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Current Drug Metabolism


ISSN (Print): 1389-2002
ISSN (Online): 1875-5453

Systematic Review Article

Review of the Clinical Pharmacokinetics, Efficacy and Safety of Pembrolizumab

Author(s): Ana Homšek, Davorin Radosavljević, Nebojša Miletić, Jelena Spasić, Marija Jovanović, Branislava Miljković, Tatjana Stanojković and Katarina Vučićević*

Volume 23, Issue 6, 2022

Published on: 22 June, 2022

Page: [460 - 472] Pages: 13

DOI: 10.2174/1389200223666220609125013

Price: $65


Background: Treatment of various types of cancer has been improved significantly with the discovery of biological drugs that act as immune checkpoint inhibitors (ICIs). Pembrolizumab is a humanized monoclonal anti- PD-1 antibody currently approved for the treatment of a wide range of tumors, with more indications still being investigated in ongoing clinical trials.

Objective: The aim of this paper is to present all currently available data regarding pembrolizumab pharmacokinetic and pharmacodynamic characteristics. Also, the possibility of using predictive biomarkers to monitor patients during cancer treatment is discussed.

Methods: Database research was carried out (PubMed, ScienceDirect). Information was gathered from original articles, the European Medicines Agency datasheets and results from clinical trials.

Results: This review summarizes present-day knowledge about the pharmacokinetics, different modeling approaches and dosage regimens, efficacy and safety of pembrolizumab and therapeutic monitoring of disease progression.

Conclusion: This review points out consistent pharmacokinetic characteristics of pembrolizumab in various cancer patients, the lack of pharmacokinetic-pharmacodynamic/outcome relationships, and the need for adequate biomarkers to predict treatment success. Hence, there is a clear necessity for more data and experience in order to optimize pembrolizumab treatment for each individual patient.

Keywords: Pembrolizumab, immune checkpoint inhibitors, monoclonal antibody, Target Mediated Drug Disposition (TMDD), pharmacokinetics, PKPD.

Graphical Abstract

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