Pembrolizumab

Pembrolizumab is a humanized monoclonal antibody that interacts with the programmed cell death receptor 1 (PD-1), an immune checkpoint, leading to increased immune reactivity and the potential to disrupt immune tolerance. This property is leveraged in the immunotherapy of cancer.

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Pharmacological Profile

Pembrolizumab (pem" broe liz' ue mab) is a recombinant monoclonal IgG4 kappa-isotype antibody that targets the programmed cell death receptor-1 (PD-1), which plays a crucial role in modulating and suppressing T cell responses. By inhibiting PD-1 receptors on activated T cells, Pembrolizumab prevents these cells from binding to the PD ligand, a binding event that typically terminates T cell activation and proliferation. The absence of PD-1 receptor engagement allows T cell responses to remain activated, enhancing cytotoxic reactivity. This potentiated immune response can disrupt immunological tolerance to cancer cell neo-antigens, making pembrolizumab a valuable tool in cancer immunotherapy.

Clinical Efficacy

In several multicenter studies, pembrolizumab therapy has demonstrated the ability to extend survival rates in patients with advanced, metastatic, or unresectable malignant melanoma. A proportion of these patients even achieved long-term remission.

Approval and Usage

The United States Food and Drug Administration (FDA) approved Pembrolizumab for use in advanced melanoma in 2014 and for advanced non-small cell lung cancer (NSCLC) in 2015. It is also actively being investigated for potential use in various other cancers, including breast and renal cancer and lymphomas.

Safety Profile

Though pembrolizumab has significant therapeutic potential, it also has an extensive range of adverse events, including serious immune-related conditions such as acute hepatitis and acute liver injury, which can be life-threatening.

Adverse Effects

Common side effects of Pembrolizumab, often immune-related due to immune enhancement, include enterocolitis, dermatitis, endocrinopathy, pneumonitis, neuropathy, nephritis, and hepatitis. Though most of these reactions respond to immunosuppressive therapy, some have resulted in fatalities and others have necessitated long-term therapy. Therefore, early detection and prompt management of these side effects are critical when using checkpoint inhibitors like Pembrolizumab.

• Dailymed label info on Pembrolizumab
• FDA Pembrolizumab

Pembrolizumab Resources
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