Identification

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Name
Cemiplimab
Accession Number
DB14707
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
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) 1,4.

Protein chemical formula
Not Available
Protein average weight
146000.0 Da
Sequences
Not Available
Synonyms
  • Cemiplimab-rwlc
External IDs
REGN-2810 / REGN2810
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LibtayoSolution350 mgIntravenousSanofi Aventis2019-05-24Not applicableCanada
LibtayoSolution250 mgIntravenousSanofi Aventis2019-05-24Not applicableCanada
LibtayoInjection50 mg/1mLIntravenousRegeneron Pharmaceuticals, Inc.2018-09-28Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories
UNII
6QVL057INT
CAS number
1801342-60-8

Pharmacology

Indication

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 Label,1.

Associated Conditions
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 Label, 1, 3.

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 Label.

TargetActionsOrganism
AProgrammed cell death protein 1
inhibitor
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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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 Label.

Volume of distribution

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

Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

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

Toxicity

The most common adverse reactions (incidence ≥ 20%) were fatigue, rash, and diarrhea in clinical studies 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 Label.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Cemiplimab.
AbituzumabThe risk or severity of adverse effects can be increased when Abituzumab is combined with Cemiplimab.
AbrilumabThe risk or severity of adverse effects can be increased when Cemiplimab is combined with Abrilumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Cemiplimab.
AdecatumumabThe risk or severity of adverse effects can be increased when Adecatumumab is combined with Cemiplimab.
AducanumabThe risk or severity of adverse effects can be increased when Aducanumab is combined with Cemiplimab.
AfelimomabThe risk or severity of adverse effects can be increased when Afelimomab is combined with Cemiplimab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Cemiplimab.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Cemiplimab.
AmatuximabThe risk or severity of adverse effects can be increased when Amatuximab is combined with Cemiplimab.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
  1. Migden MR, Rischin D, Schmults CD, Guminski A, Hauschild A, Lewis KD, Chung CH, Hernandez-Aya L, Lim AM, Chang ALS, Rabinowits G, Thai AA, Dunn LA, Hughes BGM, Khushalani NI, Modi B, Schadendorf D, Gao B, Seebach F, Li S, Li J, Mathias M, Booth J, Mohan K, Stankevich E, Babiker HM, Brana I, Gil-Martin M, Homsi J, Johnson ML, Moreno V, Niu J, Owonikoko TK, Papadopoulos KP, Yancopoulos GD, Lowy I, Fury MG: PD-1 Blockade with Cemiplimab in Advanced Cutaneous Squamous-Cell Carcinoma. N Engl J Med. 2018 Jul 26;379(4):341-351. doi: 10.1056/NEJMoa1805131. Epub 2018 Jun 4. [PubMed:29863979]
  2. Authors unspecified: Drug and Device News. P T. 2017 Nov;42(11):665-691. [PubMed:29089720]
  3. Sidaway P: Cemiplimab effective in cutaneous SCC. Nat Rev Clin Oncol. 2018 Aug;15(8):472. doi: 10.1038/s41571-018-0056-5. [PubMed:29921845]
  4. FDA Approves Libtayo [Link]
  5. Libtayo, Regeneron [Link]
External Links
Wikipedia
Cemiplimab
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (239 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentAdvanced Malignancies / Cancer, Advanced1
1Active Not RecruitingTreatmentMelanoma1
1Active Not RecruitingTreatmentMetastatic Squamous Cell Carcinoma Neck / Metastatic Squamous Cell Carcinoma of Head / Recurrent Squamous Cell Carcinoma of Head / Recurrent Squamous Cell Carcinoma of Neck1
1RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Malignant Lymphomas1
1RecruitingTreatmentAdvanced Malignancies1
1RecruitingTreatmentCutaneous Squamous Cell Carcinoma1
1RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1RecruitingTreatmentMalignancies1
