NAV

Fremanezumab

Identification

Summary

Fremanezumab is a humanized monoclonal antibody directed against human calcitonin-gene related peptide to prevent migraines.

Brand Names
Ajovy
Generic Name
Fremanezumab
DrugBank Accession Number
DB14041
Background

Fremanezumab is a humanized monoclonal antibody targeted against human calcitonin gene-related peptide (CGRP) for the prevention of migraine headaches.7 It was developed by Teva Pharmaceuticals USA and approved by the FDA in September 2018.8 Along with other recently approved anti-CGRP therapies such as galcanezumab, erenumab, and the oral CGRP antagonist ubrogepant, fremanezumab represents an important step forward in the treatment and prevention of migraine headaches.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Protein Chemical Formula
Not Available
Protein Average Weight
148000.0 Da
Sequences
>fremanezumab|Heavy
EVQLVESGGGLVQPGGSLRLSCAASGFTFSNYWISWVRQAPGKGLEWVAEIRSESDASAT
HYAEAVKGRFTISRDNAKNSLYLQMNSLRAEDTAVYYCLAYFDYGLAIQNYWGQGTLVTV
SSASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQ
SSGLYSLSSVVTVPSSNFGTQTYTCNVDHKPSNTKVDKTVERKCCVECPPCPAPPVAGPS
VFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNST
FRVVSVLTVVHQDWLNGKEYKCKVSNKGLPSSIEKTISKTKGQPREPQVYTLPPSREEMT
KNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSKLTVDKSRWQQ
GNVFSCSVMHEALHNHYTQKSLSLSPGK
>fremanezumab|Light
EIVLTQSPATLSLSPGERATLSCKASKRVTTYVSWYQQKPGQAPRLLIYGASNRYLGIPA
RFSGSGSGTDFTLTISSLEPEDFAVYYCSQSYNYPYTFGQGTKLEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
Synonyms
  • Fremanezumab
External IDs
  • TEV-48125
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Pharmacology

Indication

Fremanezumab is indicated for the preventative treatment of migraine in adults.7

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prevention ofMigraine••••••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Fremanezumab is a subcutaneous injection that targets the calcitonin gene-related peptide (CGRP) ligand, preventing its binding to the CGRP receptor.3,7 It possesses a long duration of action requiring only monthly or quarterly administration and appears well-tolerated in clinical trials.7

Mechanism of action

Studies dating back to 1985 have demonstrated that CGRP levels increase during acute migraine attacks in migraine-suffering patients but normalize after administration of antimigraine therapy such as sumatriptan.4 Moreover, research has shown that intravenous administration of CGRP can induce migraine-like attacks in migraine-suffering patients.4 For these reasons, and despite the fact that their role in migraine headaches has not been entirely elucidated, CGRP and its receptors have become desirable targets for antimigraine therapies. Fremanezumab is a humanized monoclonal antibody directed against endogenous CGRP - it interferes with the activity of CGRP, preventing its downstream effects and ultimately mitigating the development of migraine headaches.7

TargetActionsOrganism
ACalcitonin gene-related peptide 1
binder
antibody
Humans
ACalcitonin gene-related peptide 2
binder
antibody
Humans
Absorption

Geometric mean ratios (GMRs) for Cmax for Japanese and Caucasian study subjects were 0.91, 1.04, and 1.14 for 225 mg, 675 mg, and 900 mg doses of fremanezumab 2. GMRs for AUC (0-inf) were 0.96, 1.09, and 0.98, respectively 2. Mean Tmax in a range of 5 to 11 days were similar across doses for both ethnicities as well 2.

Volume of distribution

Fremanezumab has an apparent volume of distribution of approximately 6 liters which indicates very little distribution into tissue.7

Protein binding

Data regarding protein binding of fremanezumab are not readily available.

