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15445 details
Primary information
ID15445
Therapeutic IDTh1597
Protein NameFremanezumab
Sequence>Th1597_Fremanezumab EVQLVESGGGLVQPGGSLRLSCAASGFTFSNYWISWVRQAPGKGLEWVAEIRSESDASATHYAEAVKGRFTISRDNAKNSLYLQMNSLRAEDTAVYYCLAYFDYGLAIQNYWGQGTLVTVSSASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSNFGTQTYTCNVDHKPSNTKVDKTVERKCCVECPPCPAPPVAGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGKEYKCKVSNKGLPSSIEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
Molecular Weight148000
Chemical FormulaNA
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeThe 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.[A33125,L11749]
DescriptionFremanezumab is a humanized monoclonal antibody targeted against human calcitonin gene-related peptide (CGRP) for the prevention of migraine headaches.[L11749] It was developed by Teva Pharmaceuticals USA and approved by the FDA in September 2018.[L11779] 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.
Indication/DiseaseFremanezumab is indicated for the preventative treatment of migraine in adults.[L11749]
PharmacodynamicsFremanezumab is a subcutaneous injection that targets the calcitonin gene-related peptide (CGRP) ligand, preventing its binding to the CGRP receptor.[A33114,L11749] It possesses a long duration of action requiring only monthly or quarterly administration and appears well-tolerated in clinical trials.[L11749]
Mechanism of ActionStudies 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].[A33090] Moreover, research has shown that intravenous administration of CGRP can induce migraine-like attacks in migraine-suffering patients.[A33090] 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.[L11749]
ToxicityInformation 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.[L11749]
MetabolismLike other monoclonal antibodies, fremanezumab is expected to undergo enzymatic proteolysis into smaller peptides and amino acids.[L11749]
AbsorptionGeometric 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 [A33125]. GMRs for AUC (0-inf) were 0.96, 1.09, and 0.98, respectively [A33125]. Mean Tmax in a range of 5 to 11 days were similar across doses for both ethnicities as well [A33125].
Fremanezumab has an apparent volume of distribution of approximately 6 liters which indicates very little distribution into tissue.[L11749]
ClearanceThe apparent clearance of fremanezumab is 0.141 L/day.[L11749]
CategoriesAntibodies, Monoclonal, Humanized
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetCalcitonin gene-related peptide 1,Calcitonin gene-related peptide 2
Brand NameNA
CompanyNA
Brand DescriptionNA
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA