Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 versus reference denosumab in healthy males: A randomized phase I study

Abstract Denosumab is a human IgG2 monoclonal antibody against receptor activator of nuclear factor kappa‐B ligand (RANKL) for the treatment of osteoporosis and bone loss. HLX14 is a proposed biosimilar of denosumab. This randomized, parallel‐group, two‐part, phase I study aimed to compare the pharm...

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Main Authors: Nanyang Li, Nannan Chu, Leilei Zhu, Xiaojie Wu, Qiong Wei, Jiahui Wang, Xuhui Hu, Haoyu Yu, Qingyu Wang, Wei'an Yuan, Kai Huang, Jing Zhang
Format: Article
Language:English
Published: Wiley 2024-12-01
Series:Clinical and Translational Science
Online Access:https://doi.org/10.1111/cts.70089
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author Nanyang Li
Nannan Chu
Leilei Zhu
Xiaojie Wu
Qiong Wei
Jiahui Wang
Xuhui Hu
Haoyu Yu
Qingyu Wang
Wei'an Yuan
Kai Huang
Jing Zhang
author_facet Nanyang Li
Nannan Chu
Leilei Zhu
Xiaojie Wu
Qiong Wei
Jiahui Wang
Xuhui Hu
Haoyu Yu
Qingyu Wang
Wei'an Yuan
Kai Huang
Jing Zhang
author_sort Nanyang Li
collection DOAJ
description Abstract Denosumab is a human IgG2 monoclonal antibody against receptor activator of nuclear factor kappa‐B ligand (RANKL) for the treatment of osteoporosis and bone loss. HLX14 is a proposed biosimilar of denosumab. This randomized, parallel‐group, two‐part, phase I study aimed to compare the pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 with reference denosumab in Chinese healthy adult male participants. In Part 1, participants were randomized 1:1 and given HLX14 or reference denosumab sourced from the European Union (EU). In double‐blind Part 2, participants were randomized 1:1:1:1 to receive HLX14 or denosumab sourced from the United States, EU, or China. All study drugs were administered via subcutaneous injection at a single dose of 60 mg. The primary endpoints were area under the serum drug concentration–time curve from time 0 to the last concentration‐quantifiable time t (AUC0–t), maximum serum drug concentration (Cmax), and area under the serum drug concentration–time curve from time 0 to infinity (AUC0–inf). Twenty‐four participants were randomized in Part 1 and 228 in Part 2. The 90% confidence intervals of geometric mean ratio of AUC0–t, Cmax, and AUC0–inf between HLX14 and denosumab from different sources fell within the pre‐specified similarity margins of 0.80–1.25 (AUC0–t, 0.91–1.13; Cmax, 0.91–1.13; AUC0–inf, 0.91–1.12), demonstrating pharmacokinetic similarity. No notable difference was observed among treatment groups in pharmacodynamics, safety, or immunogenicity. HLX14 demonstrated highly similar pharmacokinetic characteristics with comparable pharmacodynamics, safety, and immunogenicity to denosumab, supporting its further investigation as a potential denosumab biosimilar.
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spelling doaj-art-3d24eb07e1d64344ab25d11bbe1bb7f12024-12-24T15:26:30ZengWileyClinical and Translational Science1752-80541752-80622024-12-011712n/an/a10.1111/cts.70089Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 versus reference denosumab in healthy males: A randomized phase I studyNanyang Li0Nannan Chu1Leilei Zhu2Xiaojie Wu3Qiong Wei4Jiahui Wang5Xuhui Hu6Haoyu Yu7Qingyu Wang8Wei'an Yuan9Kai Huang10Jing Zhang11Clinical Pharmacology Research Center, Huashan Hospital Fudan University Shanghai ChinaPhase I Clinical Research Center The Affiliated Wuxi People's Hospital of Nanjing Medical University Wuxi ChinaPhase I Clinical Research Center Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine Shanghai ChinaClinical Pharmacology Research Center, Huashan Hospital Fudan University Shanghai ChinaClinical Pharmacology Research Center, Huashan Hospital Fudan University Shanghai ChinaShanghai Henlius Biotech, Inc. Shanghai ChinaShanghai Henlius Biotech, Inc. Shanghai ChinaShanghai Henlius Biotech, Inc. Shanghai ChinaShanghai Henlius Biotech, Inc. Shanghai ChinaPhase I Clinical Research Center Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine Shanghai ChinaPhase I Clinical Research Center The Affiliated Wuxi People's Hospital of Nanjing Medical University Wuxi ChinaClinical Pharmacology Research Center, Huashan Hospital Fudan University Shanghai ChinaAbstract Denosumab is a human IgG2 monoclonal antibody against receptor activator of nuclear factor kappa‐B ligand (RANKL) for the treatment of osteoporosis and bone loss. HLX14 is a proposed biosimilar of denosumab. This randomized, parallel‐group, two‐part, phase I study aimed to compare the pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 with reference denosumab in Chinese healthy adult male participants. In Part 1, participants were randomized 1:1 and given HLX14 or reference denosumab sourced from the European Union (EU). In double‐blind Part 2, participants were randomized 1:1:1:1 to receive HLX14 or denosumab sourced from the United States, EU, or China. All study drugs were administered via subcutaneous injection at a single dose of 60 mg. The primary endpoints were area under the serum drug concentration–time curve from time 0 to the last concentration‐quantifiable time t (AUC0–t), maximum serum drug concentration (Cmax), and area under the serum drug concentration–time curve from time 0 to infinity (AUC0–inf). Twenty‐four participants were randomized in Part 1 and 228 in Part 2. The 90% confidence intervals of geometric mean ratio of AUC0–t, Cmax, and AUC0–inf between HLX14 and denosumab from different sources fell within the pre‐specified similarity margins of 0.80–1.25 (AUC0–t, 0.91–1.13; Cmax, 0.91–1.13; AUC0–inf, 0.91–1.12), demonstrating pharmacokinetic similarity. No notable difference was observed among treatment groups in pharmacodynamics, safety, or immunogenicity. HLX14 demonstrated highly similar pharmacokinetic characteristics with comparable pharmacodynamics, safety, and immunogenicity to denosumab, supporting its further investigation as a potential denosumab biosimilar.https://doi.org/10.1111/cts.70089
spellingShingle Nanyang Li
Nannan Chu
Leilei Zhu
Xiaojie Wu
Qiong Wei
Jiahui Wang
Xuhui Hu
Haoyu Yu
Qingyu Wang
Wei'an Yuan
Kai Huang
Jing Zhang
Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 versus reference denosumab in healthy males: A randomized phase I study
Clinical and Translational Science
title Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 versus reference denosumab in healthy males: A randomized phase I study
title_full Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 versus reference denosumab in healthy males: A randomized phase I study
title_fullStr Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 versus reference denosumab in healthy males: A randomized phase I study
title_full_unstemmed Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 versus reference denosumab in healthy males: A randomized phase I study
title_short Pharmacokinetics, pharmacodynamics, safety, and immunogenicity of HLX14 versus reference denosumab in healthy males: A randomized phase I study
title_sort pharmacokinetics pharmacodynamics safety and immunogenicity of hlx14 versus reference denosumab in healthy males a randomized phase i study
url https://doi.org/10.1111/cts.70089
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