Metabolism

Like other monoclonal antibodies, fremanezumab is expected to undergo enzymatic proteolysis into smaller peptides and amino acids.7

Route of elimination

Monoclonal antibody agents like fremanezumab are generally not eliminated via hepatic, renal, or biliary routes.9

Half-life

The mean half-life recorded for fremanezumab was similar across doses for Japanese and Caucasian study subjects and was estimated to be approximately 31-39 days.2,7

Clearance

The apparent clearance of fremanezumab is 0.141 L/day.7

Adverse Effects
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Toxicity

Information regarding overdose of fremanezumab is not readily available. The most common adverse events that led to discontinuation of fremanezumab therapy were injection site reactions including erythema, induration, and pain.7

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
Integrate drug-drug
interactions in your software
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Fremanezumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Fremanezumab.
AducanumabThe risk or severity of adverse effects can be increased when Aducanumab is combined with Fremanezumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Fremanezumab.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Fremanezumab.
Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AjovySolution225 mg / 1.5 mLSubcutaneousTEVA Canada Limited2020-08-04Not applicableCanada flag
AjovyInjection, solution225 mgSubcutaneousTeva2020-12-16Not applicableEU flag
AjovyInjection225 mg/1.5mLSubcutaneousTeva Pharmaceuticals USA, Inc.2020-03-29Not applicableUS flag
AjovyInjection, solution225 mgSubcutaneousTeva2020-12-16Not applicableEU flag
AjovySolution225 mg / 1.5 mLSubcutaneousTEVA Canada Limited2021-04-01Not applicableCanada flag

Categories

ATC Codes
N02CD03 — Fremanezumab
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
PF8K38CG54
CAS number
1655501-53-3

References

General References
  1. 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]
  2. Cohen-Barak O, Weiss S, Rasamoelisolo M, Faulhaber N, Yeung PP, Loupe PS, Yoon E, Gandhi MD, Spiegelstein O, Aycardi E: A phase 1 study to assess the pharmacokinetics, safety, and tolerability of fremanezumab doses (225 mg, 675 mg and 900 mg) in Japanese and Caucasian healthy subjects. Cephalalgia. 2018 Jan 1:333102418771376. doi: 10.1177/0333102418771376. [Article]
  3. 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]
  4. 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]
  5. Monteith D, Collins EC, Vandermeulen C, Van Hecken A, Raddad E, Scherer JC, Grayzel D, Schuetz TJ, de Hoon J: Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the CGRP Binding Monoclonal Antibody LY2951742 (Galcanezumab) in Healthy Volunteers. Front Pharmacol. 2017 Oct 17;8:740. doi: 10.3389/fphar.2017.00740. eCollection 2017. [Article]
  6. JAMA Network: Effect of Fremanezumab Compared With Placebo for Prevention of Episodic Migraine [Link]
  7. FDA Approved Drug Products: Ajovy (fremanezumab-vfrm) subcutaneous injection [Link]
  8. FDA Drug Approval Package: Ajovy (fremanezumab-vfrm) [Link]
  9. Presentation on CGRP, MONOCLONAL ANTIBODIES AND SMALL MOLECULES (-GEPANTS) [File]
RxNav
2056691
Wikipedia
Fremanezumab

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionCoronavirus Disease 2019 (COVID‑19) / Major Depressive Disorder (MDD) / Migraine1
4CompletedSupportive CareMigraine1
4Not Yet RecruitingTreatmentMenstrually Related Migraine / Migraine / Migraine;Menstrual1
4RecruitingOtherMigraine / Sleep disorders and disturbances1
4RecruitingTreatmentBrain Disorders / Migraine / Migraine With Aura / Migraine Without Aura1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionSubcutaneous225 mg/1.5mL
Injection, solutionParenteral; Subcutaneous225 MG
Injection, solutionSubcutaneous225 mg
Injection, solutionSubcutaneous225 mg/1.5mL
SolutionSubcutaneous225 mg / 1.5 mL
SolutionSubcutaneous225.00 mg
Injection, solution225 mg/1.5ml
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

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Details1. Calcitonin gene-related peptide 1
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
Antibody
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
  1. FDA Approved Drug Products: Ajovy (fremanezumab-vfrm) subcutaneous injection [Link]
Details2. Calcitonin gene-related peptide 2
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
Antibody
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
  1. FDA Approved Drug Products: Ajovy (fremanezumab-vfrm) subcutaneous injection [Link]

Drug created at May 18, 2018 14:04 / Updated at June 03, 2022 07:24