Rapid LC-MS/MS method for quantifying imatinib in plasma.

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Journal name: World Journal of Pharmaceutical Research
Original article title: Simple and rapid method for the quantification of imatinib mesylate and desmethyl imatinib in human plasma usinglc-ms/ms and its application to routine therapeutic drug monitoring
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Original source:

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Author:

Jose Francis Biswajit Dubashi Rajan Sundaram Suresh Chandra Pradhan Adithan, Chandrasekaran


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Simple and rapid method for the quantification of imatinib mesylate and desmethyl imatinib in human plasma usinglc-ms/ms and its application to routine therapeutic drug monitoring

Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research


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Summary of article contents:

Introduction

Imatinib mesylate is a well-established tyrosine kinase inhibitor used in the treatment of chronic myeloid leukemia (CML), significantly improving patient prognosis. Despite its success, not all patients respond equally to the treatment, often due to pharmacokinetic variability. To address this challenge, therapeutic drug monitoring (TDM) is essential for optimizing treatment regimens, allowing for dose modifications in cases of suboptimal response. The study focused on developing a simple, cost-effective, and rapid method for quantifying imatinib mesylate and its metabolite, desmethyl imatinib, in human plasma using liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS).

Method Development and Validation

The methodology employed a straightforward protein precipitation approach for sample preparation, utilizing an XTerra MS C18 column for effective separation of imatinib and desmethyl imatinib. The analysis was conducted with a triple quadrupole tandem mass spectrometer in positive electrospray ionization mode and used verapamil as an internal standard for its cost-effectiveness and availability. Validation of the method indicated high precision and accuracy within the determined dynamic ranges—5 ng/mL to 8 µg/mL for imatinib and 5 ng/mL to 1 µg/mL for desmethyl imatinib. The method showcased excellent linearity, sensitivity, and stability, indicating its viability for clinical application.

Application in Therapeutic Drug Monitoring

The developed bio-analytical method was applied to TDM for CML patients undergoing imatinib therapy at the Jawaharlal Institute of Postgraduate Medical Education and Research (JIPMER). Data collected over nearly two years showed a total of 119 patients who began treatment, with trough level concentrations assessed for 85 patients who reached steady-state drug levels. The mean trough concentration observed was 1437 ± 459 ng/mL, demonstrating its clinical relevance and alignment with previous findings that recommend maintaining trough levels above 1000 ng/mL for effective therapy.

Advantages of the Method

This study highlights several advantages of the newly developed LC-MS/MS method. By utilizing a readily available and inexpensive internal standard, combined with an uncomplicated extraction process, the method significantly simplifies routine application in a clinical setting. Furthermore, the shorter run times and high stability of the analytes contribute to the efficiency of the monitoring process, which is pivotal in ensuring adherence to therapy and managing potential toxicity in patients receiving imatinib treatment.

Conclusion

In summary, the research successfully established a simple, rapid, and cost-effective method for quantifying imatinib mesylate and its metabolite in human plasma, providing a valuable tool for therapeutic drug monitoring in clinical practice. The validation demonstrated that this method meets essential analytical criteria and could facilitate personalized medicine approaches, aiding in treatment optimization by allowing healthcare providers to adjust dosing regimens based on individual pharmacokinetics. This methodological advancement is particularly significant in managing chronic myeloid leukemia, ensuring patients receive the most effective therapeutic interventions.

FAQ section (important questions/answers):

What is the purpose of the study on imatinib mesylate?

The study aimed to develop a simple, cost-effective, and rapid method for quantifying imatinib mesylate and its metabolite in human plasma using LC-MS/MS for routine therapeutic drug monitoring.

What are the key findings regarding the method's validation?

The method showed precision and accuracy within the specified dynamic ranges, with a lower limit of quantification of 5 ng/mL, making it suitable for monitoring imatinib levels in patients.

How does the method compare to other analytical techniques?

Unlike other methods, this study used verapamil as an internal standard, offering a lower cost and simplifying the extraction process while maintaining good specificity and sensitivity.

What were the mean trough levels found in chronic myeloid leukemia patients?

The study found that the mean trough level concentration for imatinib in patients was 1437±459 ng/mL, with a range from 781.7 to 2940.4 ng/mL.

How can the developed method be utilized in clinical settings?

This method can be applied for routine therapeutic drug monitoring to ensure treatment adherence and identify potential toxic effects of imatinib mesylate in CML patients.

What acknowledgments are mentioned regarding the study's support?

The authors acknowledged Naprod Life Sciences Pvt. Ltd. for supplying imatinib mesylate and received support from JIPMER intramural research and SERB research grants.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Rapid LC-MS/MS method for quantifying imatinib in plasma.”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.

1) Drug:
The term 'drug' refers to Imatinib mesylate, an essential pharmaceutical used in treating chronic myeloid leukemia (CML). This study developed a method for measuring this drug and its metabolite in human plasma, aiding in therapeutic drug monitoring, which is crucial for optimizing patient treatment plans and ensuring adherence.

2) India:
India is the geographical context in which this study's research was conducted. The institutions involved are located in Puducherry, India, highlighting the country's role in advancing medical research, particularly regarding therapy for diseases like chronic myeloid leukemia, which poses public health challenges.

3) Water:
Water, specifically Milli-Q water, is a crucial solvent used in the experimental protocols of the study for sample preparation and mobile phase creation. The purity of water impacts the accuracy and reliability of liquid chromatography and mass spectrometry (LC-MS/MS) analyses, which are central to the study's methodology.

