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Updated: Oct 29, 2025
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Published on: January 7, 2015
Contribution of membrane transporters to chemotherapy-induced cardiotoxicity
Muhammad Erfan Uddin1, Angie Moseley1, Shuiying Hu1
1Division of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, Columbus, Ohio, USA.
Abstract:
Membrane transporters play a key role in determining the pharmacokinetic profile, therapeutic safety, and efficacy of many chemotherapeutic drugs by regulating cellular influx and efflux. Rapidly emerging evidence has shown that tissue-specific expression of transporters contributes to local drug accumulation and drug-drug interactions and that functional alterations in these transporters can directly influence an individual's susceptibility to drug-induced toxicity. Comprehending the complex mechanism of transporter function in regulating drug distribution in tissues, such as the heart, is necessary in order to acquire novel therapeutic strategies aimed at evading unwanted drug accumulation and toxicities and to ameliorate the safety of current therapeutic regimens. Here, we provide an overview of membrane transporters with a role in chemotherapy-induced cardiotoxicity and discuss novel strategies to improve therapeutic outcomes.
Insights
Membrane transporters regulate chemotherapy drug distribution, impacting safety and efficacy. Understanding their role in cardiotoxicity is crucial for developing safer treatments and reducing drug side effects.
Area of Science:
- Pharmacology
- Molecular Biology
- Cardiology
Background:
- Membrane transporters control drug entry and exit in cells, influencing chemotherapy effectiveness and toxicity.
- Tissue-specific transporter expression can lead to localized drug accumulation and interactions, affecting patient outcomes.
- Altered transporter function is linked to increased susceptibility to drug-induced toxicities.
Purpose of the Study:
- To provide an overview of membrane transporters involved in chemotherapy-induced cardiotoxicity.
- To discuss novel strategies for improving therapeutic outcomes by targeting these transporters.
Main Methods:
- Literature review of studies on membrane transporters and cardiotoxicity.
- Analysis of existing data on transporter function in drug distribution.
- Synthesis of information on emerging therapeutic strategies.
Main Results:
- Membrane transporters significantly impact chemotherapy pharmacokinetics, safety, and efficacy.
- Specific transporters contribute to drug accumulation and toxicity in tissues like the heart.
- Functional transporter alterations increase vulnerability to cardiotoxicity.
Conclusions:
- A comprehensive understanding of transporter mechanisms in the heart is essential for managing chemotherapy-induced cardiotoxicity.
- Targeting membrane transporters offers potential for novel therapeutic strategies to improve treatment safety and efficacy.
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