Population pharmacokinetics and exposure–response analyses of safety (ARIA‐E and isolated ARIA‐H) of lecanemab in subjects with early Alzheimer's disease

Abstract Lecanemab (Leqembi®) was recently approved by health authorities in the United States, Japan, and China to treat early Alzheimer's disease (AD), including patients with mild cognitive impairment (MCI) or mild dementia due to Alzheimer's disease upon confirmation of amyloid beta pa...

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Main Authors: Oneeb Majid, Youfang Cao, Brian A. Willis, Seiichi Hayato, Osamu Takenaka, Bojan Lalovic, Sree Harsha Sreerama Reddy, Natasha Penner, Larisa Reyderman, Sanae Yasuda, Ziad Hussein
Format: Article
Language:English
Published: Wiley 2024-12-01
Series:CPT: Pharmacometrics & Systems Pharmacology
Online Access:https://doi.org/10.1002/psp4.13224
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author Oneeb Majid
Youfang Cao
Brian A. Willis
Seiichi Hayato
Osamu Takenaka
Bojan Lalovic
Sree Harsha Sreerama Reddy
Natasha Penner
Larisa Reyderman
Sanae Yasuda
Ziad Hussein
author_facet Oneeb Majid
Youfang Cao
Brian A. Willis
Seiichi Hayato
Osamu Takenaka
Bojan Lalovic
Sree Harsha Sreerama Reddy
Natasha Penner
Larisa Reyderman
Sanae Yasuda
Ziad Hussein
author_sort Oneeb Majid
collection DOAJ
description Abstract Lecanemab (Leqembi®) was recently approved by health authorities in the United States, Japan, and China to treat early Alzheimer's disease (AD), including patients with mild cognitive impairment (MCI) or mild dementia due to Alzheimer's disease upon confirmation of amyloid beta pathology. Extensively and sparsely sampled PK profiles from 1619 AD subjects and 21,929 serum lecanemab observations from two phase I, one phase II, and one phase III studies were well characterized using a two‐compartment model with first‐order elimination. The final PK model quantified covariate effects of body weight and sex on clearance and central volume of distribution, ADA‐positive status, and albumin on clearance, and of Japanese ethnicity on central and peripheral volumes of distribution. Exposure to lecanemab was comparable between two lecanemab‐manufacturing processes. However, none of the identified covariates in the model had a clinically relevant impact on model‐predicted lecanemab Cmax or AUC at steady state following 10 mg/kg bi‐weekly. Importantly, age, a well‐recognized risk factor for AD, was not found to significantly affect lecanemab PK. The incidence of ARIA‐E as a function of lecanemab exposure was modeled using a logit function with data pooled from 2641 subjects from the phase II and phase III studies, in which a total of 177 incidences of ARIA‐E were observed. The probability of ARIA‐E was significantly correlated with model‐predicted Cmax and predicted to be higher in subjects homozygous for APOE4. The incidence of isolated ARIA‐H was not associated with lecanemab exposure and was similar between placebo and lecanemab‐treated subjects.
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spelling doaj-art-a55a0026de99493fbad772650f77e12c2024-12-16T05:57:55ZengWileyCPT: Pharmacometrics & Systems Pharmacology2163-83062024-12-0113122111212310.1002/psp4.13224Population pharmacokinetics and exposure–response analyses of safety (ARIA‐E and isolated ARIA‐H) of lecanemab in subjects with early Alzheimer's diseaseOneeb Majid0Youfang Cao1Brian A. Willis2Seiichi Hayato3Osamu Takenaka4Bojan Lalovic5Sree Harsha Sreerama Reddy6Natasha Penner7Larisa Reyderman8Sanae Yasuda9Ziad Hussein10Eisai Ltd. Hatfield UKEisai Inc. Nutley New Jersey USAEisai Inc. Nutley New Jersey USAEisai Co., Ltd. Tokyo JapanEisai Co., Ltd. Tokyo JapanEisai Inc. Nutley New Jersey USAEisai Inc. Nutley New Jersey USAEisai Inc. Nutley New Jersey USAEisai Inc. Nutley New Jersey USAEisai Co., Ltd. Tokyo JapanEisai Ltd. Hatfield UKAbstract Lecanemab (Leqembi®) was recently approved by health authorities in the United States, Japan, and China to treat early Alzheimer's disease (AD), including patients with mild cognitive impairment (MCI) or mild dementia due to Alzheimer's disease upon confirmation of amyloid beta pathology. Extensively and sparsely sampled PK profiles from 1619 AD subjects and 21,929 serum lecanemab observations from two phase I, one phase II, and one phase III studies were well characterized using a two‐compartment model with first‐order elimination. The final PK model quantified covariate effects of body weight and sex on clearance and central volume of distribution, ADA‐positive status, and albumin on clearance, and of Japanese ethnicity on central and peripheral volumes of distribution. Exposure to lecanemab was comparable between two lecanemab‐manufacturing processes. However, none of the identified covariates in the model had a clinically relevant impact on model‐predicted lecanemab Cmax or AUC at steady state following 10 mg/kg bi‐weekly. Importantly, age, a well‐recognized risk factor for AD, was not found to significantly affect lecanemab PK. The incidence of ARIA‐E as a function of lecanemab exposure was modeled using a logit function with data pooled from 2641 subjects from the phase II and phase III studies, in which a total of 177 incidences of ARIA‐E were observed. The probability of ARIA‐E was significantly correlated with model‐predicted Cmax and predicted to be higher in subjects homozygous for APOE4. The incidence of isolated ARIA‐H was not associated with lecanemab exposure and was similar between placebo and lecanemab‐treated subjects.https://doi.org/10.1002/psp4.13224
spellingShingle Oneeb Majid
Youfang Cao
Brian A. Willis
Seiichi Hayato
Osamu Takenaka
Bojan Lalovic
Sree Harsha Sreerama Reddy
Natasha Penner
Larisa Reyderman
Sanae Yasuda
Ziad Hussein
Population pharmacokinetics and exposure–response analyses of safety (ARIA‐E and isolated ARIA‐H) of lecanemab in subjects with early Alzheimer's disease
CPT: Pharmacometrics & Systems Pharmacology
title Population pharmacokinetics and exposure–response analyses of safety (ARIA‐E and isolated ARIA‐H) of lecanemab in subjects with early Alzheimer's disease
title_full Population pharmacokinetics and exposure–response analyses of safety (ARIA‐E and isolated ARIA‐H) of lecanemab in subjects with early Alzheimer's disease
title_fullStr Population pharmacokinetics and exposure–response analyses of safety (ARIA‐E and isolated ARIA‐H) of lecanemab in subjects with early Alzheimer's disease
title_full_unstemmed Population pharmacokinetics and exposure–response analyses of safety (ARIA‐E and isolated ARIA‐H) of lecanemab in subjects with early Alzheimer's disease
title_short Population pharmacokinetics and exposure–response analyses of safety (ARIA‐E and isolated ARIA‐H) of lecanemab in subjects with early Alzheimer's disease
title_sort population pharmacokinetics and exposure response analyses of safety aria e and isolated aria h of lecanemab in subjects with early alzheimer s disease
url https://doi.org/10.1002/psp4.13224
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