Cemiplimab
Identification
- Summary
Cemiplimab is a programmed death receptor-1 blocking antibody used to treat cutaneous squamous cell carcinoma, basal cell carcinoma, and non-small cell lung cancer.
- Brand Names
- Libtayo
- Generic Name
- Cemiplimab
- DrugBank Accession Number
- DB14707
- Background
Cemiplimab is a fully human monoclonal antibody that works against programmed death receptor-1 (PD-1), which is a negative regulator of T cell function. By blocking PD-1, cemiplimab works to enhance T cell-mediated antitumour responses.6
Cemiplimab was first approved by the FDA on September 28, 2018, as the first FDA-approved treatment for advanced cutaneous squamous cell carcinoma (CSCC).1,2,5 It was later approved to be used in basal cell carcinoma and non-small non-small cell lung cancer.6 Cemiplimab was also approved by the European Commission on June 28, 2019.8 In October 2022, the EMA's Committee for Medicinal Products for Human Use (CHMP) recommended cemiplimab be granted marketing authorization for the treatment of cervical cancer.7
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- C6380H9808N1688O2000S44
- Protein Average Weight
- 146000.0 Da (approximate)
- Sequences
>Cemiplimab heavy chain EVQLLESGGVLVQPGGSLRLSCAASGFTFSNFGMTWVRQAPGKGLEWVSGISGGGRDTYF ADSVKGRFTISRDNSKNTLYLQMNSLKGEDTAVYYCVKWGNIYFDYWGQGTLVTVSSAST KGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLY SLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFLGGPSVFLF PPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVV SVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQV SLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNVF SCSVMHEALHNHYTQKSLSLSLGK
>Cemiplimab light chain DIQMTQSPSSLSASVGDSITITCRASLSINTFLNWYQQKPGKAPNLLIYAASSLHGGVPS RFSGSGSGTDFTLTIRTLQPEDFATYYCQQSSNTPFTFGPGTVVDFRRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA FormatReferences:
- KEGG DRUG: Cemiplimab [Link]
- Synonyms
- Cemiplimab
- Cemiplimab-rwlc
- External IDs
- REGN-2810
- REGN2810
Pharmacology
- Indication
Cemiplimab is indicated to treat:
Locally advanced or metastatic cutaneous squamous cell carcinoma (mCSCC) in patients who are not candidates for curative surgery or curative radiation.6,8
Locally advanced basal cell carcinoma (laBCC) in previously treated patients with a hedgehog pathway inhibitor or for whom a hedgehog pathway inhibitor is not appropriate.6,8
Metastatic basal cell carcinoma (mBCC) in patients who were previously treated with a hedgehog pathway inhibitor or for whom a hedgehog pathway inhibitor is not appropriate. This indication is approved under accelerated approval based on tumour response rate and durability of response. Continued approval for mBCC may be contingent upon verification and description of clinical benefit.6,8
Locally advanced non-small cell lung cancer (NSCLC) in combination with platinum‐based chemotherapy for the first‐line treatment of adults with no EGFR, ALK or ROS1 aberrations, who are not candidates for surgical resection or definitive chemoradiation. It is also indicated to treat metastatic NSCLC in combination with platinum‐based chemotherapy as first-line treatment in adults.9
Locally advanced or metastatic NSCLC as monotherapy for the first-line treatment of adults whose tumours have high PD-L1 expression [Tumor Proportion Score (TPS) ≥ 50%] as determined by an FDA-approved test, with no EGFR, ALK or ROS1 aberrations. Patients with locally advanced NSCLC must not be candidates for surgical resection or definitive chemoradiation.9
Recurrent or metastatic cervical cancer in adults with disease progression on or after platinum-based chemotherapy.8
