Immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodies

IntroductionImmunogenicity continues to be a challenge for development and clinical utility of monoclonal antibodies, and there are gaps in our current ability to prevent anti-drug antibody development in a safe and antigen-specific manner.MethodsTo mitigate immunogenicity of monoclonal antibodies a...

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Main Authors: Nicole L. Jarvi, Manali Patel, Krithika A. Shetty, Nhan H. Nguyen, Brooke F. Grasperge, Donald E. Mager, Robert M. Straubinger, Sathy V. Balu-Iyer
Format: Article
Language:English
Published: Frontiers Media S.A. 2024-12-01
Series:Frontiers in Immunology
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Online Access:https://www.frontiersin.org/articles/10.3389/fimmu.2024.1496169/full
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author Nicole L. Jarvi
Manali Patel
Krithika A. Shetty
Nhan H. Nguyen
Brooke F. Grasperge
Donald E. Mager
Donald E. Mager
Robert M. Straubinger
Sathy V. Balu-Iyer
author_facet Nicole L. Jarvi
Manali Patel
Krithika A. Shetty
Nhan H. Nguyen
Brooke F. Grasperge
Donald E. Mager
Donald E. Mager
Robert M. Straubinger
Sathy V. Balu-Iyer
author_sort Nicole L. Jarvi
collection DOAJ
description IntroductionImmunogenicity continues to be a challenge for development and clinical utility of monoclonal antibodies, and there are gaps in our current ability to prevent anti-drug antibody development in a safe and antigen-specific manner.MethodsTo mitigate immunogenicity of monoclonal antibodies administered subcutaneously, O-phospho-L-serine (OPLS)—the head group of the tolerance-inducing phospholipid, phosphatidylserine—was investigated as an immunoregulatory adjuvant.ResultsFormulations of adalimumab, trastuzumab or rituximab with OPLS showed reduction in relative immunogenicity in mice compared to vehicle formulations, indicated by reduced anti-drug antibody development and significant reductions in CD138+ plasma cell differentiation in bone marrow. Titer development toward recombinant human hyaluronidase, a dispersion enhancer that was co-formulated with monoclonal antibodies, was similarly reduced. Subcutaneous administration of adalimumab with OPLS resulted in a two-fold increase in expression of type 1 regulatory (Tr1) T cell subset in the spleen. This is consistent with in vitro studies where co-culturing of dendritic cells primed with ovalbumin in the presence and absence of OPLS and antigen specific T-cells induced expression of Tr1 phenotype on live CD4+ T cells.ConclusionThis adjuvant does not impact immune competence of non-human primates and mice, and repeated administration of the adjuvant does not show renal or hepatic toxicity. Formulation of monoclonal antibodies with the immunoregulatory adjuvant, OPLS, was found to be safe and effective at mitigating immunogenicity.
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spelling doaj-art-7c7da71065644d71b0fbb527a18021ab2025-08-20T01:59:17ZengFrontiers Media S.A.Frontiers in Immunology1664-32242024-12-011510.3389/fimmu.2024.14961691496169Immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodiesNicole L. Jarvi0Manali Patel1Krithika A. Shetty2Nhan H. Nguyen3Brooke F. Grasperge4Donald E. Mager5Donald E. Mager6Robert M. Straubinger7Sathy V. Balu-Iyer8Department of Pharmaceutical Sciences, University at Buffalo, The State University of New York, Buffalo, NY, United StatesDepartment of Pharmaceutical Sciences, University at Buffalo, The State University of New York, Buffalo, NY, United StatesDepartment of Pharmaceutical Sciences, University at Buffalo, The State University of New York, Buffalo, NY, United StatesTruvai Biosciences, LLC, Buffalo, NY, United StatesDivision of Veterinary Medicine, Tulane National Primate Research Center, Covington, LA, United StatesDepartment of Pharmaceutical Sciences, University at Buffalo, The State University of New York, Buffalo, NY, United StatesEnhanced Pharmacodynamics, LLC, Buffalo, NY, United StatesDepartment of Pharmaceutical Sciences, University at Buffalo, The State University of New York, Buffalo, NY, United StatesDepartment of Pharmaceutical Sciences, University at Buffalo, The State University of New York, Buffalo, NY, United StatesIntroductionImmunogenicity continues to be a challenge for development and clinical utility of monoclonal antibodies, and there are gaps in our current ability to prevent anti-drug antibody development in a safe and antigen-specific manner.MethodsTo mitigate immunogenicity of monoclonal antibodies administered subcutaneously, O-phospho-L-serine (OPLS)—the head group of the tolerance-inducing phospholipid, phosphatidylserine—was investigated as an immunoregulatory adjuvant.ResultsFormulations of adalimumab, trastuzumab or rituximab with OPLS showed reduction in relative immunogenicity in mice compared to vehicle formulations, indicated by reduced anti-drug antibody development and significant reductions in CD138+ plasma cell differentiation in bone marrow. Titer development toward recombinant human hyaluronidase, a dispersion enhancer that was co-formulated with monoclonal antibodies, was similarly reduced. Subcutaneous administration of adalimumab with OPLS resulted in a two-fold increase in expression of type 1 regulatory (Tr1) T cell subset in the spleen. This is consistent with in vitro studies where co-culturing of dendritic cells primed with ovalbumin in the presence and absence of OPLS and antigen specific T-cells induced expression of Tr1 phenotype on live CD4+ T cells.ConclusionThis adjuvant does not impact immune competence of non-human primates and mice, and repeated administration of the adjuvant does not show renal or hepatic toxicity. Formulation of monoclonal antibodies with the immunoregulatory adjuvant, OPLS, was found to be safe and effective at mitigating immunogenicity.https://www.frontiersin.org/articles/10.3389/fimmu.2024.1496169/fullprotein therapeuticsimmunogenicityimmune toleranceanti-drug antibodiessubcutaneous administrationformulation
spellingShingle Nicole L. Jarvi
Manali Patel
Krithika A. Shetty
Nhan H. Nguyen
Brooke F. Grasperge
Donald E. Mager
Donald E. Mager
Robert M. Straubinger
Sathy V. Balu-Iyer
Immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodies
Frontiers in Immunology
protein therapeutics
immunogenicity
immune tolerance
anti-drug antibodies
subcutaneous administration
formulation
title Immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodies
title_full Immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodies
title_fullStr Immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodies
title_full_unstemmed Immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodies
title_short Immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodies
title_sort immune regulatory adjuvant approach to mitigate subcutaneous immunogenicity of monoclonal antibodies
topic protein therapeutics
immunogenicity
immune tolerance
anti-drug antibodies
subcutaneous administration
formulation
url https://www.frontiersin.org/articles/10.3389/fimmu.2024.1496169/full
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