Fremanezumab: First Global Approval

Hoy, Sheridan M.

doi:10.1007/s40265-018-1004-5

Cited by 45 publications

(44 citation statements)

References 9 publications

(45 reference statements)

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“…Fremanezumab (Ajovy Ò ) is a fully humanized IgG2 monoclonal antibody, approved by the FDA and the European Medicines Agency (EMA) for the prevention of episodic or chronic migraine in adults [76,77]. The drug was produced by Teva Pharmaceuticals via recombinant DNA technology in Chinese hamster ovary (CHO) cells [76].…”

Section: Fremanezumabmentioning

confidence: 99%

“…The drug was produced by Teva Pharmaceuticals via recombinant DNA technology in Chinese hamster ovary (CHO) cells [76]. Fremanezumab selectively binds to and blocks the calcitonin gene-related peptide (CGRP), a neuropeptide that is increased in migraine [76][77][78][79]. The recommended dosage is 225 mg monthly or 675 mg (three consecutive injections of 225 mg each) every 3 months administered subcutaneously in the abdomen, thigh, or upper arm [76].…”

Section: Fremanezumabmentioning

confidence: 99%

“…Fremanezumab needs to be stored in a refrigerator protected from light and should be discarded if it has been at room temperature for 24 h or longer [76]. Randomized placebo-controlled trials in adults with episodic and chronic migraine validated the effectiveness of fremanezumab as preventive therapy for migraine [76,77,[80][81][82][83][84][85]. The most common adverse reactions reported in clinical trials were injection site reactions which include pain, induration, and erythema at the site of injection [76].…”

Section: Fremanezumabmentioning

confidence: 99%

“…The pathophysiology of migraine is linked to activation of the trigeminovascular system, which releases several neuropeptides including CGRP, a 37-amino acid peptide neurotransmitter found in sensory nerves throughout the central and peripheral nervous systems [36,[77][78][79][86][87][88]. CGRP exists in two isoforms, a and b, but since the b form is found in the enteric nervous system, hereafter the paper will focus on a-CGRP, which is a peptide derived from the calcitonin gene on chromosome 11 via alternative mRNA splicing and proteolytic cleavage [75,79,89,90].…”

Section: Cgrp As a Target: Mechanism Of Actionmentioning

confidence: 99%

“…Fremanezumab specifically targets CGRP and prevents it from binding to its receptor, thereby preventing activation of the trigeminovascular pain pathway [36,[77][78][79][86][87][88]. The pharmacological properties of fremanezumab make it a safe and tolerable drug for migraine prophylaxis.…”

Section: Pharmacokinetics and Pharmacodynamicsmentioning

confidence: 99%

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An Evidence-Based Review of Fremanezumab for the Treatment of Migraine

Urits

Clark

et al. 2020

Pain Ther

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Migraine headache is a common, chronic, debilitating disease with a complex etiology. Current therapy for migraine headache comprises either treatments targeting acute migraine pain or prophylactic therapy aimed at increasing the length of time between migraine episodes. Recent evidence suggests that calcium gene-related peptide (CGRP) is a critical component in the pathogenesis of migraines. Fremanezumab, a monoclonal antibody against CGRP, was recently approved by the Food and

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Section: Fremanezumabmentioning

confidence: 99%

Section: Fremanezumabmentioning

confidence: 99%

Section: Fremanezumabmentioning

confidence: 99%

Section: Cgrp As a Target: Mechanism Of Actionmentioning

confidence: 99%

Section: Pharmacokinetics and Pharmacodynamicsmentioning

confidence: 99%

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An Evidence-Based Review of Fremanezumab for the Treatment of Migraine

Urits

Clark

et al. 2020

Pain Ther

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Relationship of the Calcitonin Gene‐Related Peptide Monoclonal Antibody Galcanezumab Pharmacokinetics and Capsaicin‐Induced Dermal Blood Flow in Healthy Subjects

Fiedler‐Kelly

Raddad

Hoon

et al. 2021

Clinical Pharm in Drug Dev

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Galcanezumab, a humanized monoclonal antibody targeting calcitonin gene‐related peptide, was recently approved for migraine prophylaxis. The pharmacokinetic/pharmacodynamic (PK/PD) relationship between galcanezumab concentration and inhibition of capsaicin‐induced dermal blood flow (CIDBF) was evaluated using first‐in‐human data following 6 single subcutaneous doses (1 to 600 mg) or multiple (4) 150‐mg doses every 2 weeks in 7 cohorts (7 actively treated subjects and 2 placebo‐treated healthy subjects). Galcanezumab pharmacokinetics were best described by a 1‐compartment model with delayed first‐order absorption/linear elimination. Apparent estimates (between‐subject variability) of clearance, volume of distribution, absorption rate constant, and lag time were 0.0106 L/h (27%CV), 11.2 L (21%CV), 0.0192 h–1 (89%CV), and 0.202 hours, respectively. Estimated elimination half‐life was about 30 days. An effect compartment link model described the concentration‐effect relationship; estimated maximum inhibitory effect was 70.5%, and 50% maximum inhibitory effect concentration (IC50) was 1060 ng/mL. Galcanezumab showed dose‐ and concentration‐dependent potent and durable inhibition of CIDBF. Simulated effect compartment concentrations were maintained above IC50 after 12 weeks of dosing. Near‐maximal CIDBF inhibition occurred with 150 mg biweekly for 12 weeks lasting ≥24 weeks or with ≥30 mg every 2 weeks or 195 mg every 13 weeks. Quantitative modeling of galcanezumab PK/PD supported dose selection for the phase 2 proof‐of‐concept study.

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