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Locally advanced basal cell carcinoma •••••••••••• •••••••• ••••••••• •••• •••••••• ••••••• ••••••••• ••••••••• Treatment of Locally advanced basal cell carcinoma •••••••••••• ••• • ••••••••• ••• •••••••• ••••••• ••••••••• ••••••• ••••••••• Treatment of Locally advanced cutaneous squamous cell carcinoma •••••••••••• ••• • ••••••••• ••• •••••••• ••••••• •• ••••••••• ••••••••• Treatment of Locally advanced non-small cell lung cancer •••••••••••• ••••• ••• • ••••••••• ••• ••••••• •• •••••••••• •••••••••••••• ••••••••• Adjunct therapy in treatment of Locally advanced non-small cell lung cancer •••••••••••• ••••• ••• • ••••••••• ••• ••••••• •• •••••••••• •••••••••••••• ••••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Cemiplimab inhibits tumour growth via an immune-mediated mechanism.1,6 Cemiplimab works to promote T cell-mediated immune response against tumours by blocking programmed death-1 (PD-1), a negative regulator of T cells. Cemiplimab targets PD-1 with high affinity and potency.1 In syngeneic mouse tumour models, blocking PD-1 activity by cemiplimab resulted in decreased tumour growth.6
- Mechanism of action
T cells mediate antitumour activity following activation by antigen receptor signalling and CD28 costimulatory signalling.2,3 T cell proliferation and activation are regulated by a number of T cell immune regulatory checkpoints, including programmed death-1 (PD-1).2 PD-1 is an inhibitory co-receptor that is predominantly expressed on the surface of T cells to block T cell activation.2,3,2 Its ligands, PD-L1 and PD-L2, bind to PD-1 to activate downstream signalling cascades that ultimately result in the inhibition of T cell function such as T cell proliferation, cytokine production, and cytotoxicity.6,8 PD-1 receptor signalling pathway serves to maintain tolerance and regulate any ineffective or harmful immune responses; however, PD-1 signalling can also attenuate immune responses in cases where such protection is needed, such as autoimmune disorders and malignancy.3
PD-L1 and PD-L2 are expressed on antigen-presenting cells (APCs) as well as on some types of tumour cells 2,8 as part of an adaptive immune response by tumours.2,4 PD-1 is also upregulated in some cancers, impeding T cell-mediated antitumour activity.6 Cemiplimab is a human PD-1-blocking antibody that binds to PD-1 and blocks its interaction with its ligands. By disinhibiting PD-1 mediated suppression of T cell activity, cemiplimab works to potentiate T cell cytotoxicity against tumours.6
Target Actions Organism AProgrammed cell death protein 1 inhibitorantibodyHumans - Absorption
In a pharmacokinetic study involving patients with various solid tumours, the pharmacokinetics of cemiplimab was linear and dose-proportional in the dose range of 1 mg/kg to 10 mg/kg cemiplimab administered intravenously every two weeks. When cemiplimab was administered at a dose of 350 mg every three weeks, the median steady-state concentrations (coefficient of variation, CV%) of cemiplimab ranged between 61 mg/L (45%) and 171 mg/L (28%).6
Steady-state exposure is achieved after four months of treatment.6
- Volume of distribution
The volume of distribution (coefficient of variation, CV%) of cemiplimab at steady-state is 5.3 L (26%).6
- Protein binding
No information is available.
- Metabolism
As with other monoclonal antibodies, cemiplimab is expected to undergo nonspecific degradation into small peptides and individual amino acids.8
- Route of elimination
No information is available.
- Half-life
The elimination half-life (CV%) at steady state is 20.3 days (29%).6
- Clearance
Cemiplimab clearance (CV%) after the first dose is 0.29 L/day (33%) and decreases over time by 29%, resulting in a steady-state clearance (CLss) (CV%) of 0.2 L/day (40%).6
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
There is limited information regarding acute toxicity and overdose of cemiplimab. In case of overdose, patients should be closely monitored for signs or symptoms of adverse reactions, and appropriate symptomatic treatment should be initiated.8
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Cemiplimab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Cemiplimab. Aducanumab The risk or severity of adverse effects can be increased when Aducanumab is combined with Cemiplimab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Cemiplimab. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Cemiplimab. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Libtayo Solution 250 mg / 5 mL Intravenous Sanofi Aventis 2019-05-24 2023-12-08 Canada Libtayo Injection, solution, concentrate 350 mg Intravenous Regeneron Ireland Designated Activity Company (Dac) 2021-01-12 Not applicable EU Libtayo Injection 50 mg/1mL Intravenous Regeneron Pharmaceuticals, Inc. 2018-09-28 Not applicable US Libtayo Solution 350 mg / 7 mL Intravenous Sanofi Aventis 2019-05-24 Not applicable Canada
Categories
- ATC Codes
- L01FF06 — Cemiplimab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antineoplastic Agents
- Antineoplastic Agents, Immunological
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Cancer immunotherapy
- Globulins
- Immune Checkpoint Inhibitors
- Immunoglobulins
- Immunoproteins
- Immunotherapy
- MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
- Narrow Therapeutic Index Drugs
- PD-1/PDL-1 (Programmed cell death protein 1/death ligand 1) inhibitors
- Programmed Death Receptor-1 Blocking Antibody
- Proteins
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- 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
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 6QVL057INT
- CAS number
- 1801342-60-8
References
- General References
- 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. [Article]
- Jiang Y, Chen M, Nie H, Yuan Y: PD-1 and PD-L1 in cancer immunotherapy: clinical implications and future considerations. Hum Vaccin Immunother. 2019;15(5):1111-1122. doi: 10.1080/21645515.2019.1571892. Epub 2019 Mar 19. [Article]
- Pedoeem A, Azoulay-Alfaguter I, Strazza M, Silverman GJ, Mor A: Programmed death-1 pathway in cancer and autoimmunity. Clin Immunol. 2014 Jul;153(1):145-52. doi: 10.1016/j.clim.2014.04.010. Epub 2014 Apr 26. [Article]
- Lee HT, Lee JY, Lim H, Lee SH, Moon YJ, Pyo HJ, Ryu SE, Shin W, Heo YS: Molecular mechanism of PD-1/PD-L1 blockade via anti-PD-L1 antibodies atezolizumab and durvalumab. Sci Rep. 2017 Jul 17;7(1):5532. doi: 10.1038/s41598-017-06002-8. [Article]
- Drugs.com: FDA Approves Libtayo [Link]
- FDA Approved Drug Products: Libtayo (cemiplimab-rwlc) for intravenous injection [Link]
- EMA Pending EC decision: Libtayo (cemiplimab) [Link]
- EMA Approved Drug Products: LIBTAYO (cemiplimab) intravenous injection [Link]
- FDA Approved Drug Products: LIBTAYO (cemiplimab-rwlc) injection, for intravenous use (November 2022) [Link]
- External Links
- 2058825
- Wikipedia
- Cemiplimab
- FDA label
- Download (239 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Active Not Recruiting Treatment Non-Small Cell Lung Cancer (NSCLC) 1 3 Active Not Recruiting Treatment Non-Small Cell Lung Cancer (NSCLC) / Non-Small Cell Lung Carcinoma 1 3 Completed Treatment Recurrent or Metastatic, Platinum-refractory Cervical Cancer / Squamous Cell Carcinoma (SCC) 1 3 Not Yet Recruiting Treatment Melanoma 1 3 Recruiting Treatment Advanced Solid Tumors / Anal Cancer / Bladder Cancer / Cervical Cancer / Cholangiocarcinoma / Colorectal Cancer / Gastric Cancer / Hepatocellular Carcinoma / Melanoma / Merkel Cell Carcinoma / Non-Small Cell Lung Cancer (NSCLC) / Renal Cancer / Squamous Cell Carcinoma of the Head and Neck (SCCHN) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous 50 mg/1mL Injection, solution, concentrate Intravenous 350 mg Injection, solution, concentrate Intravenous; Parenteral 350 MG Solution Intravenous 250 mg / 5 mL Solution Intravenous 350 mg / 7 mL Solution Intravenous 350.0 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- InhibitorAntibody
- 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
- 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. [Article]
- Authors unspecified: Drug and Device News. P T. 2017 Nov;42(11):665-691. [Article]
- FDA Approved Drug Products: Libtayo (cemiplimab-rwlc) for intravenous injection [Link]
Drug created at September 29, 2018 15:41 / Updated at December 23, 2022 00:49