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| Primary information |
|---|
| ID | 15562 |
| Therapeutic ID | Th1608 |
| Protein Name | Cemiplimab |
| Sequence | >Th1608_Cemiplimab
EVQLLESGGVLVQPGGSLRLSCAASGFTFSNFGMTWVRQAPGKGLEWVSGISGGGRDTYFADSVKGRFTISRDNSKNTLYLQMNSLKGEDTAVYYCVKWGNIYFDYWGQGTLVTVSSASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVFSCSVMHEALHNHYTQKSLSLSLGK
|
| Molecular Weight | 146000 |
| Chemical Formula | NA |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | The elimination half-life (CV%) at steady state is 19 days (30%) [FDA label]. |
| Description | The U.S. Food and Drug Administration (FDA) approved Cemiplimab (_Libtayo_), manufactured by Regeneron Pharmaceuticals, on September 28, 2018. This is the first FDA approval of a drug specifically for the treatment of advanced cutaneous squamous cell carcinoma (CSCC) [A39201, L4615]. |
| Indication/Disease | 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 [FDA label, A39201]. |
| Pharmacodynamics | Cemiplimab inhibits tumor growth by an immune-mediated mechanism, specifically by the inhibition of the programmed death receptor 1 (PD-1), treating cutaneous squamous cell carcinoma [FDA label], [A39201], [A39204]. |
| Mechanism of Action | 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 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 [FDA label]. |
| Toxicity | The most common adverse reactions (incidence = 20%) were fatigue, rash, and diarrhea in clinical studies [FDA label]. 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 [FDA label]. |
| Metabolism | NA |
| Absorption | 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 [FDA label]. |
| The volume of distribution of cemiplimab at steady state is 5.3 L (25%) [FDA label]. |
| Clearance | Cemiplimab 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%) [FDA label]. |
| Categories | Antineoplastic Agents |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Programmed cell death protein 1 |
| Brand Name | Libtayo |
| Company | Regeneron Pharmaceuticals, Inc. |
| Brand Description | Regeneron Pharmaceuticals, Inc. |
| Prescribed For | Intravenous |
| Chemical Name | 50 mg/1mL |
| Formulation | None. |
| Physical Appearance | fatigue, rash, diarrhea, itching, nausea, constipation, fatigue, musculoskeletal pain, and decreased appetite |
| Route of Administration | Libtayo is a medicine used to treat skin cancer by working with your immune system. Libtayo is used to treat a certain type of skin cancer called cutaneous squamous cell carcinoma (CSCC) that has spread to other parts of the body or cannot be treated with radiation or surgery. Libtayo is used to treat... |
| Recommended Dosage | LIBTAYO is indicated for the treatment of patients with metastatic cutaneous squamous cell carcinoma (mCSCC) or locally advanced CSCC (laCSCC) who are not candidates for curative surgery or curative radiation. |
| Contraindication | NA |
| Side Effects | Cemiplimab-rwlc is a human programmed death receptor-1 (PD-1) blocking antibody. Cemiplimab-rwlc is a recombinant human IgG4 monoclonal antibody that binds to PD-1 and blocks its interaction with PD-L1 and PD-L2. Cemiplimab-rwlc is produced by recombinant DNA technology in Chinese hamster ovary (CHO) cell suspension culture. Cemiplimab-rwlc has an approximate molecular weight of 146 kDa. |
| Useful Link 1 | Link |
| Useful Link 2 | Link |
| Remarks | NA |