Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis

Abstract Introduction Lymphocyte depletion via anti-CD52 monoclonal antibody (mAb) therapy is an effective treatment strategy for relapsing–remitting multiple sclerosis (MS) but is associated with infusion/injection-associated reactions (IARs) and autoimmune-related adverse events (AEs). Gatralimab...

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Main Authors: Fredrik N. Albach, Christian Geier, Christian Keicher, Maximilian G. Posch, Stephan J. Schreiber, Gerald Grütz, Levent Akyüz, Xiaodong Luo, Annaig Le-Halpere, Philippe Truffinet, Frank Wagner
Format: Article
Language:English
Published: Adis, Springer Healthcare 2024-09-01
Series:Neurology and Therapy
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Online Access:https://doi.org/10.1007/s40120-024-00659-w
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author Fredrik N. Albach
Christian Geier
Christian Keicher
Maximilian G. Posch
Stephan J. Schreiber
Gerald Grütz
Levent Akyüz
Xiaodong Luo
Annaig Le-Halpere
Philippe Truffinet
Frank Wagner
author_facet Fredrik N. Albach
Christian Geier
Christian Keicher
Maximilian G. Posch
Stephan J. Schreiber
Gerald Grütz
Levent Akyüz
Xiaodong Luo
Annaig Le-Halpere
Philippe Truffinet
Frank Wagner
author_sort Fredrik N. Albach
collection DOAJ
description Abstract Introduction Lymphocyte depletion via anti-CD52 monoclonal antibody (mAb) therapy is an effective treatment strategy for relapsing–remitting multiple sclerosis (MS) but is associated with infusion/injection-associated reactions (IARs) and autoimmune-related adverse events (AEs). Gatralimab is a next-generation humanized anti-CD52 mAb. Methods Two first-in-human trials were conducted in participants with progressive MS to assess the pharmacodynamics, pharmacokinetics, and safety of gatralimab administered via subcutaneous (SC) and intravenous (IV) routes, and to determine the effect of different comedication regimes on IARs to SC gatralimab. A Phase 1 trial (NCT02282826) included double-blind, placebo-controlled sequential ascending single IV (1, 3.5, and 12 mg) and SC (12, 36, and 60 mg) dose groups. A Phase 1b trial (NCT02977533) involved five groups who received SC gatralimab (36, 48, or 60 mg) and different comedications. A long-term safety (LTS) study (NCT02313285) examined safety and pharmacodynamics over 4 years. Results Gatralimab produced depletion of lymphocytes (dose-dependently) and CD4+ regulatory T cells, with partial repopulation to normal values by approximately 12 months. Peak serum gatralimab concentrations followed dose-proportionality and were delayed by 6.0–7.5 days following SC administration. Treatment-emergent AEs, including IARs, were reported for most participants but were generally of mild or moderate severity, and treatment-emergent serious AEs were mostly MS-related. Methylprednisolone and antihistamine comedications were associated with reduced incidence of fevers and skin and subcutaneous tissue AEs, respectively. During the LTS study, one participant (3.0%) experienced an autoimmune-related AE (Basedow’s disease), and subsequently died from pulmonary sepsis deemed unrelated to gatralimab by the investigator. Conclusions These data show that gatralimab achieves the desired pharmacodynamic effect of lymphocyte depletion followed by repopulation, and has an acceptable safety profile, including low risk of non-MS autoimmunity. Although gatralimab is no longer in development for MS, insights from these trials may inform the development of comedication regimes of future anti-CD52 mAbs and subcutaneous formulations of other lymphocyte-depleting mAbs. Trial registration NCT02282826, NCT02977533, NCT02313285.