4) Puducherry:
Puducherry is the specific location of the Jawaharlal Institute of Postgraduate Medical Education and Research (JIPMER), where the research was conducted. This locale is significant as it embodies the intersection of healthcare and education in India, providing a setting for clinical research and therapeutic advancements.

5) Education:
Education refers to the academic foundation required for researchers to develop and validate complex bio-analytical methods, such as those involving LC-MS/MS. This study's authors' qualifications and training in pharmacology and medical oncology illustrate the necessity of education in advancing healthcare through research.

6) Table:
A table is used in the paper primarily to present the gradient flow of the mobile phase, LLOQ details, or MRM transitions for the analytes and internal standard. Such tables facilitate the clear communication of critical experimental data, contributing to reproducibility and integrity in scientific reporting.

7) Pharmacology:
Pharmacology is the study's overarching discipline, encompassing the action of drugs in biological systems. The research focuses on therapeutic drug monitoring, an essential aspect of pharmacology, particularly with Imatinib mesylate's quantification and its implications for safe and effective treatment of CML patients.

8) Study (Studying):
The study represents a systematic investigation aimed at developing a reliable method for quantifying Imatinib and its metabolite in human plasma. It showcases the application of novel research methodologies that bridge laboratory science and clinical practice, thereby influencing therapeutic approaches in oncology.

9) Measurement:
Measurement is vital to the study, emphasizing the precision of quantifying drug concentrations using the developed LC-MS/MS method. Accurate measurement ensures appropriate drug dosing in patients, critical for efficacy and minimizing side effects, underscoring the importance of robust measurement techniques in pharmacotherapy.

10) Science (Scientific):
Science encompasses the systematic study of the natural world, which is exemplified by this research's application of analytical chemistry and pharmacology. The scientific methods employed contribute to understanding drug behavior in biological contexts, facilitating informed clinical decision-making and enhancing patient outcomes.

11) Life:
Life refers to the biological context of the study, as it investigates drug interactions within human subjects and aims to enhance therapeutic outcomes for patients with chronic myeloid leukemia. The focus on human plasma highlights the research's direct impact on patient health and quality of life.

12) Observation:
Observation in the context of this study relates to the meticulous monitoring of drug levels in patients. Systematic observation is essential for capturing variations in pharmacokinetics and treatment efficacy, thus guiding therapeutic adjustments to optimize patient care and manage chronic conditions effectively.

13) Performance:
Performance pertains to the operational efficacy of the developed LC-MS/MS method in quantifying imatinib and desmethyl imatinib. The method's performance, evaluated in terms of accuracy, precision, and sensitivity, determines its suitability for routine clinical monitoring in CML treatment.

14) Discussion:
Discussion sections in research papers synthesize findings, contextualize results within existing literature, and explore implications for clinical practice. In this study, the discussion evaluates the method's effectiveness, contributing to the broader understanding of therapeutic drug monitoring in chronic myeloid leukemia management.

15) Similarity:
Similarity focuses on the comparison of verapamil as an internal standard with imatinib and desmethyl imatinib. Highlighting similarities in physicochemical properties justifies the choice of verapamil, emphasizing the importance of selecting appropriate standards for improving method reliability in bio-analytical assays.

16) Chandra:
Chandra refers to Suresh Chandra Pradhan, one author listed in the study, who contributed to the research. His expertise in clinical pharmacology is pivotal for the study's credibility, emphasizing the collaborative effort that combines various professional insights to advance therapeutic strategies in oncology.

17) Pradhan:
Pradhan is significant as part of the research team, indicating collaboration among experts in pharmacology and oncology within JIPMER. His role highlights the diversity of expertise necessary for conducting comprehensive research, which is essential for developing new methodologies in drug monitoring.

18) Channel:
Channel refers to the specific pathways or streams through which analyses occur during the LC-MS/MS process. Effective channeling of compounds during the analytical procedures ensures accurate detection and quantification of the drugs, thus enhancing the validity of the study's findings.

19) Quality:
Quality denotes the reliability and accuracy of the developed analytical method. Ensuring high-quality results is paramount for therapeutic drug monitoring, directly impacting patient treatment strategies and health outcomes in chronic myeloid leukemia management.

20) Cancer:
Cancer is the primary focus of the study, specifically chronic myeloid leukemia. The research aims to improve drug monitoring for this condition, reflecting the ongoing efforts in oncology to enhance treatment regimens, patient survival rates, and overall quality of life.

21) Reason:
Reason pertains to the underlying justification for conducting this research, which is to optimize imatinib therapy. The variability in patient responses necessitates a nuanced approach, using pharmacokinetic data to refine treatment strategies and address issues of adherence and efficacy.

22) Powder:
Powder relates to the pure form of imatinib mesylate supplied for the study. The purity and form of the drug are critical for the development of accurate assays, impacting the subsequent drug quantification and the overall validity of the therapeutic monitoring process.

23) Rajan (Rājan, Rājaṉ):
Rajan refers to Rajan Sundaram, an author of this study, whose involvement signifies the contribution of diverse expertise to the research team. His input represents an essential facet of interdisciplinary collaboration in creating effective therapeutic monitoring strategies in pharmacology and oncology.

24) Blood:
Blood plays a pivotal role in this study as the biological matrix from which plasma is derived for analysis. The analysis of blood plasma for drug concentration is key for understanding pharmacokinetics and assessing therapeutic efficacy, highlighting the relevance of blood in clinical research.

25) Pur (Pūr):
Poor refers to the suboptimal treatment outcomes observed in some patients with chronic myeloid leukemia, emphasizing the need for therapeutic drug monitoring. Identifying patients who exhibit poor responses enables personalized medication adjustments, addressing variability in treatment efficacy and enhancing patient management strategies.

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