Ensituximab
| Ensituximab | |
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| INN | |
| Drug class | |
| Routes of administration | Intravenous |
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| Bioavailability | |
| Metabolism | |
| Elimination half-life | |
| Excretion | |
| Legal status | Investigational |
| CAS Number | |
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| DrugBank | |
| ChemSpider | |
| KEGG | |
Ensituximab is an experimental monoclonal antibody designed for the treatment of cancer. It specifically targets the epidermal growth factor receptor (EGFR), which is often overexpressed in various types of cancer cells, including colorectal cancer and head and neck cancer. Ensituximab works by binding to the EGFR, thereby inhibiting the receptor's function and preventing the cancer cells from growing and proliferating.
Mechanism of Action
Ensituximab is a chimeric (mouse/human) monoclonal antibody. It binds to the extracellular domain of the EGFR with high affinity. By binding to EGFR, ensituximab blocks the receptor's ability to activate its downstream signaling pathways, which are crucial for cell growth and survival. This inhibition can lead to apoptosis (programmed cell death) and reduced tumor growth.
Clinical Trials
Ensituximab has been evaluated in several clinical trials, primarily focusing on its efficacy and safety in patients with advanced colorectal cancer. These studies have explored its use both as a single agent and in combination with other chemotherapeutic agents. The results from these trials have provided important insights into the potential therapeutic benefits and limitations of ensituximab in treating cancer.
Side Effects
Like other EGFR inhibitors, ensituximab can cause side effects, some of which can be severe. Common side effects include skin rash, diarrhea, and an increased risk of infections. Severe side effects may include pulmonary toxicity and infusion-related reactions. Patients receiving ensituximab are closely monitored for these adverse effects during treatment.
Development and Regulatory Status
As of the last update, ensituximab remains an investigational drug and has not yet received approval from regulatory bodies such as the Food and Drug Administration (FDA) in the United States. Its development is ongoing, with additional studies needed to further define its safety profile and efficacy in different cancer populations.
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Contributors: Prab R. Tumpati, MD