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Tamoxifen Metabolism

Meaning

Tamoxifen Metabolism refers to the biotransformation of the selective estrogen receptor modulator (SERM) Tamoxifen within the body, primarily in the liver, into its active and inactive metabolites. This process is crucial because the drug’s therapeutic efficacy, particularly its anti-estrogenic effect used in breast cancer treatment, is largely dependent on the formation of the highly potent metabolite, endoxifen. The rate and extent of this metabolism are subject to significant inter-individual variability, often due to genetic polymorphisms in the cytochrome P450 enzyme system. Clinical assessment of this metabolic pathway is necessary for optimizing therapeutic outcomes.