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Pharmacogenetics of ATP-binding cassette transporters in cancer and chemotherapy

A Craig Lockhart1, Rommel G Tirona, Richard B Kim

  • 1Department of Medicine, Vanderbilt University Medical Center, Nashville, Tennessee 37232, USA.

Molecular Cancer Therapeutics
|July 29, 2003
PubMed

Insights

ATP-binding cassette (ABC) transporters influence chemotherapy efficacy and toxicity. Genetic variations in these transporters can affect drug response in cancer patients, highlighting their clinical significance.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Genetics

Background:

  • ATP-binding cassette (ABC) transporters constitute the largest gene family, responsible for translocating diverse substrates, including chemotherapy agents.
  • Expression of ABC multidrug transporters is linked to tumor cell resistance to anticancer therapies, altered chemotherapy drug disposition, and treatment-related toxicities.

Purpose of the Study:

  • To review the role of ABC transporters and their genetic polymorphisms in cancer chemotherapy.
  • To explore how genetic heterogeneity in ABC transporter genes impacts drug pharmacokinetics and pharmacodynamics.

Main Methods:

  • Literature review of studies investigating ABC transporters in cancer and chemotherapy.
  • Analysis of research on genetic polymorphisms within ABC transporter genes.

Main Results:

  • ABC transporters play a critical role in mediating resistance to chemotherapy drugs.
  • Genetic variations in ABC transporters can significantly alter the effectiveness and toxicity of cancer treatments.
  • These polymorphisms impact the pharmacokinetics and pharmacodynamics of various chemotherapeutic agents.

Conclusions:

  • Naturally occurring genetic polymorphisms in ABC transporters are important factors in cancer patient outcomes.
  • Understanding these genetic variations is crucial for personalizing chemotherapy regimens and improving treatment efficacy.
  • Targeting ABC transporters or accounting for their genetic variations may offer strategies to overcome drug resistance and reduce toxicity.

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