Drug intelligence / Profile preview

imlunestrant + carbamazepine

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

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.

Other names
LY3484356 + carbamazepine
02

Targets

ESR1 (ERα)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)

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