Identification
- Summary
Eptinezumab is a monoclonal antibody directed against CGRP infused every 3 months for the preventive treatment of migraine in adults.
- Brand Names
- Vyepti
- Generic Name
- Eptinezumab
- DrugBank Accession Number
- DB14040
- Background
Eptinezumab is a fully-humanized IgG1 antibody manufactured using yeast (Pichia pastoris) and developed by Lundbeck Seattle Biopharmaceuticals.7 Eptinezumab has been specifically designed to bind to both alpha and beta forms of the human calcitonin gene-related peptide (CGRP).8,1,2,3 It was approved by the FDA in February 2020 for the preventive treatment of migraine headaches in adults.7
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- Not Available
- Protein Average Weight
- 143000.0 Da
- Sequences
>eptinezumab|Heavy EVQLVESGGGLVQPGGSLRLSCAVSGIDLSGYYMNWVRQAPGKGLEWVGVIGINGATYYA SWAKGRFTISRDNSKTTVYLQMNSLRAEDTAVYFCARGDIWGQGTLVTVSSASTKGPSVF PLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVV TVPSSSLGTQTYICNVNHKPSNTKVDARVEPKSCDKTHTCPPCPAPELLGGPSVTLFPPK PKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYASTYRVVSVL TVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLT CLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCS VMHEALHNHYTQKSLSLSPGK
>eptinezumab|Light QVLTQSPSSLSASVGDRVTINCQASQSVYHNTYLAWYQQKPGKVPKQLIYDASTLASGVP SRFSGSGSGTDFTLTISSLQPEDVATYYCLGSYDCTNGDCFVFGGGTKVEIKRTVAAPSV FIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSL SSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format- Synonyms
- Eptinezumab
Pharmacology
- Indication
Eptinezumab is indicated for the preventive treatment of migraine in adults.7
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Eptinezumab is experimentally administered as an intravenous infusion and/or subcutaneous injection 1,3. During Phase 3 clinical trials, it was noted that patients with episodic migraine who on average had 8.6 days of migraine per month demonstrated significant reductions in migraine frequency over weeks 1-12, associated with the 300mg dose arm.6 Additionally, 29.7% of patients achieved a 75% or greater reduction in migraine days from baseline, compared to 16.2% for placebo (p<0.0007).6 Moreover, a post hoc analysis revealed that those patients achieving a 75% or greater response rate had over an eight-fold increase in days between migraines.6
- Mechanism of action
Eptinezumab is a fully-humanized IgG1 antibody manufactured and designed specifically to bind both alpha and beta forms of the human calcitonin gene-related peptide (CGRP).8,1,2,3,5
Studies since 1985 have demonstrated that CGRP levels increase during acute migraine attacks in migraine-suffering patients but normalize after efficacious sumatriptan therapy.4 Moreover, research has also shown that intravenous administration of CGRP can induce migraine-like attacks in migraine-suffering patients.4 For all these reasons, the binding of CGRP to interfere with its activity was specifically designed to be the form and mechanism of action for eptinezumab. The binding of eptinezumab to natural endogenous CGRP subsequently interferes with its activities, such as its binding to CGRP receptors, for example.
Target Actions Organism ACalcitonin gene-related peptide 1 binderantibodyHumans ACalcitonin gene-related peptide 2 binderantibodyHumans - Absorption
Eptinezumab is the only potent and selective and anti-calcitonin gene-related peptide (CGRP) monoclonal antibody administered by quarterly infusion for migraine prevention delivering 100% bioavailability by way of the intravenous route of administration to immediately inhibit CGRP .6
With an intravenous dose of eptinezumab 1000 mg, the mean maximum concentration of 336.4 ug/mL (SD 79.9) occurred after 4.8 hours after the start of the 1 hour infusion 3. The mean exposure to free eptinezumab, as characterized by area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration and from time zero to infinity were 8245 days per ug per mL (SD 2619) and 8722 days per ug per mL (SD 2522), respectively 3.
