Avelumab

Identification

Summary

Avelumab is an anti-PD-L1 monoclonal antibody used to treat metastatic merkel cell carcinoma, metastatic urothelial carcinoma, or renal cell carcinoma.

Brand Names

Bavencio

Generic Name

Avelumab

DrugBank Accession Number

DB11945

Background

Avelumab is a human IgG1 lambda monoclonal antibody that binds programmed cell death ligand-1 (PD-L1) to block its interaction with its receptors found on T cells and antigen-presenting cells.³ Avelumab was first approved by the FDA on March 23, 2017.³ On September 18 and December 18 of the same year, it was also granted approval by EMA ⁸ and Health Canada,⁹ respectively. It is used in the treatment of Merkel cell carcinoma, metastatic urothelial carcinoma, or renal cell carcinoma.

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Monoclonal antibody (mAb)

Protein Chemical Formula

C₆₃₇₄H₉₈₉₈N₁₆₉₄O₂₀₁₀S₄₄

Protein Average Weight

147000.0 Da (approximate including glycans)

Sequences

>Heavy chain
EVQLLESGGGLVQPGGSLRLSCAASGFTFSSYIMMWVRQAPGKGLEWVSSIYPSGGITFY
ADTVKGRFTISRDNSKNTLYLQMNSLRAEDTAVYYCARIKLGTVTTVDYWGQGTLVTVSS
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGG
PSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYN
STYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDE
LTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRW
QQGNVFSCSVMHEALHNHYTQKSLSLSPGK

>Light chain
QSALTQPASVSGSPGQSITISCTGTSSDVGGYNYVSWYQQHPGKAPKLMIYDVSNRPSGV
SNRFSGSKSGNTASLTISGLQAEDEADYYCSSYTSSSTRVFGTGTKVTVLGQPKANPTVT
LFPPSSEELQANKATLVCLISDFYPGAVTVAWKADGSPVKAGVETTKPSKQSNNKYAASS
YLSLTPEQWKSHRSYSCQVTHEGSTVEKTVAPTECS

References:

1. KEGG DRUG: Avelumab [Link]

Download FASTA Format

Synonyms

• Avelumab

External IDs

• MSB0010718C

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Pharmacology

Indication

Avelumab is indicated for the treatment of adults with metastatic Merkel cell carcinoma (MCC).^8,9 In the US, it is also used in patients 12 years and older.⁷

It is also indicated as the maintenance treatment in patients with locally advanced or metastatic urothelial carcinoma (UC), which has not progressed with first-line platinum-containing chemotherapy.^6,8,9 In the US, avelumab is also indicated to treat locally advanced or metastatic UC with disease progression during or after platinum-containing chemotherapy or within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy.⁶

Avelumab is indicated, in combination with axitinib, for the first-line treatment of advanced renal cell carcinoma (RCC).⁶

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Used in combination to treat	Advanced renal cell carcinoma (arcc)	Regimen in combination with: Axitinib (DB06626)	••••••••••••		••••••••• •••••
Treatment of	Metastatic urothelial cancer		••••••••••••		••••••• ••••••••••• ••••• ••••••••••••••••••• ••••••••••••
Treatment of	Metastatic urothelial cancer		••••••••••••		•••••••• •••••••••• ••••••••••••• •••••••• •••••••••••••• ••••••••••••
Treatment of	Locally advanced urothelial carcinoma		••••••••••••		••••••• ••••••••••• ••••• ••••••••••••••••••• ••••••••••••
Treatment of	Locally advanced urothelial carcinoma		••••••••••••		••••••• ••••••••••• ••••• ••••••••••••••••••• ••••••••••••

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Associated Therapies

• First Line Chemotherapy
• Maintenance therapy

Contraindications & Blackbox Warnings

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Pharmacodynamics

Avelumab is an immunotherapeutic and antineoplastic agent belonging to the immune checkpoint blockade cancer therapies group. It induces antibody-dependent cell-mediated cytotoxicity (ADCC) in vitro;^1,3,7 however it is unclear whether ADCC contributes to the therapeutic actions of avelumab.³ Avelumab decreased tumour growth in syngeneic mouse tumour models.^3,7

