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Imlunestrant (LY3484356) is an investigational, orally bioavailable selective estrogen receptor degrader (SERD) developed by Eli Lilly for the treatment of estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. It functions by binding to the estrogen receptor alpha (ERα), blocking estrogen-mediated signaling and inducing receptor degradation. Carbamazepine is a widely used anticonvulsant and mood stabilizer that acts primarily as a sodium channel blocker. In the context of this specific combination, carbamazepine is utilized as a potent inducer of the cytochrome P450 3A4 (CYP3A4) enzyme to evaluate its impact on the pharmacokinetics of imlunestrant, which is a substrate of CYP3A4. This drug-drug interaction (DDI) assessment is critical for determining dose adjustments and safety profiles when imlunestrant is co-administered with strong enzyme inducers.
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