Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors

Tamibarotene is a synthetic retinoid that inhibits tumor cell proliferation and promotes differentiation. We previously reported on the safety and tolerability of tamibarotene in patients with recurrent or refractory solid tumors. Therefore, in this study, we aimed to evaluate the pharmacokinetic pr...

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Main Authors: Takuya Azechi, Yutaka Fukaya, Chika Nitani, Junichi Hara, Hiroshi Kawamoto, Tomoaki Taguchi, Kenichi Yoshimura, Akihiro Sato, Naoko Hattori, Toshikazu Ushijima, Toshimi Kimura
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Language:English
Published: MDPI AG 2024-11-01
Series:Current Oncology
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Online Access:https://www.mdpi.com/1718-7729/31/11/527
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author Takuya Azechi
Yutaka Fukaya
Chika Nitani
Junichi Hara
Hiroshi Kawamoto
Tomoaki Taguchi
Kenichi Yoshimura
Akihiro Sato
Naoko Hattori
Toshikazu Ushijima
Toshimi Kimura
author_facet Takuya Azechi
Yutaka Fukaya
Chika Nitani
Junichi Hara
Hiroshi Kawamoto
Tomoaki Taguchi
Kenichi Yoshimura
Akihiro Sato
Naoko Hattori
Toshikazu Ushijima
Toshimi Kimura
author_sort Takuya Azechi
collection DOAJ
description Tamibarotene is a synthetic retinoid that inhibits tumor cell proliferation and promotes differentiation. We previously reported on the safety and tolerability of tamibarotene in patients with recurrent or refractory solid tumors. Therefore, in this study, we aimed to evaluate the pharmacokinetic properties of tamibarotene and construct a precise pharmacokinetic model. We also conducted a non-compartmental analysis and population pharmacokinetic (popPK) analysis based on the results of a phase I study. Targeted pediatric and young adult patients with recurrent or refractory solid tumors were administered tamibarotene at doses of 4, 6, 8, 10, and 12 g/m<sup>2</sup>/day. Serum tamibarotene concentrations were evaluated after administration, and a popPK model was constructed for tamibarotene using Phoenix NLME. During model construction, we considered the influence of various parameters (weight, height, body surface area, and age) as covariates. Notably, 22 participants were included in this study, and 109 samples were analyzed. A two-compartment model incorporating lag time was selected as the base model. In the final model, the body surface area was included as a covariate for apparent total body clearance, the central compartment volume of distribution, and the peripheral compartment volume of distribution. Visual prediction checks and bootstrap analysis confirmed the validity and predictive accuracy of the final model as satisfactory.
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spelling doaj-art-6673ca9bbc854ff79924f0043a2c1b6f2024-11-26T17:59:01ZengMDPI AGCurrent Oncology1198-00521718-77292024-11-0131117155716410.3390/curroncol31110527Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid TumorsTakuya Azechi0Yutaka Fukaya1Chika Nitani2Junichi Hara3Hiroshi Kawamoto4Tomoaki Taguchi5Kenichi Yoshimura6Akihiro Sato7Naoko Hattori8Toshikazu Ushijima9Toshimi Kimura10Department of Pharmacy, Juntendo University Hospital, Bunkyo-ku, Tokyo 113-8431, JapanDepartment of Pharmacy, Juntendo University Hospital, Bunkyo-ku, Tokyo 113-8431, JapanDepartment of Pediatric Hematology/Oncology, Osaka City General Hospital, Osaka 534-0021, Osaka, JapanDepartment of Pediatric Hematology/Oncology, Osaka City General Hospital, Osaka 534-0021, Osaka, JapanDepartment of Pediatric and Allergy, Fujimi Clinic, Ota-ku, Tokyo 143-0015, JapanFukuoka College of Health Sciences, Fukuoka 814-0193, Fukuoka, JapanDepartment of Biostatistics and Health Data Science, Nagoya City University Graduate School of Medical Science, Nagoya 467-8601, Aichi, JapanClinical Research Support Office, National Cancer Center Hospital East, Kashiwa 277-8577, Chiba, JapanDepartment of Epigenomics, Institute for Advanced Life Sciences, Hoshi University, Shinagawa-ku, Tokyo 142-8501, JapanDepartment of Epigenomics, Institute for Advanced Life Sciences, Hoshi University, Shinagawa-ku, Tokyo 142-8501, JapanDepartment of Pharmacy, Juntendo University Hospital, Bunkyo-ku, Tokyo 113-8431, JapanTamibarotene is a synthetic retinoid that inhibits tumor cell proliferation and promotes differentiation. We previously reported on the safety and tolerability of tamibarotene in patients with recurrent or refractory solid tumors. Therefore, in this study, we aimed to evaluate the pharmacokinetic properties of tamibarotene and construct a precise pharmacokinetic model. We also conducted a non-compartmental analysis and population pharmacokinetic (popPK) analysis based on the results of a phase I study. Targeted pediatric and young adult patients with recurrent or refractory solid tumors were administered tamibarotene at doses of 4, 6, 8, 10, and 12 g/m<sup>2</sup>/day. Serum tamibarotene concentrations were evaluated after administration, and a popPK model was constructed for tamibarotene using Phoenix NLME. During model construction, we considered the influence of various parameters (weight, height, body surface area, and age) as covariates. Notably, 22 participants were included in this study, and 109 samples were analyzed. A two-compartment model incorporating lag time was selected as the base model. In the final model, the body surface area was included as a covariate for apparent total body clearance, the central compartment volume of distribution, and the peripheral compartment volume of distribution. Visual prediction checks and bootstrap analysis confirmed the validity and predictive accuracy of the final model as satisfactory.https://www.mdpi.com/1718-7729/31/11/527tamibarotenepopulation pharmacokineticspediatricyoung adult
spellingShingle Takuya Azechi
Yutaka Fukaya
Chika Nitani
Junichi Hara
Hiroshi Kawamoto
Tomoaki Taguchi
Kenichi Yoshimura
Akihiro Sato
Naoko Hattori
Toshikazu Ushijima
Toshimi Kimura
Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors
Current Oncology
tamibarotene
population pharmacokinetics
pediatric
young adult
title Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors
title_full Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors
title_fullStr Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors
title_full_unstemmed Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors
title_short Population Pharmacokinetics of Tamibarotene in Pediatric and Young Adult Patients with Recurrent or Refractory Solid Tumors
title_sort population pharmacokinetics of tamibarotene in pediatric and young adult patients with recurrent or refractory solid tumors
topic tamibarotene
population pharmacokinetics
pediatric
young adult
url https://www.mdpi.com/1718-7729/31/11/527
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