Cemiplimab-rwlc

Uses

Cemiplimab-rwlc is a programmed death receptor-1 blocking antibody used to treat metastatic cutaneous squamous cell carcinoma.

This drug is a programmed death receptor-1 (PD-1) blocking antibody indicated for the treatment of patients with metastatic cutaneous squamous cell carcinoma (CSCC) or locally advanced CSCC who are not candidates for curative surgery or curative radiation .

Cemiplimab-rwlc is also used to associated treatment for these conditions: Metastatic cutaneous squamous cell carcinoma, Locally advanced cutaneous squamous cell carcinoma, and not a candidate for curative surgery or curative radiation

How Cemiplimab-rwlc works

Binding of the programmed death receptor (PD) ligands PD-L1 and PD-L2, to the PD-1 receptor, which is found on T cells, inhibits T-cell proliferation and cytokine production. The upregulation of PD-1 ligands occurs in some tumors and signaling through this pathway may contribute to the inhibition of active T-cell immune surveillance of tumors. Cemiplimab-rwlc is a recombinant human immunoglobulin G4 (IgG4) monoclonal antibody that binds to the PD-1 receptor and blocks its interaction with PD-L1 and PD-L2 ligands, causing PD-1 pathway-mediated inhibition of the immune response, including the anti-tumor immune response. In mouse tumor models, blocking PD-1 activity resulted in decreased rates of tumor growth .

Toxicity

The most common adverse reactions (incidence ≥ 20%) were fatigue, rash, and diarrhea in clinical studies . Severe and fatal immune-mediated adverse reactions may occur in any organ system or tissue, including the following: immune-mediated pneumonitis, immune-mediated colitis, immune-mediated hepatitis, immune-mediated endocrinopathies, immune-mediated dermatologic adverse reactions, and immune-mediated nephritis and renal dysfunction. Monitor for symptoms and signs of immune-mediated adverse reactions. Regularly perform chemistry panels, including liver and thyroid function, at baseline and periodically during treatment. Withhold or permanently discontinue this drug and administer corticosteroids based on the severity of the reaction. Infusion-related reactions may also occur. Interrupt, decrease the rate of infusion or permanently discontinue based on the severity of the reaction.

A note on fetal toxicity: This drug can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and use of effective contraception .

Cemiplimab-rwlc Disease Interaction

Moderate: hepatic impairment, nephritis/renal dysfunction

Volume of Distribution

The volume of distribution of cemiplimab at steady state is 5.3 L (25%) .

Elimination Route

After a dose of 350 mg cemiplimab administered intravenously every 3 weeks, median steady-state concentrations (CV%) of cemiplimab ranged between a maximum concentration (Cmax,ss) of 166 mcg/mL (28%) and a minimum concentration (Cmin,ss) of 59 mcg/mL (48%). Steady-state exposure was achieved after approximately 4 months .

Half Life

The elimination half-life (CV%) at steady state is 19 days (30%) .

Clearance

Cemiplimab-rwlc clearance (CV%) after the first dose is 0.32 L/day (39%) and decreases over time by 34%, resulting in a steady-state clearance (CLss) (CV%) of 0.21 L/day (39%) .

Innovators Monograph

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