Mechanism of action

Programmed death ligand 1 (PD-L1) is a transmembrane protein and a co-inhibitory co-inhibitory immune checkpoint to suppress cytotoxic T-cell activity, proliferation, and cytokine production. It binds to PD receptor-1 (PD-1) and B7.1 receptors expressed on cytotoxic T cells and antigen-presenting cells to mediate its actions. PD-L1 is often expressed in tumours and surrounding tumour-infiltrating immune cells as an adaptive immune mechanism, decreasing the anti-tumour immune response in the tumour microenvironment.^2,3,5,7

Avelumab binds PD-L1 and blocks its interaction with its receptors PD-1 and B7.1, disinhibiting PD-L1 effects on tumour-infiltrating lymphocytes and restoring anti-tumor immune responses.^3,7

Target	Actions	Organism
AProgrammed cell death 1 ligand 1	inhibitor antibody	Humans

Absorption

In patients who received doses ranging from 1 to 20 mg/kg every two weeks, avelumab exposure increased dose proportionally in the dose range of 10 to 20 mg/kg. Steady-state concentrations of avelumab were reached after approximately four to six weeks (two to three cycles) of repeated dosing, and the systemic accumulation was approximately 1.25-fold.⁷

Volume of distribution

The geometric mean volume of distribution at steady state for a subject receiving 10 mg/kg is 4.72 L.⁷ Avelumab is expected to be distributed in the systemic circulation and, to a lesser extent, in the extracellular space.⁹

Protein binding

Not Available

Metabolism

Avelumab undergoes nonspecific proteolytic degradation.⁷

Route of elimination

Not Available

Half-life

The terminal half-life is approximately 6.1 days in patients with solid tumours receiving 10 mg/kg.⁷

Clearance

The total systemic clearance is approximately 0.59 L/day in patients with solid tumours receiving 10 mg/kg.⁷

Adverse Effects

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Toxicity

There is limited information regarding the LD₅₀ of avelumab. Three patients who received a dose of avelumab that was 5% to 10% above the recommended dose experienced an overdose: the patients reported no symptoms and continued on avelumab therapy without requiring any treatment for the overdose. In the case of an overdose, patients should be closely monitored for signs or symptoms of adverse reactions. The treatment is directed to the management of symptoms.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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abciximab	The risk or severity of adverse effects can be increased when Abciximab is combined with Avelumab.
Adalimumab	The risk or severity of adverse effects can be increased when Adalimumab is combined with Avelumab.
Aducanumab	The risk or severity of adverse effects can be increased when Avelumab is combined with Aducanumab.
Alemtuzumab	The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Avelumab.
Alirocumab	The risk or severity of adverse effects can be increased when Alirocumab is combined with Avelumab.

Food Interactions

• Take with or without food.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Bavencio	Solution	20 mg / mL	Intravenous	Emd Serono, A Division Of Emd Inc., Canada	2017-12-18	Not applicable
Bavencio	Injection, solution, concentrate	20 mg/1mL	Intravenous	EMD Serono, Inc.	2017-03-23	Not applicable
Bavencio	Injection, solution, concentrate	20 mg/mL	Intravenous	Merck Europe B.V.	2020-12-16	Not applicable

Categories

ATC Codes

L01FF04 — Avelumab

• L01FF — PD-1/PDL-1 (Programmed cell death protein 1/death ligand 1) inhibitors
• L01F — MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
• L01 — ANTINEOPLASTIC AGENTS
• L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

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 Ligand-1 Antagonists
• Programmed Death Ligand-1 Blocker
• Programmed Death Ligand-1-directed Antibody Interactions
• 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

KXG2PJ551I

CAS number

1537032-82-8

References

General References

1. Boyerinas B, Jochems C, Fantini M, Heery CR, Gulley JL, Tsang KY, Schlom J: Antibody-Dependent Cellular Cytotoxicity Activity of a Novel Anti-PD-L1 Antibody Avelumab (MSB0010718C) on Human Tumor Cells. Cancer Immunol Res. 2015 Oct;3(10):1148-57. doi: 10.1158/2326-6066.CIR-15-0059. Epub 2015 May 26. [Article]
2. Hamilton G, Rath B: Avelumab: combining immune checkpoint inhibition and antibody-dependent cytotoxicity. Expert Opin Biol Ther. 2017 Apr;17(4):515-523. doi: 10.1080/14712598.2017.1294156. Epub 2017 Feb 22. [Article]
3. Kim ES: Avelumab: First Global Approval. Drugs. 2017 May;77(8):929-937. doi: 10.1007/s40265-017-0749-6. [Article]
4. Collins JM, Gulley JL: Product review: avelumab, an anti-PD-L1 antibody. Hum Vaccin Immunother. 2019;15(4):891-908. doi: 10.1080/21645515.2018.1551671. Epub 2018 Dec 20. [Article]
5. Han Y, Liu D, Li L: PD-1/PD-L1 pathway: current researches in cancer. Am J Cancer Res. 2020 Mar 1;10(3):727-742. eCollection 2020. [Article]
6. FDA Approved Drug Products: BAVENCIO (avelumab) injection, for intravenous use (November 2020) [Link]
7. FDA Approved Drug Products: BAVENCIO (avelumab) injection, for intravenous use (September 2023) [Link]
8. EMA Approved Drug Products: Bavencio (avelumab) Intravenous Infusion [Link]
9. Health Canada Approved Drug Products: BAVENCIO (Avelumab) injection, for intravenous infusion [Link]