1RecruitingTreatmentMalignant Solid Tumours1
1RecruitingTreatmentNeoplasms, Metastatic1
1RecruitingTreatmentRenal Cell Adenocarcinoma1
1RecruitingTreatmentStage III Prostate Cancer / Stage IIIA Prostate Cancer / Stage IIIB Prostate Cancer / Stage IIIC Prostate Cancer / Stage IV Prostate Cancer / Stage IVA Prostate Cancer / Stage IVB Prostate Cancer1
1WithdrawnTreatmentAdvanced Malignancies1
1, 2Active Not RecruitingTreatmentGlioblastomas1
1, 2Active Not RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1, 2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Prostate Cancer1
1, 2Active Not RecruitingTreatmentPlasma Cell Myeloma1
1, 2Not Yet RecruitingTreatmentHepatitis B Virus (HBV)1
1, 2RecruitingTreatmentAdvanced Platinum-resistant Fallopian Tube Cancer / Advanced Platinum-resistant Ovarian Cancer / Advanced Platinum-resistant Primary Peritoneal Cancer1
1, 2RecruitingTreatmentDiffuse Intrinsic Pontine Glioma (DIPG) / High Grade Glioma (HGG) / Refractory Central Nervous System Tumor / Refractory Solid Tumors / Relapsed Central Nervous System Tumor / Relapsed Solid Tumors1
1, 2RecruitingTreatmentMalignant Lymphomas1
1, 2RecruitingTreatmentMetastatic Castration Resistant Prostate Cancer1
2Active Not RecruitingTreatmentAdvanced Non-Small Cell Lung Carcinoma / Metastatic Non-Small Cell Lung Carcinoma1
2Not Yet RecruitingTreatmentPancreatic Cancer Metastatic1
2RecruitingTreatmentAdvanced Cutaneous Squamous Cell Carcinoma1
2RecruitingTreatmentAdvanced Cutaneous Squamous Cell Carcinoma / Cutaneous Squamous Cell Carcinoma / Metastatic cutaneous squamous cell carcinoma1
2RecruitingTreatmentAdvanced Head and Neck Squamous Cell Carcinoma / Melanoma and Other Malignant Neoplasms of Skin / Recurrent Head and Neck Squamous Cell Carcinoma / Resectable Head and Neck Squamous Cell Carcinoma / Stage III Cutaneous Squamous Cell Carcinoma of the Head and Neck AJCC v8 / Stage IV Cutaneous Squamous Cell Carcinoma of the Head and Neck AJCC v81
2RecruitingTreatmentBasal Cell Carcinoma (BCC)1
2RecruitingTreatmentCutaneous Squamous Cell Carcinoma1
2RecruitingTreatmentGlioblastomas1
2RecruitingTreatmentHPV16 Positive / Squamous Cell Carcinoma of the Oropharynx1
2RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC) / Hepatocellular,Carcinoma / Lung Cancer Non-Small Cell Cancer (NSCLC)1
2RecruitingTreatmentMetastatic Hormone Refractory Prostate Cancer1
3Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3RecruitingTreatmentCarcinoma,Non-Small-Cell Lung / Lung Cancer Non-Small Cell Cancer (NSCLC) / Lung Carcinomas, Non-Small-Cell1
3RecruitingTreatmentCutaneous Squamous Cell Carcinoma1
3RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3RecruitingTreatmentRecurrent or Metastatic, Platinum-refractory Cervical Cancer1
Not AvailableNo Longer AvailableNot AvailableCutaneous Squamous Cell Carcinoma1
Not AvailableRecruitingNot AvailableCutaneous Squamous Cell Carcinoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
InjectionIntravenous50 mg/1mL
SolutionIntravenous250 mg
SolutionIntravenous350 mg
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Signal transducer activity
Specific Function
Inhibitory cell surface receptor involved in the regulation of T-cell function during immunity and tolerance. Upon ligand binding, inhibits T-cell effector functions in an antigen-specific manner. ...
Gene Name
PDCD1
Uniprot ID
Q15116
Uniprot Name
Programmed cell death protein 1
Molecular Weight
31646.635 Da
References
  1. Migden MR, Rischin D, Schmults CD, Guminski A, Hauschild A, Lewis KD, Chung CH, Hernandez-Aya L, Lim AM, Chang ALS, Rabinowits G, Thai AA, Dunn LA, Hughes BGM, Khushalani NI, Modi B, Schadendorf D, Gao B, Seebach F, Li S, Li J, Mathias M, Booth J, Mohan K, Stankevich E, Babiker HM, Brana I, Gil-Martin M, Homsi J, Johnson ML, Moreno V, Niu J, Owonikoko TK, Papadopoulos KP, Yancopoulos GD, Lowy I, Fury MG: PD-1 Blockade with Cemiplimab in Advanced Cutaneous Squamous-Cell Carcinoma. N Engl J Med. 2018 Jul 26;379(4):341-351. doi: 10.1056/NEJMoa1805131. Epub 2018 Jun 4. [PubMed:29863979]
  2. Authors unspecified: Drug and Device News. P T. 2017 Nov;42(11):665-691. [PubMed:29089720]

Drug created on September 29, 2018 09:41 / Updated on December 13, 2019 17:22