Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach

ABSTRACT Tislelizumab 200 mg once every 3 weeks (Q3W) is approved for the treatment of multiple cancers. We used a model‐based approach to propose three alternative dosing regimens, 150 mg Q2W, 300 mg Q4W, and 400 mg Q6W, with the aims of providing flexible treatment regimens compatible with backgro...

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Main Authors: Ahsan Rizwan, Hugh Giovinazzo, Tian Yu, Yuying Gao, Kun Wang, Fengyan Xu, Ya Wan, Jun Wang, Srikumar Sahasranaman, Marcia Campbell, Patrick Schnell, Ramil Abdrashitov, William D. Hanley, Nageshwar Budha
Format: Article
Language:English
Published: Wiley 2025-05-01
Series:Clinical and Translational Science
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Online Access:https://doi.org/10.1111/cts.70223
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author Ahsan Rizwan
Hugh Giovinazzo
Tian Yu
Yuying Gao
Kun Wang
Fengyan Xu
Ya Wan
Jun Wang
Srikumar Sahasranaman
Marcia Campbell
Patrick Schnell
Ramil Abdrashitov
William D. Hanley
Nageshwar Budha
author_facet Ahsan Rizwan
Hugh Giovinazzo
Tian Yu
Yuying Gao
Kun Wang
Fengyan Xu
Ya Wan
Jun Wang
Srikumar Sahasranaman
Marcia Campbell
Patrick Schnell
Ramil Abdrashitov
William D. Hanley
Nageshwar Budha
author_sort Ahsan Rizwan
collection DOAJ
description ABSTRACT Tislelizumab 200 mg once every 3 weeks (Q3W) is approved for the treatment of multiple cancers. We used a model‐based approach to propose three alternative dosing regimens, 150 mg Q2W, 300 mg Q4W, and 400 mg Q6W, with the aims of providing flexible treatment regimens compatible with background chemotherapy and/or reducing infusion visits. A previously developed population pharmacokinetic model was used to simulate pharmacokinetic exposure of the alternative regimens. Regulatory guidance on alternative dosing was used to define pharmacokinetics‐based criteria. Alternative doses were selected by simulation, exposure matching, and comparison to the reference regimen of 200 mg Q3W. Deviations from pharmacokinetics‐based criteria were bridged using appropriate safety and efficacy references and exposure–response analyses. All three alternative dosing regimens produced comparable exposures versus 200 mg Q3W. Although simulated peak serum concentration (Cmax) at 300 mg Q4W and 400 mg Q6W was higher versus 200 mg Q3W, this was below the Cmax of the 5 mg/kg Q3W safety reference. And while the trough serum concentration (Ctrough) for 400 mg Q6W was slightly lower versus 200 mg Q3W, it was 10.7% higher than the 2 mg/kg efficacy reference Ctrough, and therefore, within the concentration range in which a flat exposure–efficacy relationship of tislelizumab has been established. Tislelizumab regimens of 150 mg Q2W, 300 mg Q4W, and 400 mg Q6W are expected to result in similar safety and efficacy as 200 mg Q3W.
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spelling doaj-art-4d8a4b193fdc4ec6b922871de526b9ec2025-08-20T03:54:11ZengWileyClinical and Translational Science1752-80541752-80622025-05-01185n/an/a10.1111/cts.70223Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based ApproachAhsan Rizwan0Hugh Giovinazzo1Tian Yu2Yuying Gao3Kun Wang4Fengyan Xu5Ya Wan6Jun Wang7Srikumar Sahasranaman8Marcia Campbell9Patrick Schnell10Ramil Abdrashitov11William D. Hanley12Nageshwar Budha13Clinical Pharmacology and Pharmacometrics BeiGene USA, Inc. San Carlos California USAClinical Pharmacology and Pharmacometrics BeiGene USA, Inc. San Carlos California USAClinical Pharmacology and Pharmacometrics BeiGene USA, Inc. San Carlos California USAPharmacometrics Shanghai Qiangshi Information Technology Co., Ltd. Shanghai ChinaPharmacometrics Shanghai Qiangshi Information Technology Co., Ltd. Shanghai ChinaPharmacometrics Shanghai Qiangshi Information Technology Co., Ltd. Shanghai ChinaScientific Programming BeiGene (Shanghai) Co., Ltd. Shanghai ChinaGlobal Statistics and Data Sciences BeiGene (Beijing), Co., Ltd. Beijing ChinaClinical Pharmacology and Pharmacometrics BeiGene USA, Inc. San Carlos California USARegulatory Affairs BeiGene (Canada) ULC Toronto Ontario CanadaProduct Safety BeiGene USA, Inc. Ridgefield New Jersey USAClinical Development BeiGene USA, Inc. Fulton Maryland USAClinical Pharmacology and Pharmacometrics BeiGene USA, Inc. San Carlos California USAClinical Pharmacology and Pharmacometrics BeiGene USA, Inc. San Carlos California USAABSTRACT Tislelizumab 200 mg once every 3 weeks (Q3W) is approved for the treatment of multiple cancers. We used a model‐based approach to propose three alternative dosing regimens, 150 mg Q2W, 300 mg Q4W, and 400 mg Q6W, with the aims of providing flexible treatment regimens compatible with background chemotherapy and/or reducing infusion visits. A previously developed population pharmacokinetic model was used to simulate pharmacokinetic exposure of the alternative regimens. Regulatory guidance on alternative dosing was used to define pharmacokinetics‐based criteria. Alternative doses were selected by simulation, exposure matching, and comparison to the reference regimen of 200 mg Q3W. Deviations from pharmacokinetics‐based criteria were bridged using appropriate safety and efficacy references and exposure–response analyses. All three alternative dosing regimens produced comparable exposures versus 200 mg Q3W. Although simulated peak serum concentration (Cmax) at 300 mg Q4W and 400 mg Q6W was higher versus 200 mg Q3W, this was below the Cmax of the 5 mg/kg Q3W safety reference. And while the trough serum concentration (Ctrough) for 400 mg Q6W was slightly lower versus 200 mg Q3W, it was 10.7% higher than the 2 mg/kg efficacy reference Ctrough, and therefore, within the concentration range in which a flat exposure–efficacy relationship of tislelizumab has been established. Tislelizumab regimens of 150 mg Q2W, 300 mg Q4W, and 400 mg Q6W are expected to result in similar safety and efficacy as 200 mg Q3W.https://doi.org/10.1111/cts.70223alternative doseanti–PD‐1exposure–responseimmunotherapypharmacokineticspharmacometrics
spellingShingle Ahsan Rizwan
Hugh Giovinazzo
Tian Yu
Yuying Gao
Kun Wang
Fengyan Xu
Ya Wan
Jun Wang
Srikumar Sahasranaman
Marcia Campbell
Patrick Schnell
Ramil Abdrashitov
William D. Hanley
Nageshwar Budha
Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach
Clinical and Translational Science
alternative dose
anti–PD‐1
exposure–response
immunotherapy
pharmacokinetics
pharmacometrics
title Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach
title_full Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach
title_fullStr Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach
title_full_unstemmed Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach
title_short Alternative Dosing Regimens of Tislelizumab Using a Pharmacometrics Model‐Based Approach
title_sort alternative dosing regimens of tislelizumab using a pharmacometrics model based approach
topic alternative dose
anti–PD‐1
exposure–response
immunotherapy
pharmacokinetics
pharmacometrics
url https://doi.org/10.1111/cts.70223
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