Toxicokinetics of a humanized anti-cocaine monoclonal antibody in male and female rats and lack of cross-reactivity

A humanized monoclonal antibody h2E2 designed to bind cocaine with high affinity, specificity, and a long half-life (~7 d in rats) is being developed as a treatment for cocaine use disorder. We report here a pharmacokinetic (PK) study of h2E2 using male and female rats conducted under a Good Laborat...

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Main Authors: Rose P. Webster, Jordan A. Marckel, Andrew B. Norman
Format: Article
Language:English
Published: Taylor & Francis Group 2023-12-01
Series:Human Vaccines & Immunotherapeutics
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Online Access:https://www.tandfonline.com/doi/10.1080/21645515.2023.2274222
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author Rose P. Webster
Jordan A. Marckel
Andrew B. Norman
author_facet Rose P. Webster
Jordan A. Marckel
Andrew B. Norman
author_sort Rose P. Webster
collection DOAJ
description A humanized monoclonal antibody h2E2 designed to bind cocaine with high affinity, specificity, and a long half-life (~7 d in rats) is being developed as a treatment for cocaine use disorder. We report here a pharmacokinetic (PK) study of h2E2 using male and female rats conducted under a Good Laboratory Practice (GLP) protocol over a dose range of 40 to 1200 mg/kg. The maximum concentration measured in rat plasma (Cmax) varied proportionately to the dose administered in both male and female rats. The terminal elimination half-lives (t1/2β) were not significantly different in male and female rats at all doses tested. Importantly, this study reports pharmacokinetics for a humanized monoclonal antibody at a dose never tested before. h2E2 has a high affinity for cocaine, whereas low or no affinity was demonstrated for cocaine metabolites (all except cocaethylene), endogenous monoamines, and methamphetamine. This demonstrates its specificity and a potential lack of interactions with physiological and endocrine systems. A review of the clinical signs in single-dose toxicity studies in rats revealed no effects on the central nervous, respiratory, or cardiovascular systems following single intravenous doses of 40 to 1200 mg/kg. This study predicts that this monoclonal antibody may be safe and effective in humans.
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spelling doaj-art-11df4beb242d4c0db3e7dcfdfd587cab2025-08-20T02:31:56ZengTaylor & Francis GroupHuman Vaccines & Immunotherapeutics2164-55152164-554X2023-12-0119310.1080/21645515.2023.2274222Toxicokinetics of a humanized anti-cocaine monoclonal antibody in male and female rats and lack of cross-reactivityRose P. Webster0Jordan A. Marckel1Andrew B. Norman2Department of Pharmacology & Systems Physiology, College of Medicine, University of Cincinnati, Cincinnati, OH, USADepartment of Pharmacology & Systems Physiology, College of Medicine, University of Cincinnati, Cincinnati, OH, USADepartment of Pharmacology & Systems Physiology, College of Medicine, University of Cincinnati, Cincinnati, OH, USAA humanized monoclonal antibody h2E2 designed to bind cocaine with high affinity, specificity, and a long half-life (~7 d in rats) is being developed as a treatment for cocaine use disorder. We report here a pharmacokinetic (PK) study of h2E2 using male and female rats conducted under a Good Laboratory Practice (GLP) protocol over a dose range of 40 to 1200 mg/kg. The maximum concentration measured in rat plasma (Cmax) varied proportionately to the dose administered in both male and female rats. The terminal elimination half-lives (t1/2β) were not significantly different in male and female rats at all doses tested. Importantly, this study reports pharmacokinetics for a humanized monoclonal antibody at a dose never tested before. h2E2 has a high affinity for cocaine, whereas low or no affinity was demonstrated for cocaine metabolites (all except cocaethylene), endogenous monoamines, and methamphetamine. This demonstrates its specificity and a potential lack of interactions with physiological and endocrine systems. A review of the clinical signs in single-dose toxicity studies in rats revealed no effects on the central nervous, respiratory, or cardiovascular systems following single intravenous doses of 40 to 1200 mg/kg. This study predicts that this monoclonal antibody may be safe and effective in humans.https://www.tandfonline.com/doi/10.1080/21645515.2023.2274222Cocaine addictionhumanizedh2E2monoclonal antibodypharmacokineticstoxicokinetics
spellingShingle Rose P. Webster
Jordan A. Marckel
Andrew B. Norman
Toxicokinetics of a humanized anti-cocaine monoclonal antibody in male and female rats and lack of cross-reactivity
Human Vaccines & Immunotherapeutics
Cocaine addiction
humanized
h2E2
monoclonal antibody
pharmacokinetics
toxicokinetics
title Toxicokinetics of a humanized anti-cocaine monoclonal antibody in male and female rats and lack of cross-reactivity
title_full Toxicokinetics of a humanized anti-cocaine monoclonal antibody in male and female rats and lack of cross-reactivity
title_fullStr Toxicokinetics of a humanized anti-cocaine monoclonal antibody in male and female rats and lack of cross-reactivity
title_full_unstemmed Toxicokinetics of a humanized anti-cocaine monoclonal antibody in male and female rats and lack of cross-reactivity
title_short Toxicokinetics of a humanized anti-cocaine monoclonal antibody in male and female rats and lack of cross-reactivity
title_sort toxicokinetics of a humanized anti cocaine monoclonal antibody in male and female rats and lack of cross reactivity
topic Cocaine addiction
humanized
h2E2
monoclonal antibody
pharmacokinetics
toxicokinetics
url https://www.tandfonline.com/doi/10.1080/21645515.2023.2274222
work_keys_str_mv AT rosepwebster toxicokineticsofahumanizedanticocainemonoclonalantibodyinmaleandfemaleratsandlackofcrossreactivity
AT jordanamarckel toxicokineticsofahumanizedanticocainemonoclonalantibodyinmaleandfemaleratsandlackofcrossreactivity
AT andrewbnorman toxicokineticsofahumanizedanticocainemonoclonalantibodyinmaleandfemaleratsandlackofcrossreactivity