NAV

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
References:
  1. KEGG DRUG: Cemiplimab [Link]
Download FASTA Format
Synonyms
  • Cemiplimab
  • Cemiplimab-rwlc
External IDs
  • REGN-2810
  • REGN2810
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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

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofLocally advanced basal cell carcinoma•••••••••••••••••••• ••••••••• •••• •••••••• ••••••• ••••••••••••••••••
Treatment ofLocally advanced basal cell carcinoma••••••••••••••• • ••••••••• ••• •••••••• ••••••• ••••••••• ••••••••••••••••
Treatment ofLocally advanced cutaneous squamous cell carcinoma••••••••••••••• • ••••••••• ••• •••••••• ••••••• •• ••••••••••••••••••
Treatment ofLocally advanced non-small cell lung cancer•••••••••••••••••••• • ••••••••• ••• ••••••• •• •••••••••• •••••••••••••••••••••••
Adjunct therapy in treatment ofLocally advanced non-small cell lung cancer•••••••••••••••••••• • ••••••••• ••• ••••••• •• •••••••••• •••••••••••••••••••••••
Associated Therapies
Contraindications & Blackbox Warnings
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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

TargetActionsOrganism
AProgrammed cell death protein 1
inhibitor
antibody
Humans
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
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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.
DrugInteraction
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interactions in your software
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Cemiplimab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Cemiplimab.
AducanumabThe risk or severity of adverse effects can be increased when Aducanumab 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.
Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LibtayoSolution250 mg / 5 mLIntravenousSanofi Aventis2019-05-242023-12-08Canada flag
LibtayoInjection, solution, concentrate350 mgIntravenousRegeneron Ireland Designated Activity Company (Dac)2021-01-12Not applicableEU flag
LibtayoInjection50 mg/1mLIntravenousRegeneron Pharmaceuticals, Inc.2018-09-28Not applicableUS flag
LibtayoSolution350 mg / 7 mLIntravenousSanofi Aventis2019-05-24Not applicableCanada flag

Categories

ATC Codes
L01FF06 — Cemiplimab
Drug Categories
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
  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. [Article]
  2. 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]
  3. 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]
  4. 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]
  5. Drugs.com: FDA Approves Libtayo [Link]
  6. FDA Approved Drug Products: Libtayo (cemiplimab-rwlc) for intravenous injection [Link]
  7. EMA Pending EC decision: Libtayo (cemiplimab) [Link]
  8. EMA Approved Drug Products: LIBTAYO (cemiplimab) intravenous injection [Link]
  9. FDA Approved Drug Products: LIBTAYO (cemiplimab-rwlc) injection, for intravenous use (November 2022) [Link]
RxNav
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);">
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentNon-Small Cell Lung Cancer (NSCLC)1
3Active Not RecruitingTreatmentNon-Small Cell Lung Cancer (NSCLC) / Non-Small Cell Lung Carcinoma1
3CompletedTreatmentRecurrent or Metastatic, Platinum-refractory Cervical Cancer / Squamous Cell Carcinoma (SCC)1
3Not Yet RecruitingTreatmentMelanoma1
3RecruitingTreatmentAdvanced 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
FormRouteStrength
InjectionIntravenous50 mg/1mL
Injection, solution, concentrateIntravenous350 mg
Injection, solution, concentrateIntravenous; Parenteral350 MG
SolutionIntravenous250 mg / 5 mL
SolutionIntravenous350 mg / 7 mL
SolutionIntravenous350.0 mg
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Targets

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Details1. Programmed cell death protein 1
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Antibody
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. [Article]
  2. Authors unspecified: Drug and Device News. P T. 2017 Nov;42(11):665-691. [Article]
  3. 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