The DOI matches its Crossref record; 134 of the 134 references it cites were found in a registry or an index.
Pharmacokinetic considerations related to therapeutic drug monitoring of tacrolimus in kidney transplant patients
Open accessAbstract
INTRODUCTION: Tacrolimus (Tac) is the cornerstone of immunosuppressive therapy after solid organ transplantation and will probably remain so. Excluding belatacept, no new immunosuppressive drugs were registered for the prevention of acute rejection during the last decade. For several immunosuppressive drugs, clinical development halted because they weren't sufficiently effective or more toxic. Areas covered: Current methods of monitoring Tac treatment, focusing on traditional therapeutic drug monitoring (TDM), controversies surrounding TDM, novel matrices, pharmacogenetic and pharmacodynamic monitoring are discussed. Expert opinion: Due to a narrow therapeutic index and large interpatient pharmacokinetic variability, TDM has been implemented for individualization of Tac dose to maintain drug efficacy and minimize the consequences of overexposure. The relationship between predose concentrations and the occurrence of rejection or toxicity is controversial. Acute cellular rejection also occurs when the Tac concentration is within the target range, suggesting that Tac whole blood concentrations don't necessarily correlate with pharmacological effect. Intracellular Tac, the unbound fraction of Tac or pharmacodynamic monitoring could be better biomarkers/tools for adequate Tac exposure - research into this has been promising. Traditional TDM, perhaps following pre-emptive genotyping for Tac-metabolizing enzymes, must suffice for a few years before these strategies can be implemented in clinical practice.
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“Although exhibiting prolonged absorption and multicompartmental pharmacokinetics, t1/2eff has not previously been explored for tacrolimus from LCPT.6,10”
From Evaluation of Effective Half-Life and Its Impact on Time to Steady State for Oral MeltDose Tacrolimus (LCPT) in De Novo Kidney Transplant Recipients (2025) · cites this paper as [10]
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Metadata
- Authors
- Andrews, L. M., Li, Y., De Winter, B. C. M., Shi, Y.-Y., Baan, C. C., Van Gelder, T., & Hesselink, D. A.
- Affiliations
- Erasmus MC (NL)
- Department of Nephrology, West China Hospital of Sichuan University, Chengdu, China
- Corresponding author
- Hesselink, Dennis A.
- ORCID
- Venue
- Expert Opinion on Drug Metabolism & Toxicology
- Publisher
- Informa UK Limited
- Published
- 2017-10-30
- Volume
- 13
- Issue
- 12
- Pages
- 1225-1236
- ISSN
- 1742-5255 (ISSN-L)
- 1744-7607
- OpenAlex
- W2765312142
- Cited by
- 142
- References
- 134
- Citations by year
- 2026: 9 · 2025: 8 · 2024: 16 · 2023: 19 · 2022: 9 · 2021: 17 · 2020: 30 · 2019: 16 · 2018: 9
- FWCI
- 4.00
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Expert Opinion on Drug Metabolism & Toxicology (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- EUR Research Repository (Erasmus University Rotterdam) (submittedVersion, other-oa)
- RePub (Erasmus University Rotterdam) (submittedVersion, other-oa)
- Topics
- Health Sciences › Medicine › Transplantation › Renal Transplantation Outcomes and Treatments
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Pharmacology (medical) › Antibiotics Pharmacokinetics and Efficacy
- Keywords
- tacrolimus, therapeutic drug monitoring, kidney transplantation, immunosuppressive therapy, pharmacokinetics, pharmacogenetics, pharmacodynamic monitoring, acute cellular rejection, individualized dosing, drug toxicity
- MeSH terms
- Dose-Response Relationship, Drug, Genotype, Graft Rejection, Humans, Immunosuppressive Agents, Pharmacogenetics, Kidney Transplantation, Tacrolimus, Drug Monitoring
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