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spelling doaj-art-e79ea53e5efa49fd8676ff1f7d2685da2025-08-20T02:50:08ZengAdis, Springer HealthcareNeurology and Therapy2193-82532193-65362024-09-011361607162510.1007/s40120-024-00659-wPhase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple SclerosisFredrik N. Albach0Christian Geier1Christian Keicher2Maximilian G. Posch3Stephan J. Schreiber4Gerald Grütz5Levent Akyüz6Xiaodong Luo7Annaig Le-Halpere8Philippe Truffinet9Frank Wagner10Charité Research Organisation GmbHCharité Research Organisation GmbHCharité Research Organisation GmbHCharité Research Organisation GmbHDepartment of Neurology, Oberhavel ClinicBIH Centre for Regenerative Therapies (BCRT), Immunocheck-Biomarker Unit, Charité–Universitätsmedizin BerlinBIH Centre for Regenerative Therapies (BCRT), Immunocheck-Biomarker Unit, Charité–Universitätsmedizin BerlinSanofiSanofiSanofiCharité Research Organisation GmbHAbstract Introduction Lymphocyte depletion via anti-CD52 monoclonal antibody (mAb) therapy is an effective treatment strategy for relapsing–remitting multiple sclerosis (MS) but is associated with infusion/injection-associated reactions (IARs) and autoimmune-related adverse events (AEs). Gatralimab is a next-generation humanized anti-CD52 mAb. Methods Two first-in-human trials were conducted in participants with progressive MS to assess the pharmacodynamics, pharmacokinetics, and safety of gatralimab administered via subcutaneous (SC) and intravenous (IV) routes, and to determine the effect of different comedication regimes on IARs to SC gatralimab. A Phase 1 trial (NCT02282826) included double-blind, placebo-controlled sequential ascending single IV (1, 3.5, and 12 mg) and SC (12, 36, and 60 mg) dose groups. A Phase 1b trial (NCT02977533) involved five groups who received SC gatralimab (36, 48, or 60 mg) and different comedications. A long-term safety (LTS) study (NCT02313285) examined safety and pharmacodynamics over 4 years. Results Gatralimab produced depletion of lymphocytes (dose-dependently) and CD4+ regulatory T cells, with partial repopulation to normal values by approximately 12 months. Peak serum gatralimab concentrations followed dose-proportionality and were delayed by 6.0–7.5 days following SC administration. Treatment-emergent AEs, including IARs, were reported for most participants but were generally of mild or moderate severity, and treatment-emergent serious AEs were mostly MS-related. Methylprednisolone and antihistamine comedications were associated with reduced incidence of fevers and skin and subcutaneous tissue AEs, respectively. During the LTS study, one participant (3.0%) experienced an autoimmune-related AE (Basedow’s disease), and subsequently died from pulmonary sepsis deemed unrelated to gatralimab by the investigator. Conclusions These data show that gatralimab achieves the desired pharmacodynamic effect of lymphocyte depletion followed by repopulation, and has an acceptable safety profile, including low risk of non-MS autoimmunity. Although gatralimab is no longer in development for MS, insights from these trials may inform the development of comedication regimes of future anti-CD52 mAbs and subcutaneous formulations of other lymphocyte-depleting mAbs. Trial registration NCT02282826, NCT02977533, NCT02313285.https://doi.org/10.1007/s40120-024-00659-wClinical trialDisease-modifying therapiesMultiple sclerosisProgressiveTreatment response
spellingShingle Fredrik N. Albach
Christian Geier
Christian Keicher
Maximilian G. Posch
Stephan J. Schreiber
Gerald Grütz
Levent Akyüz
Xiaodong Luo
Annaig Le-Halpere
Philippe Truffinet
Frank Wagner
Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis
Neurology and Therapy
Clinical trial
Disease-modifying therapies
Multiple sclerosis
Progressive
Treatment response
title Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis
title_full Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis
title_fullStr Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis
title_full_unstemmed Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis
title_short Phase 1 Trials of Gatralimab, a Next-Generation Humanized Anti-CD52 Monoclonal Antibody, in Participants with Progressive Multiple Sclerosis
title_sort phase 1 trials of gatralimab a next generation humanized anti cd52 monoclonal antibody in participants with progressive multiple sclerosis
topic Clinical trial
Disease-modifying therapies
Multiple sclerosis
Progressive
Treatment response
url https://doi.org/10.1007/s40120-024-00659-w
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