Literature DB >> 30040076

Neonatal Fc receptor antagonist efgartigimod safely and sustainably reduces IgGs in humans.

Peter Ulrichts1, Antonio Guglietta1, Torsten Dreier1, Tonke van Bragt1, Valérie Hanssens1, Erik Hofman1, Bernhardt Vankerckhoven1, Peter Verheesen1, Nicolas Ongenae1, Valentina Lykhopiy1, F Javier Enriquez1, JunHaeng Cho2, Raimund J Ober2,3, E Sally Ward2,4, Hans de Haard1, Nicolas Leupin1.   

Abstract

BACKGROUND: Intravenous Ig (IVIg), plasma exchange, and immunoadsorption are frequently used in the management of severe autoimmune diseases mediated by pathogenic IgG autoantibodies. These approaches modulating IgG levels can, however, be associated with some severe adverse reactions and a substantial burden to patients. Targeting the neonatal Fc receptor (FcRn) presents an innovative and potentially more effective, safer, and more convenient alternative for clearing pathogenic IgGs.
METHODS: A randomized, double-blind, placebo-controlled first-in-human study was conducted in 62 healthy volunteers to explore single and multiple ascending intravenous doses of the FcRn antagonist efgartigimod. The study objectives were to assess safety, tolerability, pharmacokinetics, pharmacodynamics, and immunogenicity. The findings of this study were compared with the pharmacodynamics profile elicited by efgartigimod in cynomolgus monkeys.
RESULTS: Efgartigimod treatment resulted in a rapid and specific clearance of serum IgG levels in both cynomolgus monkeys and healthy volunteers. In humans, single administration of efgartigimod reduced IgG levels up to 50%, while multiple dosing further lowered IgGs on average by 75% of baseline levels. Approximately 8 weeks following the last administration, IgG levels returned to baseline. Efgartigimod did not alter the homeostasis of albumin or Igs other than IgG, and no serious adverse events related to efgartigimod infusion were observed.
CONCLUSION: Antagonizing FcRn using efgartigimod is safe and results in a specific, profound, and sustained reduction of serum IgG levels. These results warrant further evaluation of this therapeutic approach in IgG-driven autoimmune diseases. TRIAL REGISTRATION: Clinicaltrials.gov NCT03457649. FUNDING: argenx BVBA.

Entities:  

Keywords:  Autoimmune diseases; Autoimmunity; Immunoglobulins; Therapeutics

Mesh:

Substances:

Year:  2018        PMID: 30040076      PMCID: PMC6159959          DOI: 10.1172/JCI97911

Source DB:  PubMed          Journal:  J Clin Invest        ISSN: 0021-9738            Impact factor:   14.808


  53 in total

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Journal:  Leukemia       Date:  2012-05-03       Impact factor: 11.528

3.  Fc Engineering of Human IgG1 for Altered Binding to the Neonatal Fc Receptor Affects Fc Effector Functions.

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Journal:  J Immunol       Date:  2015-04-22       Impact factor: 5.422

4.  Using multifocal plane microscopy to reveal novel trafficking processes in the recycling pathway.

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5.  Comparing the autoantibody levels and clinical efficacy of double filtration plasmapheresis, immunoadsorption, and intravenous immunoglobulin for the treatment of late-onset myasthenia gravis.

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Journal:  Ther Apher Dial       Date:  2010-04       Impact factor: 1.762

6.  The MHC class I-related receptor, FcRn, plays an essential role in the maternofetal transfer of gamma-globulin in humans.

Authors:  M Firan; R Bawdon; C Radu; R J Ober; D Eaken; F Antohe; V Ghetie; E S Ward
Journal:  Int Immunol       Date:  2001-08       Impact factor: 4.823

7.  The transmission of immunity from mother to young and the catabolism of immunoglobulins.

Authors:  F W Brambell
Journal:  Lancet       Date:  1966-11-19       Impact factor: 79.321

8.  The MHC class I-like IgG receptor controls perinatal IgG transport, IgG homeostasis, and fate of IgG-Fc-coupled drugs.

Authors:  Derry C Roopenian; Gregory J Christianson; Thomas J Sproule; Aaron C Brown; Shreeram Akilesh; Nadja Jung; Stefka Petkova; Lia Avanessian; Eun Young Choi; Daniel J Shaffer; Peter A Eden; Clark L Anderson
Journal:  J Immunol       Date:  2003-04-01       Impact factor: 5.422

9.  Rebound and overshoot after plasma exchange in humans.

Authors:  R H Derksen; H J Schuurman; F H Gmelig Meyling; A Struyvenberg; L Kater
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10.  Abnormally short serum half-lives of IgG in beta 2-microglobulin-deficient mice.

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  49 in total

1.  Randomized phase 2 study of FcRn antagonist efgartigimod in generalized myasthenia gravis.

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Journal:  Neurology       Date:  2019-05-22       Impact factor: 9.910

Review 2.  The neonatal Fc receptor: Key to homeostasic control of IgG and IgG-related biopharmaceuticals.

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Review 6.  Clinical Significance of Serum Albumin and Implications of FcRn Inhibitor Treatment in IgG-Mediated Autoimmune Disorders.

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Review 7.  Neonatal Fc Receptor-Targeted Therapies in Neurology.

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8.  FcRn augments induction of tissue factor activity by IgG-containing immune complexes.

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Review 9.  Immune Thrombocytopenia: Recent Advances in Pathogenesis and Treatments.

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Review 10.  Development of Therapeutic Antibodies and Modulating the Characteristics of Therapeutic Antibodies to Maximize the Therapeutic Efficacy.

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