- Volume of distribution
The central volume of distribution for eptinezumab is approximately 3.7 L.7
- Protein binding
Readily accessible data regarding the protein binding of eptinezumab is not available.
- Metabolism
Monoclonal antibody agents like eptinezumab are not expected to generate toxic metabolites as they generally undergo proteolysis to their constituent amino acids.8
- Route of elimination
Monoclonal antibody agents like eptinezumab are generally not eliminated via hepatic, renal, or biliary routes.8
- Half-life
The plasma half-life after an intravenous infusion is approximately 27 days.7
- Clearance
The apparent clearance of eptinezumab is 0.006 L/h.7
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The most frequent adverse events associated with eptinezumab use include upper respiratory tract infection, urinary tract infection, fatigue, back pain, arthralgia, and nausea and vomiting 3. No data regarding overdosage has been reported yet.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Eptinezumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Eptinezumab. Aducanumab The risk or severity of adverse effects can be increased when Aducanumab is combined with Eptinezumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Eptinezumab. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Eptinezumab. Amivantamab The risk or severity of adverse effects can be increased when Eptinezumab is combined with Amivantamab. Anifrolumab The risk or severity of adverse effects can be increased when Anifrolumab is combined with Eptinezumab. Ansuvimab The risk or severity of adverse effects can be increased when Eptinezumab is combined with Ansuvimab. Anthrax immune globulin human The risk or severity of adverse effects can be increased when Anthrax immune globulin human is combined with Eptinezumab. Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Antilymphocyte immunoglobulin (horse) is combined with Eptinezumab. 
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- 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 Vyepti Injection 100 mg/1mL Intravenous Lundbeck Pharmaceuticals Llc 2020-02-21 Not applicable US 
Vyepti Injection, solution, concentrate 100 mg Intravenous H. Lundbeck A/S 2022-05-04 Not applicable EU 
Vyepti Solution 100 mg / mL Intravenous Lundbeck Inc. 2022-08-17 Not applicable Canada 
Vyepti Injection, solution, concentrate 100 mg Intravenous H. Lundbeck A/S 2023-02-08 Not applicable EU
Categories
- ATC Codes
- N02CD05 — Eptinezumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Analgesics
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antimigraine Preparations
- Blood Proteins
- Calcitonin Gene-Related Peptide (CGRP) Antagonists
- Calcitonin Gene-related Peptide Antagonist
- Globulins
- Immunoglobulins
- Immunoproteins
- Nervous System
- 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
- 8202AY8I7H
- CAS number
- 1644539-04-7
References
- General References
- Pellesi L, Guerzoni S, Pini LA: Spotlight on Anti-CGRP Monoclonal Antibodies in Migraine: The Clinical Evidence to Date. Clin Pharmacol Drug Dev. 2017 Nov;6(6):534-547. doi: 10.1002/cpdd.345. Epub 2017 Apr 14. [Article]
- Benemei S, Cortese F, Labastida-Ramirez A, Marchese F, Pellesi L, Romoli M, Vollesen AL, Lampl C, Ashina M: Triptans and CGRP blockade - impact on the cranial vasculature. J Headache Pain. 2017 Oct 10;18(1):103. doi: 10.1186/s10194-017-0811-5. [Article]
- Dodick DW, Goadsby PJ, Silberstein SD, Lipton RB, Olesen J, Ashina M, Wilks K, Kudrow D, Kroll R, Kohrman B, Bargar R, Hirman J, Smith J: Safety and efficacy of ALD403, an antibody to calcitonin gene-related peptide, for the prevention of frequent episodic migraine: a randomised, double-blind, placebo-controlled, exploratory phase 2 trial. Lancet Neurol. 2014 Nov;13(11):1100-1107. doi: 10.1016/S1474-4422(14)70209-1. Epub 2014 Oct 5. [Article]
