigen presentation, continuous antigen exposure owing to chronic infection or tumor-associated antigens can lead to high and sustained expression of LAG-3 on T-cells, which eventually lose their effector functions by becoming functionally "exhausted". This loss of T-cell function leads to lessened immunosurveillance and promotes tumor escape. Relatlimab is a human IgG4 monoclonal antibody that binds LAG-3 and inhibits its signaling pathway, the antagonism of which promotes T-cell proliferation, cytokine secretion, and, subsequently, restored tumor immunosurveillance. Used in combination with , a PD-1 receptor blocker, relatlimab has been shown to potentiate the anti-tumor effects of PD-1 blockade. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Relatlimab belongs to the None, classified under the direct parent group Peptides. This compound is a part of the Organic Compounds, falling under the Organic Acids superclass, and categorized within the Carboxylic Acids and Derivatives class, specifically within the Amino Acids, Peptides, and Analogues subclass.

Experimental Properties:

Further physical and chemical characteristics of Relatlimab include:

• Molecular Weight: 148000.0
• Molecular Formula: C6472H9940O2026N1704S38