External Links

PubChem Substance

347911260

RxNav

1875534

Wikipedia

Avelumab

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	First Line Non-Small Cell Lung Cancer	1
3	Active Not Recruiting	Treatment	Locally Advanced Bladder Urothelial Carcinoma / Locally Advanced Renal Pelvis Urothelial Carcinoma / Locally Advanced Ureter Urothelial Carcinoma / Locally Advanced Urethral Urothelial Carcinoma / Locally advanced Urothelial Carcinoma / Metastatic Renal Pelvis Urothelial Carcinoma / Metastatic Ureter Urothelial Carcinoma / Metastatic Urethral Urothelial Carcinoma / Metastatic Urothelial Carcinoma (UC) / Metastatic Urothelial Carcinoma of the Bladder	1
3	Active Not Recruiting	Treatment	Renal Cell Carcinoma (RCC)	1
3	Active Not Recruiting	Treatment	Solid Tumors	1
3	Active Not Recruiting	Treatment	Squamous Cell Carcinoma of the Head and Neck (SCCHN)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution, concentrate	Intravenous	20 mg/mL
Injection, solution, concentrate	Intravenous	20 mg/1mL
Injection, solution, concentrate	Intravenous; Parenteral	20 MG/ML
Solution	Intravenous	20 mg / mL
Solution	Intravenous	200 mg
Injection, solution	Intravenous	200 mg/10ml
Injection, solution, concentrate	Intravenous	200 mg/10ml
Solution	Intravenous	20 mg

Prices

Not Available

Patents

Not Available

Properties

State

Liquid

Experimental Properties

Not Available

Targets

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Details1. Programmed cell death 1 ligand 1

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

Antibody

General Function

Not Available

Specific Function

Involved in the costimulatory signal, essential for T-cell proliferation and production of IL10 and IFNG, in an IL2-dependent and a PDCD1-independent manner. Interaction with PDCD1 inhibits T-cell ...

Gene Name

CD274

Uniprot ID

Q9NZQ7

Uniprot Name

Programmed cell death 1 ligand 1

Molecular Weight

33275.095 Da

References

1. Hamid O, Robert C, Daud A, Hodi FS, Hwu WJ, Kefford R, Wolchok JD, Hersey P, Joseph RW, Weber JS, Dronca R, Gangadhar TC, Patnaik A, Zarour H, Joshua AM, Gergich K, Elassaiss-Schaap J, Algazi A, Mateus C, Boasberg P, Tumeh PC, Chmielowski B, Ebbinghaus SW, Li XN, Kang SP, Ribas A: Safety and tumor responses with lambrolizumab (anti-PD-1) in melanoma. N Engl J Med. 2013 Jul 11;369(2):134-44. doi: 10.1056/NEJMoa1305133. Epub 2013 Jun 2. [Article]
2. Kyriakidis I, Vasileiou E, Rossig C, Roilides E, Groll AH, Tragiannidis A: Invasive Fungal Diseases in Children with Hematological Malignancies Treated with Therapies That Target Cell Surface Antigens: Monoclonal Antibodies, Immune Checkpoint Inhibitors and CAR T-Cell Therapies. J Fungi (Basel). 2021 Mar 5;7(3). pii: jof7030186. doi: 10.3390/jof7030186. [Article]
3. FDA Approved Drug Products: BAVENCIO (avelumab) injection, for intravenous use (September 2023) [Link]

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Drug created at October 20, 2016 21:03 / Updated at November 20, 2023 20:11