- Deen M, Correnti E, Kamm K, Kelderman T, Papetti L, Rubio-Beltran E, Vigneri S, Edvinsson L, Maassen Van Den Brink A: Blocking CGRP in migraine patients - a review of pros and cons. J Headache Pain. 2017 Sep 25;18(1):96. doi: 10.1186/s10194-017-0807-1. [Article]
- Vollbracht S, Rapoport AM: New treatments for headache. Neurol Sci. 2014 May;35 Suppl 1:89-97. doi: 10.1007/s10072-014-1747-z. [Article]
- EconoTimes Business Article: Alder BioPharmaceuticals® New Data Demonstrated Eptinezumab Increased Migraine-Free Intervals (Up to 32.5 days) and Improved Quality-of-Life Outcomes in Patients with Episodic Migraine [Link]
- FDA Approved Drug Products: Vyepti (eptinezumab-jjmr) for intravenous injection [Link]
- Presentation on CGRP, MONOCLONAL ANTIBODIES AND SMALL MOLECULES (-GEPANTS) [File]
- External Links
- 2282660
- Wikipedia
- Eptinezumab
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Recruiting Prevention Medication Overuse Headache / Migraine 1 4 Terminated Treatment Migraine 1 3 Active Not Recruiting Treatment Episodic Cluster Headache 1 3 Active Not Recruiting Treatment Migraine 1 3 Completed Prevention Migraine 3 3 Completed Treatment Chronic Cluster Headache 1 3 Completed Treatment Medication Overuse Headache / Migraine 1 3 Completed Treatment Migraine 2 3 Recruiting Treatment Chronic Migraine in Children 1 3 Recruiting Treatment Migraine 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous 100 mg/1mL Injection, solution, concentrate Intravenous 100 mg Solution Intravenous 100 mg / mL Solution Intravenous 100.00 mg Solution Intravenous drip 100 MG/ML - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- BinderAntibody
- General Function
- Receptor binding
- Specific Function
- CGRP induces vasodilation. It dilates a variety of vessels including the coronary, cerebral and systemic vasculature. Its abundance in the CNS also points toward a neurotransmitter or neuromodulato...
- Gene Name
- CALCA
- Uniprot ID
- P06881
- Uniprot Name
- Calcitonin gene-related peptide 1
- Molecular Weight
- 13897.755 Da
References
- Dodick DW, Goadsby PJ, Silberstein SD, Lipton RB, Olesen J, Ashina M, Wilks K, Kudrow D, Kroll R, Kohrman B, Bargar R, Hirman J, Smith J: Safety and efficacy of ALD403, an antibody to calcitonin gene-related peptide, for the prevention of frequent episodic migraine: a randomised, double-blind, placebo-controlled, exploratory phase 2 trial. Lancet Neurol. 2014 Nov;13(11):1100-1107. doi: 10.1016/S1474-4422(14)70209-1. Epub 2014 Oct 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- BinderAntibody
- General Function
- Neuropeptide hormone activity
- Specific Function
- CGRP induces vasodilation. It dilates a variety of vessels including the coronary, cerebral and systemic vasculature. Its abundance in the CNS also points toward a neurotransmitter or neuromodulato...
- Gene Name
- CALCB
- Uniprot ID
- P10092
- Uniprot Name
- Calcitonin gene-related peptide 2
- Molecular Weight
- 13705.56 Da
References
- Dodick DW, Goadsby PJ, Silberstein SD, Lipton RB, Olesen J, Ashina M, Wilks K, Kudrow D, Kroll R, Kohrman B, Bargar R, Hirman J, Smith J: Safety and efficacy of ALD403, an antibody to calcitonin gene-related peptide, for the prevention of frequent episodic migraine: a randomised, double-blind, placebo-controlled, exploratory phase 2 trial. Lancet Neurol. 2014 Nov;13(11):1100-1107. doi: 10.1016/S1474-4422(14)70209-1. Epub 2014 Oct 5. [Article]
Drug created at May 18, 2018 14:03 / Updated at July 02, 2021 03:58